PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 2475163-12 1989 The spectroscopic properties of the fluorescent probe ethidium have been used to investigate the effect of the mAbs on the interaction of the agonist carbamylcholine with nAChR in membranes. Ethidium 54-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 171-176 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Nicotine 121-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Carbachol 135-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Pancuronium 175-186 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Tubocurarine 191-205 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Salts 248-252 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Sodium Chloride 282-286 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). fitc-alpha-bgt 9-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). fitc-alpha-bgt 9-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 2514612-8 1989 Specific FITC-alpha-BGT binding to the nAChR protein on the optic fibers was inhibited by agonists (e.g., acetylcholine, nicotine, and carbamylcholine) and antagonists (e.g., pancuronium and d-tubocurarine) of the nAChR and was insensitive to high salt concentrations (e.g., 154 mM NaCl). Acetylcholine 106-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2475163-12 1989 The spectroscopic properties of the fluorescent probe ethidium have been used to investigate the effect of the mAbs on the interaction of the agonist carbamylcholine with nAChR in membranes. Carbachol 150-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 171-176 34058639-1 2021 meta-Chlorophenylguanidine (1) is a non-competitive alpha7 nicotinic acetylcholine receptor (nAChR) antagonist. meta-chlorophenylguanidine 0-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 33929716-6 2021 Oxantel pamoate acts locally in the human gastrointestinal tract and binds to the parasite"s nicotinic acetylcholine receptor (nAChR), leading to a spastic paralysis of the worm and subsequent expulsion. oxantel pamoate 0-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-125 33929716-6 2021 Oxantel pamoate acts locally in the human gastrointestinal tract and binds to the parasite"s nicotinic acetylcholine receptor (nAChR), leading to a spastic paralysis of the worm and subsequent expulsion. oxantel pamoate 0-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 34001335-2 2021 We explore how rising global trends in the use nicotine as well as neonics impacts vulnerability, within and across species, and posit that evolutionary conservation at the nicotinic acetylcholine receptor (nAChR) provides an operational strategy map for pathogens and disease. Nicotine 47-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 207-212 34058639-4 2021 To establish a structural basis for the mode of interaction of guanidines 1 and 2, we generated 100 homology models of the halpha7 nAChR. Guanidines 63-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 33917953-7 2021 Studies on dorsal raphe nucleus serotoninergic neurons support the concept that SSRI-induced nAChR inhibition decreases the glutamatergic hyperstimulation observed in stress conditions, which compensates the excessive 5-HT overflow in these neurons and, consequently, ameliorates depression symptoms. Serotonin 218-222 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 33400965-6 2021 The NMDAR-independent LTP may require activation of glutamate metabotropic receptors (mGluR) or ionotropic receptors other than NMDAR such as nicotinic acetylcholine receptor (alpha7-nAChR), serotonin 5-HT3 receptor or calcium-permeable AMPA receptor (CP-AMPAR). Glutamic Acid 52-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 33977560-2 2021 As a step towards assessing if alpha4beta2* nicotinic acetylcholine receptor (nAChR) stimulation improves gait-balance function, we assessed target engagement of the alpha4beta2* nAChR partial agonist varenicline. Varenicline 201-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 33977560-4 2021 alpha4beta2* nAChR occupancy after subacute oral varenicline treatment was measured with [18F]flubatine PET. fluoronorchloroepibatidine 94-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 33917953-9 2021 According to the functional and structural results, SSRIs bind within the nAChR ion channel at high-affinity sites that are spread out between serine and valine rings. Serine 143-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 33917953-9 2021 According to the functional and structural results, SSRIs bind within the nAChR ion channel at high-affinity sites that are spread out between serine and valine rings. Valine 154-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 33284031-0 2021 Nicotine: A Targeted Therapy for Epilepsy Due to nAChR Gene Variants. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 33506493-1 2021 BACKGROUND AND PURPOSE: The alpha7 and alpha4beta2* (* denotes possibly assembly with another subunit) nicotinic acetylcholine receptors (nAChR) are the most abundant nAChR in the mammalian brain. Acetylcholine 113-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 33506493-1 2021 BACKGROUND AND PURPOSE: The alpha7 and alpha4beta2* (* denotes possibly assembly with another subunit) nicotinic acetylcholine receptors (nAChR) are the most abundant nAChR in the mammalian brain. Acetylcholine 113-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 33506493-4 2021 We have developed C(10) variants of cytisine, a partial agonist of alpha4beta2 nAChR that has been used for smoking cessation. cytisine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 33506493-6 2021 EXPERIMENTAL APPROACH: The structural underpinning of the selectivity of 10-methylcytisine for alpha7 and alpha4beta2 nAChR was investigated using molecular dynamics simulations, mutagenesis and whole-cell and single-channel current recordings. 10-methylcytisine 73-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 33506493-7 2021 KEY RESULTS: We identified a conserved arginine in the beta3-strand that exhibits a non-conserved function in nAChR. Arginine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 33506493-8 2021 In alpha4beta2 nAChR, the arginine forms a salt-bridge with an aspartate residue in loop B that is necessary for receptor expression, whereas in alpha7 nAChR, this residue is not stabilised by electrostatic interactions, making its side chain highly mobile. Arginine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 33506493-8 2021 In alpha4beta2 nAChR, the arginine forms a salt-bridge with an aspartate residue in loop B that is necessary for receptor expression, whereas in alpha7 nAChR, this residue is not stabilised by electrostatic interactions, making its side chain highly mobile. Aspartic Acid 63-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 33548485-3 2021 Our study systematically investigates the nicotinic acetylcholine receptor (nAChR) gene family, in order to identify the receptor subunits critical to the insect response to insecticides from three distinct chemical classes (neonicotinoids, spinosyns and sulfoximines). Neonicotinoids 225-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 33548485-3 2021 Our study systematically investigates the nicotinic acetylcholine receptor (nAChR) gene family, in order to identify the receptor subunits critical to the insect response to insecticides from three distinct chemical classes (neonicotinoids, spinosyns and sulfoximines). sulfoximines 255-267 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 33284031-3 2021 In preclinical models, pathogenic nAChR variants cause a gain of function mutation with sensitivity to acetylcholine antagonists and agonists. Acetylcholine 103-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 33284031-10 2021 CONCLUSIONS: Treatment with a nicotine patch can be an effective therapy in epilepsy patients with nAChR gene variants. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 33284031-11 2021 We propose consideration of transdermal nicotine treatment in intractable epilepsy with known nAChR variants as an experimental therapy. Nicotine 40-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 33216167-10 2021 CONCLUSIONS: The finding that nAChR tone reduction by mecamylamine weakened task-induced DMN deactivation indicates that a constant tone of nAChR activation helps regulate DMN activity in healthy individuals. Mecamylamine 54-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 33482275-0 2021 Molecular determinants of binding of non-oxime bispyridinium nerve agent antidote compounds to the adult muscle nAChR. oxime bispyridinium 41-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 33482275-4 2021 Non-oxime bispyridinium compounds (BPDs) have been shown previously to partially counteract the effects of NAs at skeletal muscle tissue, and this has been attributed to inhibition of the muscle nAChR. non-oxime bispyridinium compounds 0-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 33482275-4 2021 Non-oxime bispyridinium compounds (BPDs) have been shown previously to partially counteract the effects of NAs at skeletal muscle tissue, and this has been attributed to inhibition of the muscle nAChR. bpds 35-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 33482275-6 2021 Molecular dynamics simulations of the adult muscle nAChR in the presence of BPDs identified key residues likely to be involved in binding. bpds 76-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 32935187-1 2021 PURPOSES: We present the first in-human brain PET imaging data of the new alpha4beta2 nicotinic acetylcholine receptor (nAChR)-targeting radioligand (+)-[18F]Flubatine. Acetylcholine 96-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 32935187-1 2021 PURPOSES: We present the first in-human brain PET imaging data of the new alpha4beta2 nicotinic acetylcholine receptor (nAChR)-targeting radioligand (+)-[18F]Flubatine. fluoronorchloroepibatidine 158-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 32935187-17 2021 Overall, (+)-[18F]Flubatine showed favorable characteristics and has therefore the potential to serve as alpha4beta2 nAChR-targeting PET ligand in further clinical trials. fluoronorchloroepibatidine 18-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 33422895-4 2021 The results show that mutant LRRK2 prevents the membrane localization of both the dopamine D3 receptors (D3R) and the nicotinic acetylcholine receptors (nAChR) and the formation of the D3R-nAChR heteromer, a molecular unit crucial for promoting neuronal homeostasis and preserving dopaminergic neuron health. Dopamine 82-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 33668830-1 2021 alpha-Conotoxin GeXIVA[1,2] is a highly potent and selective antagonist of the alpha9alpha10 nicotinic acetylcholine receptor (nAChR) subtype. gexiva 16-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 32841724-6 2021 We also identified a novel SNP in the beta4 nAChR subunit, part of the same gene cluster in the human genome and potentially altering CHRNA5 expression, associated with shorter time to relapse to cocaine use in patients. Cocaine 196-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 33823404-0 2021 Synthesis and evaluation of disulfide-rich cyclic alpha-conotoxin [S9A]TxID analogues as novel alpha3beta4 nAChR antagonists. Disulfides 28-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 33823404-0 2021 Synthesis and evaluation of disulfide-rich cyclic alpha-conotoxin [S9A]TxID analogues as novel alpha3beta4 nAChR antagonists. cyclic alpha-conotoxin 43-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 33823404-0 2021 Synthesis and evaluation of disulfide-rich cyclic alpha-conotoxin [S9A]TxID analogues as novel alpha3beta4 nAChR antagonists. s9a 67-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 33823404-0 2021 Synthesis and evaluation of disulfide-rich cyclic alpha-conotoxin [S9A]TxID analogues as novel alpha3beta4 nAChR antagonists. txid 71-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 33836585-0 2021 Acetylcholine ameliorates colitis by promoting IL-10 secretion of monocytic myeloid-derived suppressor cells through the nAChR/ERK pathway. Acetylcholine 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 33836585-5 2021 Furthermore, ACh was demonstrated to promote interleukin-10 secretion of M-MDSCs and suppress the inflammation through activating the nAChR/ERK pathway. Acetylcholine 13-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 33630646-2 2022 Modulated by glutamate neurotransmission, this sensory process has also been shown to relate to the alpha7 nicotinic acetylcholine receptor (nAChR) system, a prioritized molecular target for the development of novel cognition targeted pharmacological treatments. Glutamic Acid 13-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 33380469-5 2021 Using whole-cell recordings, we found that the alpha3beta4* nAChR-selective antagonist alpha-conotoxin AuIB almost completely abolished nicotine-evoked currents in mHb neurons. Nicotine 136-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 33380469-6 2021 By contrast, the alpha3beta2* nAChR-selective antagonist alpha-conotoxin MII only partially attenuated these currents. Methicillin 73-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 33380469-9 2021 These findings provide mechanistic insights into how CHRNA3 risk alleles can increase the risk of tobacco dependence and smoking-related diseases in human smokers.SIGNIFICANCE STATEMENTAllelic variation in CHRNA3, which encodes the alpha3 nicotinic acetylcholine receptor (nAChR) subunit gene, increases risk of tobacco dependence but underlying mechanisms are unclear. Acetylcholine 249-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 273-278 33613194-1 2021 The alpha9alpha10 nicotinic acetylcholine receptor (nAChR) plays a fundamental role in inner ear physiology. Acetylcholine 28-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 33216167-10 2021 CONCLUSIONS: The finding that nAChR tone reduction by mecamylamine weakened task-induced DMN deactivation indicates that a constant tone of nAChR activation helps regulate DMN activity in healthy individuals. Mecamylamine 54-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 32248535-5 2020 On the contrary, PNU-120596 exerted an inhibitory effect on the receptors mediating anion currents in Lymnaea stagnalis neurons: two nAChR subtypes, GABA and glutamate receptors. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 17-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 33276105-2 2021 Choline is also a selective agonist of some neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Choline 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-85 33276105-2 2021 Choline is also a selective agonist of some neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Choline 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 33253222-1 2020 The pathway from the medial habenular nucleus to the interpeduncular nucleus, in which nicotinic acetylcholine receptor (nAChR) including the alpha3 and alpha5 subunits (alpha3 * and alpha5 * nAChRs) are expressed, is implicated in nicotine dependence. Nicotine 232-240 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 33253222-7 2020 The inhibition of alpha3 *, alpha5 *, alpha7 nAChR and voltage-gated Ca2+ channels by using siRNAs and selective antagonists revealed the involvement of these nAChR subunits and channels in nicotine-induced [Ca2+]i elevation. Nicotine 190-198 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 33253222-8 2020 To distinguish and characterize the alpha3 * and alpha5 * nAChR-mediated Ca2+ influx, we measured the [Ca2+]i elevation induced by nonmembrane-permeating acetylcholine when muscarinic receptors, alpha7nAChR and Ca2+ channels were blocked. Acetylcholine 154-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 33074244-1 2020 The alpha6beta4 nicotinic acetylcholine receptor (nAChR) is enriched in dorsal root ganglia neurons and is an attractive non-opioid therapeutic target for pain. Acetylcholine 26-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 33335227-3 2020 Other studies have shown that the stimulation of alpha7 nicotinic acetylcholine receptor (nAChR) can have neuroprotective effects in some models of neurodegenerative disease, as well as prevent glutamate-induced motor neuronal death. Glutamic Acid 194-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 33343327-4 2020 Interestingly, this gene cluster contains a non-synonymous single-nucleotide polymorphism (SNP) in the human CHRNA5 gene, causing an aspartic acid (D) to asparagine (N) substitution at amino acid position 398 in the alpha5 nAChR subunit. Aspartic Acid 133-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 223-228 33253222-10 2020 These findings suggest that alpha3 * and alpha5 * nAChR-mediated Ca2+ influx is possibly regulated by cAMP at the transcriptional level. Cyclic AMP 102-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 33329690-3 2020 Nicotinic acetylcholine receptor (nAChR) is a ligand-gated Ca2+/Na+ channel, and its opening is the first signaling event leading to catecholamine secretion by AGCCs. Catecholamines 133-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 33143415-5 2020 We also solved the peptide:alpha-Cbtx cocrystal structure, revealing that the peptide, although of unique primary sequence, binds to alpha-Cbtx by mimicking structural features of the nAChR binding pocket. -cbtx 32-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 33184264-7 2020 In contrast, ACh-m/nAChR inhibitor or knockdown of VEGF-A/B by shRNA powerfully abrogated these effects mediated by VNS. Acetylcholine 13-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 32248535-8 2020 A comparison of PNU-120596 molecule docked to the models of transmembrane domains of the human alpha7 AChR and two subunits of L. stagnalis nAChR demonstrated some differences in contacts with the amino acid residues important for PNU-120596 action on the alpha7 nAChR. N-neopentyl-N-nitrosourea 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 32707263-5 2020 Nicotine acts directly at nicotinic acetylcholine receptors (nAChR) to have its pharmacological effect. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 32738311-1 2020 Nicotinic acetylcholine receptors (nAChR) are homo- or hetero-pentameric ligand-gated ion channels of the Cys-loop superfamily and play important roles in the nervous system and muscles. Cysteine 106-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 32738311-1 2020 Nicotinic acetylcholine receptors (nAChR) are homo- or hetero-pentameric ligand-gated ion channels of the Cys-loop superfamily and play important roles in the nervous system and muscles. Cysteine 106-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 32707263-5 2020 Nicotine acts directly at nicotinic acetylcholine receptors (nAChR) to have its pharmacological effect. Acetylcholine 36-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 32707263-7 2020 Research utilizing genetically engineered rodents and pharmacological manipulations suggest a role for nAChR in several ethanol behaviors. Ethanol 120-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 32707263-8 2020 The current manuscript collates this literature and discusses findings that implicate specific nAChR subunits in ethanol phenotypes. Ethanol 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 32649832-1 2020 Engineering the selectivity of alpha-conotoxins for nicotinic acetylcholine receptors (nAChRs) presents considerable complexity and challenges, as it involves the optimization of their binding affinities to multiple highly conserved nAChR subtypes. Acetylcholine 62-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 32957649-0 2020 Low-Dose Nicotine Activates EGFR Signaling via alpha5-nAChR and Promotes Lung Adenocarcinoma Progression. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 32957649-5 2020 Screening of nicotinic acetylcholine receptor subunits in lung cancer cell lines demonstrated a particularly high expression level of nicotinic acetylcholine receptor subunit alpha5 (alpha 5-nAChR) in LAC cell lines. Acetylcholine 144-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 32947868-2 2020 One group of proteins affected by 3FTX are nicotinic acetylcholine receptors (nAChR). 3ftx 34-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-76 32957649-7 2020 In LAC cell lines alpha 5-nAChR interacts with epidermal growth factor receptor (EGFR), positively regulates EGFR pathway, enhances the expression of epithelial-mesenchymal transition markers, and is essential for low-dose nicotine-induced EGFR phosphorylation. Nicotine 223-231 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 32957649-8 2020 Functionally, low-dose nicotine requires alpha 5-nAChR to enhance cell migration, invasion, and proliferation. Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 32957649-11 2020 Our data identified alpha 5-nAChR as an essential mediator for low-dose nicotine-dependent LAC progression possibly through signaling crosstalk with EGFR, supporting the involvement of environmental smoke in tumor progression in LAC patients. Nicotine 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 32947868-2 2020 One group of proteins affected by 3FTX are nicotinic acetylcholine receptors (nAChR). 3ftx 34-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 32947868-9 2020 Overall, the docking protocol predicted the qualitative and some specific aspects of 3FTX binding to nAChR with reasonable success and shed light on unknown aspects of 3FTX binding to different receptor subtypes. 3ftx 85-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 32590127-0 2020 Swertiamarin, a secoiridoid glycoside modulates nAChR and AChE activity. swertiamarin 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 32590127-0 2020 Swertiamarin, a secoiridoid glycoside modulates nAChR and AChE activity. Glycosides 28-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 32590127-3 2020 Using Caenorhabditis elegans as a model, SW was found to enhance neurotransmission by modulating AChE and nicotinic acetylcholine receptor (nAChR) activity; being orchestrated through up-regulation of unc-17 and unc-50. Acetylcholine 116-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 32923455-1 2020 Previous studies from this lab have determined that dedifferentiation of Muller glia occurs after eye drop application of an alpha7 nicotinic acetylcholine receptor (nAChR) agonist, PNU-282987, to the adult rodent eye. PNU-282987 182-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 32867140-3 2020 In the complementary beta4-subunit of the alpha3beta4 nAChR binding pocket, non-conserved AspB173 through a salt bridge was found to be the key determinant for the alpha3beta4 selectivity of the quinuclidine-triazole chemotype, explaining the 47-327-fold affinity of the (S)-enantiomers as compared to their (R)-enantiomer counterparts. aspb173 90-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 32867140-3 2020 In the complementary beta4-subunit of the alpha3beta4 nAChR binding pocket, non-conserved AspB173 through a salt bridge was found to be the key determinant for the alpha3beta4 selectivity of the quinuclidine-triazole chemotype, explaining the 47-327-fold affinity of the (S)-enantiomers as compared to their (R)-enantiomer counterparts. Quinuclidines 195-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 32867140-3 2020 In the complementary beta4-subunit of the alpha3beta4 nAChR binding pocket, non-conserved AspB173 through a salt bridge was found to be the key determinant for the alpha3beta4 selectivity of the quinuclidine-triazole chemotype, explaining the 47-327-fold affinity of the (S)-enantiomers as compared to their (R)-enantiomer counterparts. Triazoles 208-216 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 32806654-1 2020 alpha7 nicotinic acetylcholine receptors (nAChR) is an important nicotinic acetylcholine receptors subtype and closely associated with cognitive disorders, such as Alzheimer"s and schizophrenia disease. Acetylcholine 17-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 32806654-1 2020 alpha7 nicotinic acetylcholine receptors (nAChR) is an important nicotinic acetylcholine receptors subtype and closely associated with cognitive disorders, such as Alzheimer"s and schizophrenia disease. Acetylcholine 75-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 32806654-2 2020 The mutant ArIB (V11L, V16A) of alpha-conotoxin ArIB with 17-amino acid residues specifically targets alpha7 nAChR with no obvious effect on other nAChR subtypes. 17-amino acid 58-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 32659920-4 2020 Interestingly, there is evidence that nicotinic acetylcholine receptors (nAChR) located on DA neurons also provide neurotrophic support to DA neurons, an effect requiring functional D3R and suggesting the existence of a positive cross-talk between these receptor systems. Dopamine 91-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-71 32577853-2 2020 Following existing support for a role of the alpha7 and beta2 nicotinic acetylcholine receptor (nAChR) subunits in apoptotic regulation, we aimed to determine whether these subunits are altered in the SIDS hippocampus and if they are correlated with cell death markers of active caspase-3 (Casp-3) and TUNEL. Acetylcholine 72-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 30999028-0 2020 Calcium influx through muscle nAChR-channels: One route, multiple roles. Calcium 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 32659920-4 2020 Interestingly, there is evidence that nicotinic acetylcholine receptors (nAChR) located on DA neurons also provide neurotrophic support to DA neurons, an effect requiring functional D3R and suggesting the existence of a positive cross-talk between these receptor systems. Dopamine 91-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 32659920-4 2020 Interestingly, there is evidence that nicotinic acetylcholine receptors (nAChR) located on DA neurons also provide neurotrophic support to DA neurons, an effect requiring functional D3R and suggesting the existence of a positive cross-talk between these receptor systems. Dopamine 139-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-71 32659920-4 2020 Interestingly, there is evidence that nicotinic acetylcholine receptors (nAChR) located on DA neurons also provide neurotrophic support to DA neurons, an effect requiring functional D3R and suggesting the existence of a positive cross-talk between these receptor systems. Dopamine 139-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 32659920-6 2020 Among them, we recently identified a receptor heteromer containing the nAChR and the D3R as the molecular effector of nicotine-mediated neurotrophic effects. Nicotine 118-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 32659920-8 2020 In particular, the molecular and functional features of the D3R-nAChR heteromer will be especially discussed since it may represent a possible key etiologic effector for DA-related pathologies, such as Parkinson"s disease (PD), and a target for drug design. Dopamine 170-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 32894468-6 2020 Coincubation of U251 MG cells with rSLURP-1 and the nAChR inhibitor mecamylamine attenuates the antiproliferative activity of rSLURP-1, indicating nAChR as a molecular target for the rSLURP-1 action in gliomas. Mecamylamine 68-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 32894468-6 2020 Coincubation of U251 MG cells with rSLURP-1 and the nAChR inhibitor mecamylamine attenuates the antiproliferative activity of rSLURP-1, indicating nAChR as a molecular target for the rSLURP-1 action in gliomas. Mecamylamine 68-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 31925927-9 2020 The effects of nicotine on attenuating TXNIP and preserving Insulin 1 expression levels were attenuated by pharmacological and genetical inhibition of alpha7 nAChR. Nicotine 15-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 32342646-6 2020 Carbamazepine, which should be carefully used in BECTS, was observed to be effective in the treatment of our atypical BECTS proband based on the molecular diagnosis of CHRNA4. Carbamazepine 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-174 32169758-2 2020 The activation of alpha4beta2-nAChR in the RTN increased GABA release in MoTN resulting in reduced glutamatergic transmission in thalamic hyperdirect pathway of wild-type. gamma-Aminobutyric Acid 57-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 32349117-3 2020 This study aimed to investigate how administering multiple doses of tropisetron, a partial agonist of nAChR, for 1 day would affect cognitive deficits and P50 inhibition deficits in SCZ patients. Tropisetron 68-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 102-107 32349117-10 2020 One day of treatment with tropisetron improved both cognitive and P50 inhibition deficits, suggesting that longer term treatment with alpha7 nAChR agonists for these deficits in SCZ may be promising. Tropisetron 26-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 33184579-10 2020 Stimulation of nAChR with nicotine did not ameliorate TNF-alpha induced permeability nor alter 70 kDa dextran transport. Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 32493979-5 2020 Polyamines are classically studied as regulators of ion channel gating that engage the nAChR channel pore. Polyamines 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 32493979-6 2020 In contrast, we find polyamine effects on assembly involve the nAChR cytosolic loop. Polyamines 21-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 32493979-8 2020 Our pharmacological and transgenic animal studies find that reducing polyamines enhances cortical neuron nAChR expression and augments nicotine-mediated neuroprotection. Polyamines 69-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 32493979-9 2020 Taken together, we describe a most unexpected role for polyamines in regulating ion channel assembly, which provides a new avenue for nAChR neuropharmacology. Polyamines 55-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 32169758-3 2020 Contrary to wild-type, activation of S286L-mutant alpha4beta2-nAChR (loss-of-function) in the RTN relatively enhanced glutamatergic transmission in thalamic hyperdirect pathway of S286L-TG via impaired GABAergic inhibition in intra-thalamic (RTN-MoTN) pathway. Thioguanine 186-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 32017982-3 2020 MB266 acted as an antagonist at acetylcholine receptors, displaying 18-fold selectivity for mAChR versus nAChR (compared to the 15,200-fold selectivity observed for QNB). Acetylcholine 32-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 31614011-3 2020 AIM: To determine tissue levels of Acetylcholine (ACh) and its muscarinic and nicotinic receptors (mAChR and nAChR), in psoriasis vulgaris lesions in comparison to normal control skin. Acetylcholine 35-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 32448416-6 2020 Our finding that an HAE fraction consisting almost entirely of harmonine had a strong inhibitory effect points to this alkaloid as a key component of nAChR inhibitory actions. harmonine 63-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 31096265-2 2020 Varenicline, an alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to increase smoking quit rates compared with nicotine-based products. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 32463026-3 2020 Prior studies have demonstrated that the destructive neurological effects of rabies virus (RABV) infections are mediated by CNS transport of the virus tightly bound to the nicotinic acetylcholine receptor (nAChR). Acetylcholine 182-195 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 31294817-9 2020 Candidates supported by both FTND and TTFC (CHRNA4, THSD7B, RBFOX1, and ZNF804A) were associated with addiction to alcohol, cocaine, and heroin, and were associated with autism and schizophrenia. Alcohols 115-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-50 31294817-9 2020 Candidates supported by both FTND and TTFC (CHRNA4, THSD7B, RBFOX1, and ZNF804A) were associated with addiction to alcohol, cocaine, and heroin, and were associated with autism and schizophrenia. Cocaine 124-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-50 32208709-2 2020 Glycosylphosphatidylinositol (GPI)-linked lynx1 is an allosteric modulator of nAChR function, including shifts in agonist sensitivity, reduced desensitization, and slower recovery from desensitization. Glycosylphosphatidylinositols 0-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 32208709-2 2020 Glycosylphosphatidylinositol (GPI)-linked lynx1 is an allosteric modulator of nAChR function, including shifts in agonist sensitivity, reduced desensitization, and slower recovery from desensitization. Glycosylphosphatidylinositols 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 32234761-3 2020 We observed that Czon1107 strongly inhibits the human alpha3beta4 (IC50 15.7 +- 3.0 mum) and alpha7 (IC50 77.1 +- 0.05 mum) nicotinic acetylcholine receptor (nAChR) subtypes, but the activity of Cca1669 remains to be identified. czon1107 17-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-156 32234761-3 2020 We observed that Czon1107 strongly inhibits the human alpha3beta4 (IC50 15.7 +- 3.0 mum) and alpha7 (IC50 77.1 +- 0.05 mum) nicotinic acetylcholine receptor (nAChR) subtypes, but the activity of Cca1669 remains to be identified. czon1107 17-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 32234761-8 2020 The cis conformation at the Cys6-Pro7 peptide bond was essential for alpha3beta4 nAChR subtype allosteric selectivity. Peptides 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 32272701-1 2020 The alpha9-containing nicotinic acetylcholine receptor (nAChR) is increasingly emerging as a new tumor target owing to its high expression specificity in breast cancer. Acetylcholine 32-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 32113032-2 2020 This receptor plays a critical role in nicotine addiction, with potential smoking cessation therapeutics producing modulation of alpha4beta2 nAChR. Nicotine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 32272701-12 2020 This demonstrates that GeXIVA induced a downregulation of alpha9-nAChR expression, and the growth of MDA-MB-157 alpha9-nAChR KO cell line was inhibited as well, due to alpha9-nAChR deletion. gexiva 23-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 32272701-12 2020 This demonstrates that GeXIVA induced a downregulation of alpha9-nAChR expression, and the growth of MDA-MB-157 alpha9-nAChR KO cell line was inhibited as well, due to alpha9-nAChR deletion. gexiva 23-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 32272701-12 2020 This demonstrates that GeXIVA induced a downregulation of alpha9-nAChR expression, and the growth of MDA-MB-157 alpha9-nAChR KO cell line was inhibited as well, due to alpha9-nAChR deletion. gexiva 23-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 32272701-13 2020 GeXIVA inhibits the growth of breast cancer cell MDA-MB-157 cells in vitro and may occur in a mechanism abolishing alpha9-nAChR. gexiva 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 32007796-9 2020 Endogenous ACh is synthesized in the intestinal epithelium and drives organoid growth and differentiation through activation of nAChR signaling. Acetylcholine 11-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 32044666-2 2020 We have shown that GTS-21, a selective alpha7 nAChR agonist, downregulates APC-dependent CD4+ T cell differentiation into regulatory T cells (Tregs) and effector Th1, Th2 and Th17 cells by inhibiting antigen processing, thereby interfering with antigen presentation. 3-(2,4-dimethoxybenzylidene)anabaseine 19-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 31887290-4 2020 Here, we report the discovery and characterization of AN6001, a novel selective alpha6beta2* nAChR PAM. an6001 54-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 31887290-5 2020 AN6001 mediated increases in both nicotine potency and efficacy at the human alpha6/alpha3beta2beta3V9"S nAChR in HEK293 cells, and it positively modulated ACh-evoked currents through both alpha6/alpha3beta2beta3V9"S and a concatenated beta3-alpha6-beta2-alpha6-beta2 receptor in Xenopus oocytes, displaying EC50 values of 0.58 microM and 0.40 microM, respectively. Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 31686175-3 2020 OBJECTIVE: The aim was to test whether galantamine, a PAM at several nAChR subtypes, can potentiate the cognitive-enhancing effects of nicotine. Galantamine 39-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 32059521-7 2020 In the A549 lung cancer cells, where alpha7 nAChR activation stimulates proliferation, Ol-CHOL, Ln-CHOL, and AA-CHOL dose-dependently decreased cell viability by up to 45%. N(1)-cholesterylcarbamoyl-N(8)-(4-nitrobenzo-2-oxa-1,3-diazole)-3,6-dioxaoctyl-1,8-diamine 109-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 32031532-0 2020 Two mutations in the nicotinic acetylcholine receptor subunit A4 (CHRNA4) in a family with autosomal dominant sleep-related hypermotor epilepsy. Acetylcholine 31-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-72 30378732-10 2020 Overall, these findings suggest that alpha3beta4* and alpha6beta4* nAChR subtypes represent viable targets for the development of medications to counteract THC dependence. Dronabinol 156-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 31956359-4 2020 Activation of nicotine/nAChR signaling is associated with lung cancer risk and drug resistance. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 31956359-5 2020 We focused on nAChR pathways activated by nicotine and its downstream signaling involved in regulating apoptotic factors of mitochondria and drug resistance in lung cancer. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-19 33022581-1 2020 The thalamus, with the highest density of nicotinic acetylcholine receptor (nAChR) in the brain, plays a central role in thalamo-cortical circuits that are implicated in nicotine addiction. Nicotine 170-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-74 33022581-1 2020 The thalamus, with the highest density of nicotinic acetylcholine receptor (nAChR) in the brain, plays a central role in thalamo-cortical circuits that are implicated in nicotine addiction. Nicotine 170-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 32044666-2 2020 We have shown that GTS-21, a selective alpha7 nAChR agonist, downregulates APC-dependent CD4+ T cell differentiation into regulatory T cells (Tregs) and effector Th1, Th2 and Th17 cells by inhibiting antigen processing, thereby interfering with antigen presentation. 3,4-APC 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Tyrosine 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Nicotine 144-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Calcium 161-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Calcium 180-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Bungarotoxins 286-304 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). Bungarotoxins 306-315 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). methyllycaconitine 321-339 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32044666-3 2020 alpha7 nAChRs on Jurkat human leukemic T cells require functional T cell receptors (TCRs)/CD3 and leukocyte-specific tyrosine kinase to mediate nicotine-induced Ca2+-signaling via Ca2+ release from intracellular stores, and are insensitive to two conventional alpha7 nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and methyllycaconitine (MLA). methyllycaconitine 341-344 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 32048843-1 2020 We utilize various computational methodologies to study menthol"s interaction with multiple organic phases, a lipid bilayer, and the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) --- the most abundant nAChR in the brain. Menthol 56-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 32048843-1 2020 We utilize various computational methodologies to study menthol"s interaction with multiple organic phases, a lipid bilayer, and the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) --- the most abundant nAChR in the brain. Menthol 56-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 32048843-1 2020 We utilize various computational methodologies to study menthol"s interaction with multiple organic phases, a lipid bilayer, and the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) --- the most abundant nAChR in the brain. Acetylcholine 161-174 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 32048843-6 2020 The most likely binding mode of menthol to a desensitized membrane-embedded alpha4beta2 nAChR is identified to be via a membrane-mediated pathway in which menthol binds to the sites at the lipid-protein interface after partitioning in the membrane. Menthol 32-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 32048843-6 2020 The most likely binding mode of menthol to a desensitized membrane-embedded alpha4beta2 nAChR is identified to be via a membrane-mediated pathway in which menthol binds to the sites at the lipid-protein interface after partitioning in the membrane. Menthol 155-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 31399700-3 2020 In this study, we investigated the effects of cocaine on a special subtype of neuronal nAChR, alpha3beta4-nAChR expressed in native SH-SY5Y cells. Cocaine 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 31399700-8 2020 Kinetic analysis showed that cocaine accelerated alpha3beta4-nAChR desensitization, which caused a reduction of the amplitude of nicotine-induced currents. Cocaine 29-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 31399700-8 2020 Kinetic analysis showed that cocaine accelerated alpha3beta4-nAChR desensitization, which caused a reduction of the amplitude of nicotine-induced currents. Nicotine 129-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 32451953-5 2020 In this paper, we review the structure and diversity of nAChR subunits and our understanding for how different nAChR subtypes play specific roles in the phenomenon of nicotine addiction. Nicotine 167-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 32451953-5 2020 In this paper, we review the structure and diversity of nAChR subunits and our understanding for how different nAChR subtypes play specific roles in the phenomenon of nicotine addiction. Nicotine 167-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 31789411-1 2020 Nicotinic acetylcholine receptor (nAChR) subunit alpha5 (alpha5-nAChR) is involved in tumor cell proliferation, inhibition of apoptosis, progression of metastasis, and induction of angiogenesis in certain solid tumors. Acetylcholine 10-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 31789411-1 2020 Nicotinic acetylcholine receptor (nAChR) subunit alpha5 (alpha5-nAChR) is involved in tumor cell proliferation, inhibition of apoptosis, progression of metastasis, and induction of angiogenesis in certain solid tumors. Acetylcholine 10-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 31813155-1 2019 OBJECTIVE: To assess the association of single nucleotide polymorphisms (SNPs) CHRNA4 gene with response to selective serotonin re-uptake inhibitors (SSRIs) for the treatment of major depressive disorder (MDD). Serotonin 118-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-85 30526213-2 2019 Cytisine, a partial agonist for the alpha4beta2-nAChR, is used as a smoking cessation medication. cytisine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 30552041-1 2019 The nicotinic acetylcholine receptor (nAChR) agonist nicotine and the noradrenaline transporter inhibitor atomoxetine are widely studied substances due to their propensity to alleviate cognitive deficits in psychiatric and neurological patients and their beneficial effects on some aspects of cognitive functions in healthy individuals. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 30552041-1 2019 The nicotinic acetylcholine receptor (nAChR) agonist nicotine and the noradrenaline transporter inhibitor atomoxetine are widely studied substances due to their propensity to alleviate cognitive deficits in psychiatric and neurological patients and their beneficial effects on some aspects of cognitive functions in healthy individuals. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 30552041-11 2019 This finding is compatible with previous evidence of nicotine effects on stop-signal task performance in highly impulsive individuals and implicates the nAChR in the neural basis of impulsivity. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 30623678-2 2019 Herein, we report the molecular modelling and design of an optimised peptide sequence based on interactions of RDP with the alpha7 subunit of the nicotinic acetylcholine receptor (nAChR). Acetylcholine 156-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 31492697-2 2019 To check wheth er peptides built exclusively from arginine residues will interact with different nAChR subtypes or with such their structural homologues as the acetylcholine binding protein and ligand binding domain of nAChR alpha9 subunit, we synthesized a series of R3, R6, R8 and R16 oligoarginines and investigate their activity by competition with radioiodinated alpha- bungarotoxin, by two electrode voltage clamp electrophysiology and calcium imaging. Arginine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 31492697-7 2019 Since modified oligoarginines and other cationic molecules are widely used as cell penetrating peptides, we studied several cationic polymers and demonstrated their nAChR inhibitory activity. oligoarginines 15-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 31492697-7 2019 Since modified oligoarginines and other cationic molecules are widely used as cell penetrating peptides, we studied several cationic polymers and demonstrated their nAChR inhibitory activity. Polymers 133-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 31421156-1 2019 At vertebrate motor endplates, the conversion of nerve impulses into muscle contraction is initiated by binding of acetylcholine to its nicotinic receptor (nAChR) at the postsynapse. Acetylcholine 115-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 31671780-6 2019 Only 2-(3-pyridyl)-1,4,5,6-tetrahydropyrimidine monohydrogen chloride (PTHP), the cyclic iminium analog, displayed nAChR potencies and binding affinities similar to anabaseine. 2-(3-pyridyl)-1,4,5,6-tetrahydropyrimidine monohydrogen chloride 5-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 31671780-6 2019 Only 2-(3-pyridyl)-1,4,5,6-tetrahydropyrimidine monohydrogen chloride (PTHP), the cyclic iminium analog, displayed nAChR potencies and binding affinities similar to anabaseine. pthp 71-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 31411453-7 2019 Second-generation mutants of Vc1.1 [S4 Dab, N9A] and [S4 Dab, N9W] increased potency at the alpha9alpha10 nAChR by 20-fold compared with that of Vc1.1. diazobenzenesulfonic acid 39-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 31411453-7 2019 Second-generation mutants of Vc1.1 [S4 Dab, N9A] and [S4 Dab, N9W] increased potency at the alpha9alpha10 nAChR by 20-fold compared with that of Vc1.1. diazobenzenesulfonic acid 57-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 31221718-0 2019 Discovery of an intrasubunit nicotinic acetylcholine receptor-binding site for the positive allosteric modulator Br-PBTC. Br-PBTC 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-61 31401009-4 2019 Because A85380 is known as a potent alpha4beta2-nAChR agonist, we prepared A85380 derivatives labeled with 99mTc using a bifunctional chelate system. A 85380 8-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 31401009-6 2019 We used non-radioactive rhenium (Re) for a 99mTc analog and found that one of the derivatives, Re-A-YN-IDA-C4, exhibited high binding affinity at alpha4beta2-nAChR in both the docking simulation (-19.3 kcal/mol) and binding assay (Ki = 0.4 +- 0.04 nM). re-a-yn-ida-c4 95-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 31401009-8 2019 Consequently, we found that 99mTc-A-YN-IDA-C4, with a structure optimized by using computational chemistry techniques, maintained affinity and selectivity for nAChR in vitro and possessed efficient characteristics as a nuclear medicine molecular imaging probe, demonstrated usefulness of computational scientific approach for molecular improvement strategy. 99mtc-a-yn-ida-c4 28-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 31278882-1 2019 alpha-Conotoxin (CTx) TxID is a potent alpha3beta4 nicotinic acetylcholine receptor (nAChR) antagonist that has been suggested as a potential drug candidate to treat addiction and small cell lung cancer. txid 22-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 31518499-5 2019 Here, we evaluate the extent to which this model applies to cytisine at the alpha4beta2 nAChR, which is a subtype that is known to play a prominent role in nicotine addiction. cytisine 60-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 31518499-5 2019 Here, we evaluate the extent to which this model applies to cytisine at the alpha4beta2 nAChR, which is a subtype that is known to play a prominent role in nicotine addiction. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 31581202-3 2019 The alpha7 nicotinic acetylcholine receptor (nAChR) is highly expressed in the hippocampus and reduced expression and function of this receptor are linked with cognitive impairments in Alzheimer"s disease and schizophrenia. Acetylcholine 21-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 31221718-2 2019 nAChR PAMs have therapeutic potential for the treatment of nicotine addiction and several neuropsychiatric disorders. Nicotine 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 31221718-17 2019 Br-PBTC and its derivatives should prove useful as alpha subunit-selective nAChR PAMs. Br-PBTC 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 31175218-1 2019 Homomeric alpha7 nicotinic acetylcholine receptors (nAChR) have an intrinsically low probability of opening that can be overcome by alpha7-selective positive allosteric modulators (PAMs), which bind at a site involving the second transmembrane domain (TM2). Acetylcholine 27-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 31062355-4 2019 EXPERIMENTAL APPROACH: The competitive antagonist dihydro-beta-erythroidine (DHbetaE) was modelled by replacement of the agonist nicotine in the alpha4beta2 nAChR experimental structure. Dihydro-beta-Erythroidine 50-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 31062355-4 2019 EXPERIMENTAL APPROACH: The competitive antagonist dihydro-beta-erythroidine (DHbetaE) was modelled by replacement of the agonist nicotine in the alpha4beta2 nAChR experimental structure. Dihydro-beta-Erythroidine 77-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 31062355-4 2019 EXPERIMENTAL APPROACH: The competitive antagonist dihydro-beta-erythroidine (DHbetaE) was modelled by replacement of the agonist nicotine in the alpha4beta2 nAChR experimental structure. Nicotine 129-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 31175218-2 2019 Mutation of a methionine that is unique to alpha7 at the 15" position of TM2 to leucine, the residue in most other nAChR subunits, largely eliminates the activity of such PAMs. Methionine 14-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 31175218-2 2019 Mutation of a methionine that is unique to alpha7 at the 15" position of TM2 to leucine, the residue in most other nAChR subunits, largely eliminates the activity of such PAMs. Leucine 80-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 31330850-9 2019 Human intoxication by ingestion of PnTXs could result in various symptoms observed in episodes of poisoning with natural nAChR antagonists. pntxs 35-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 31242717-8 2019 We observed that ACh bound to nAChR on activated immune cells and led to the inhibition of lymphocyte proliferation and of proinflammatory-cytokine production. Acetylcholine 17-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 30659887-7 2019 Currents were blocked by the nAChR antagonists mecamylamine (30 micromol/L), but not by the TRPA1 selective antagonist HC-030031 (10 micromol/L). Mecamylamine 47-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 31333465-4 2019 The IC50 values measured in competition with radioiodinated alpha-bungarotoxin for binding to the membrane-bound Torpedo californica nAChR were 4.9 and 7.4 microM for Lynx1 and SSS fragments, but over 300 microM for SLURP1 or SLURP2 fragments. sss 177-180 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 31333465-5 2019 The affinity of these compounds for the alpha7 nAChR in the rat pituitary tumor-derived cell line GH4C1 was different: 13.1 and 147 microM for SSS and Lynx1 fragments, respectively. sss 143-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 31333465-6 2019 In competition for the ligand-binding domain of the alpha9 nAChR subunit, SSS and Lynx1 fragments had IC50 values of about 40 microM, which correlates with the value found for the latter with the rat alpha9alpha10 nAChR expressed in the Xenopus oocytes. sss 74-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 31333465-6 2019 In competition for the ligand-binding domain of the alpha9 nAChR subunit, SSS and Lynx1 fragments had IC50 values of about 40 microM, which correlates with the value found for the latter with the rat alpha9alpha10 nAChR expressed in the Xenopus oocytes. sss 74-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 31130483-3 2019 In this in silico study, we use a combination of equilibrium and nonequilibrium molecular dynamics simulations to map dynamic and structural changes induced by nicotine in the human alpha4beta2 nAChR. Nicotine 160-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. dihydro 4-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-99 30874860-1 2019 RATIONALE: The non-selective nicotinic acetylcholine receptor (nAChR) agonist nicotine has been argued to improve attention via enhanced filtering of irrelevant stimuli. Nicotine 78-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-61 30874860-1 2019 RATIONALE: The non-selective nicotinic acetylcholine receptor (nAChR) agonist nicotine has been argued to improve attention via enhanced filtering of irrelevant stimuli. Nicotine 78-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 31078264-7 2019 Considering that D3R plays important roles in mediating reward-related physiological actions of alpha4beta2 nAChR, this study could provide a new insight into the regulatory mechanism involved in nicotine addiction. Nicotine 196-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. dihydro 4-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. -erythroidine 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-99 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. -erythroidine 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. Dihydro-beta-Erythroidine 31-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-99 31122014-3 2019 (+)-Dihydro-beta-erythroidine (DHbetaE), the most potent nicotine acetylcholine receptor antagonist (nAChR) of the Erythrina family, is synthesized for the first time in 13 steps from commercially available material. Dihydro-beta-Erythroidine 31-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 30718376-10 2019 In the ER, the inside-out pathway begins when nicotine becomes a stabilizing pharmacological chaperone for some nAChR subtypes, even at concentrations as low as ~10 nM. Nicotine 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 30664881-1 2019 Reconstituted nicotinic acetylcholine receptors (nAChRs) exhibit significant gain-of-function upon addition of cholesterol to reconstitution mixtures, and cholesterol affects the organization of nAChRs within domain-forming membranes, but whether nAChR partitions to cholesterol-rich liquid-ordered ("raft" or lo) domains or cholesterol-poor liquid-disordered (ldo) domains is unknown. Cholesterol 111-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 31137661-10 2019 These results indicate the importance of the cyclic imine for interacting with the adult mammalian muscle-type nAChR. cyclic imine 45-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 30923128-2 2019 Allopregnanolone and its synthetic analog alphaxalone are GABAAR-positive allosteric modulators (PAMs), whereas alphaxalone and most neuroactive steroids are nAChR inhibitors. alphaxalone 112-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 30923128-2 2019 Allopregnanolone and its synthetic analog alphaxalone are GABAAR-positive allosteric modulators (PAMs), whereas alphaxalone and most neuroactive steroids are nAChR inhibitors. Steroids 145-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 30923128-3 2019 In this report, we used 11beta-(p-azidotetrafluorobenzoyloxy)allopregnanolone (F4N3Bzoxy-AP), a general anesthetic and photoreactive allopregnanolone analog that is a potent GABAAR PAM, to characterize steroid-binding sites in the Torpedo alpha2betagammadelta nAChR in its native membrane environment. 11beta-(p-azidotetrafluorobenzoyloxy)allopregnanolone 24-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 260-265 30923128-3 2019 In this report, we used 11beta-(p-azidotetrafluorobenzoyloxy)allopregnanolone (F4N3Bzoxy-AP), a general anesthetic and photoreactive allopregnanolone analog that is a potent GABAAR PAM, to characterize steroid-binding sites in the Torpedo alpha2betagammadelta nAChR in its native membrane environment. f4n3bzoxy-ap 79-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 260-265 30923128-3 2019 In this report, we used 11beta-(p-azidotetrafluorobenzoyloxy)allopregnanolone (F4N3Bzoxy-AP), a general anesthetic and photoreactive allopregnanolone analog that is a potent GABAAR PAM, to characterize steroid-binding sites in the Torpedo alpha2betagammadelta nAChR in its native membrane environment. Pregnanolone 61-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 260-265 30923128-6 2019 Photolabeling identified three distinct [3H]F4N3Bzoxy-AP-binding sites in the nAChR transmembrane domain: 1) in the ion channel, identified by photolabeling in the M2 helices of betaVal-261 and deltaVal-269 (position M2-13"); 2) at the interface between the alphaM1 and alphaM4 helices, identified by photolabeling in alphaM1 (alphaCys-222/alphaLeu-223); and 3) at the lipid-protein interface involving gammaTrp-453 (M4), a residue photolabeled by small lipophilic probes and promegestone, a steroid nAChR antagonist. Steroids 492-499 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 30923128-7 2019 Photolabeling in the ion channel and alphaM1 was higher in the nAChR-desensitized state than in the resting state and inhibitable by promegestone. Promegestone 133-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 30923128-8 2019 These results directly indicate a steroid-binding site in the nAChR ion channel and identify additional steroid-binding sites also occupied by other lipophilic nAChR antagonists. Steroids 34-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 30923128-8 2019 These results directly indicate a steroid-binding site in the nAChR ion channel and identify additional steroid-binding sites also occupied by other lipophilic nAChR antagonists. Steroids 34-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 30923128-8 2019 These results directly indicate a steroid-binding site in the nAChR ion channel and identify additional steroid-binding sites also occupied by other lipophilic nAChR antagonists. Steroids 104-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 30923128-8 2019 These results directly indicate a steroid-binding site in the nAChR ion channel and identify additional steroid-binding sites also occupied by other lipophilic nAChR antagonists. Steroids 104-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 30665006-0 2019 The alpha3 and alpha4 nicotinic acetylcholine receptor (nAChR) subunits in the brainstem medulla of sudden infant death syndrome (SIDS). Acetylcholine 32-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. 1,2-Dipalmitoylphosphatidylcholine 10-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. Cholesterol 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. Cholesterol 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 326-331 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. 1,2-Dipalmitoylphosphatidylcholine 54-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. 1,2-Dipalmitoylphosphatidylcholine 54-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 326-331 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. 1,2-Dipalmitoylphosphatidylcholine 89-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 30664881-3 2019 In binary Dipalmitoylphosphatidylcholine:Cholesterol (DPPC:CHOL) mixtures, both CHOL and DPPC acyl chains were observed spontaneously entering deep "non-annular" cavities in the nAChR TMD, particularly at the subunit interface and the beta subunit center, facilitated by the low amino acid density in the cryo-EM structure of nAChR in a native membrane. 1,2-Dipalmitoylphosphatidylcholine 89-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 326-331 30664881-6 2019 nAChR partitioned to any cholesterol-poor ldo domain that was present, regardless of whether the ldo or lo domain lipids had PC or PE headgroups. Cholesterol 25-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Acetylcholine 10-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Norepinephrine 132-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Norepinephrine 132-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Dopamine 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Dopamine 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Serotonin 158-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Serotonin 158-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Glutamic Acid 172-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 30914244-1 2019 Nicotinic acetylcholine receptors (nAChR) are ion channels which regulate a numerous of neurotransmitters, including acetylcholine, norepinephrine, dopamine, serotonin and glutamate. Glutamic Acid 172-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 30772268-1 2019 In this paper, we designed, synthesized and tested a small set of three new derivatives potentially targeting the D3R-nAChR heteromer, a receptor complex recently identified and characterized as the molecular entity that, in dopaminergic neurons, mediates the neurotrophic effects of nicotine. Nicotine 284-292 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 30550855-0 2019 TRPC channels mediated calcium entry is required for proliferation of human airway smooth muscle cells induced by nicotine-nAChR. Calcium 23-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 30550855-8 2019 Nicotine promoted HASMC proliferation, which was accompanied by elevated alpha5-nAchR and TRPC3 expressions, basal [Ca2+]cyt, store-operated calcium entry (SOCE) and the rate of Mn2+ quenching in HASMCs. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 30137518-1 2019 Interest in nicotinic acetylcholine receptor (nAChR) ligands as potential therapeutic agents for cognitive disorders began more than 30 years ago when it was first demonstrated that the tobacco alkaloid nicotine could improve cognitive function in nicotine-deprived smokers as well as nonsmokers. Nicotine 203-211 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 30550855-8 2019 Nicotine promoted HASMC proliferation, which was accompanied by elevated alpha5-nAchR and TRPC3 expressions, basal [Ca2+]cyt, store-operated calcium entry (SOCE) and the rate of Mn2+ quenching in HASMCs. hasmc 18-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 30550855-9 2019 Further investigation indicated that nicotine-induced Ca2+ response and TRPC3 up-regulation was reversibly blocked by small interfering RNA (siRNA) suppression of alpha5-nAChR. Nicotine 37-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 30550855-11 2019 In conclusion, nicotine-induced HASMC proliferation was mediated by TRPC3-dependent calcium entry via alpha5-nAchR, which provided a potential target for treatment of COPD. Nicotine 15-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 30550855-11 2019 In conclusion, nicotine-induced HASMC proliferation was mediated by TRPC3-dependent calcium entry via alpha5-nAchR, which provided a potential target for treatment of COPD. hasmc 32-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 30137518-1 2019 Interest in nicotinic acetylcholine receptor (nAChR) ligands as potential therapeutic agents for cognitive disorders began more than 30 years ago when it was first demonstrated that the tobacco alkaloid nicotine could improve cognitive function in nicotine-deprived smokers as well as nonsmokers. Nicotine 248-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 29637850-0 2019 NAChR alpha4beta2 subtype and their relation with nicotine addiction, cognition, depression and hyperactivity disorder. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 30837868-2 2019 Here, we report a novel effect that cocaine directly inhibits alpha6N/alpha3Cbeta2beta3-nAChR (alpha6*-nAChRs) function. Cocaine 36-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 30837868-8 2019 Furthermore, analysis of whole-cell current kinetics demonstrated that cocaine slows nAChR channel activation but accelerates whole-cell current decay time. Cocaine 71-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 30837868-10 2019 Additionally, in Xenopus oocytes, cocaine inhibits both alpha6N/alpha3Cbeta2beta3-nAChRs and alpha6M211L/alpha3ICbeta2beta3-nCAhRs similarly, suggesting that cocaine may not act on the alpha3 transmembrane domain of chimeric alpha6N/alpha3Cbeta2beta3-nAChR. Cocaine 34-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 30837868-11 2019 In mechanically isolated VTA DA neurons, cocaine abolishes alpha6*-nAChR-mediated enhancement of spontaneous inhibitory postsynaptic currents (sIPSCs). Cocaine 41-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 29881944-7 2019 Initially, we performed a computational prediction of the molecular interactions between the nicotine analogs with the alpha7 nicotinic acetylcholine receptor (nAChR). Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 30687021-8 2018 By including models of nAChR-mediated currents in the VTA DA-GABA circuit, we showed that nicotine should reduce the acetylcholine action on the VTA GABA neurons by receptor desensitization and potentially boost DA responses to reward-related signals in a non-trivial manner. gamma-Aminobutyric Acid 61-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30687021-8 2018 By including models of nAChR-mediated currents in the VTA DA-GABA circuit, we showed that nicotine should reduce the acetylcholine action on the VTA GABA neurons by receptor desensitization and potentially boost DA responses to reward-related signals in a non-trivial manner. Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30687021-8 2018 By including models of nAChR-mediated currents in the VTA DA-GABA circuit, we showed that nicotine should reduce the acetylcholine action on the VTA GABA neurons by receptor desensitization and potentially boost DA responses to reward-related signals in a non-trivial manner. Acetylcholine 117-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30687084-3 2018 These disulfide-rich peptides provide a large number of evolutionarily refined templates that can be used to develop conopeptides that are highly selective for the various nAChR subtypes. Disulfides 6-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 30809122-10 2019 The mutation reduced the maximal currents by approximately 80% in response to saturating concentrations of nicotine in homo- and heterozygous form, in both the alpha2beta4 and alpha2beta2 nAChR subtypes. Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 30541909-8 2019 DA release evoked by single electrical pulses in the presence of the nAChR antagonist dihydro-beta-erythroidine was reduced by GABA or agonists of GABAA or GABAB receptors, with effects prevented by selective GABA receptor antagonists. Dopamine 0-2 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 30541909-8 2019 DA release evoked by single electrical pulses in the presence of the nAChR antagonist dihydro-beta-erythroidine was reduced by GABA or agonists of GABAA or GABAB receptors, with effects prevented by selective GABA receptor antagonists. Dihydro-beta-Erythroidine 86-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 30541909-8 2019 DA release evoked by single electrical pulses in the presence of the nAChR antagonist dihydro-beta-erythroidine was reduced by GABA or agonists of GABAA or GABAB receptors, with effects prevented by selective GABA receptor antagonists. gamma-Aminobutyric Acid 127-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 29637850-2 2019 This work aims review the structure and functioning of the alpha4beta2 nAChR emphasizing its role in the treatment of associated diseases like nicotine addiction and underlying pathologies such as cognition, depression and attention-deficit hyperactivity disorder. Nicotine 143-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 30403486-0 2018 Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an alpha7-nAChR, alpha9-nAChR Antagonist and of a Pro-Oxidant Mitocan. onium-alkyloxy-stilbene 50-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 31731917-11 2019 AZD1446 (alpha4beta2 nAChR agonist) improves the Groton Maze task due to high nAChR in dPCC/RSC engaged in spatial orientation. 3-(5-chloro-2-furoyl)-3,7-diazabicyclo(3.3.0)octane 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 31731917-11 2019 AZD1446 (alpha4beta2 nAChR agonist) improves the Groton Maze task due to high nAChR in dPCC/RSC engaged in spatial orientation. 3-(5-chloro-2-furoyl)-3,7-diazabicyclo(3.3.0)octane 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 30362667-0 2018 Synthesis of a Series of Non-Symmetric Bispyridinium and Related Compounds and Their Affinity Characterization at the Nicotinic Acetylcholine Receptor. bispyridinium 39-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-150 30362667-2 2018 In case the reactivation is insufficient, acetylcholine concentrations that rise to pathophysiological levels force the nicotinic acetylcholine receptor (nAChR) into a desensitized state and hence a functionally inactive state. Acetylcholine 42-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-152 30362667-2 2018 In case the reactivation is insufficient, acetylcholine concentrations that rise to pathophysiological levels force the nicotinic acetylcholine receptor (nAChR) into a desensitized state and hence a functionally inactive state. Acetylcholine 42-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 30362667-4 2018 Previous electrophysiological studies identified the symmetric bispyridinium compound 1,1"-(propane-1,3-diyl)bis[4-(tert-butyl)pyridin-1-ium] diiodide (MB327) as a re-sensitizer of the desensitized nAChR. bispyridinium compound 1,1"-(propane-1,3-diyl)bis[4-(tert-butyl)pyridin-1-ium] diiodide 63-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-203 30362667-4 2018 Previous electrophysiological studies identified the symmetric bispyridinium compound 1,1"-(propane-1,3-diyl)bis[4-(tert-butyl)pyridin-1-ium] diiodide (MB327) as a re-sensitizer of the desensitized nAChR. MB327 152-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-203 30403486-0 2018 Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an alpha7-nAChR, alpha9-nAChR Antagonist and of a Pro-Oxidant Mitocan. onium-alkyloxy-stilbene 50-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 30403486-4 2018 We found that lengthening the ethylene bridge in the triethylammonium derivatives results in more potent and selective toxicity toward adenocarcinoma and glioblastoma cells, which was paralleled by increased alpha7 and alpha9alpha10 nAChR antagonism and improved ability of reducing mitochondrial ATP production. ethylene 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 30403486-4 2018 We found that lengthening the ethylene bridge in the triethylammonium derivatives results in more potent and selective toxicity toward adenocarcinoma and glioblastoma cells, which was paralleled by increased alpha7 and alpha9alpha10 nAChR antagonism and improved ability of reducing mitochondrial ATP production. triethylammonium 53-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 30248622-3 2018 METHODS: In a four-way cross-over study, eyes-closed rest EEG was recorded in 28 healthy subjects receiving mecamylamine-a nicotinic acetylcholine receptor (nAChR) antagonist, which induces temporary cognitive dysfunction in healthy subjects-with co-administration of placebo, nicotine or galantamine. mecamylamine-a 108-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 30069700-2 2018 We demonstrate that two short-chain alpha-neurotoxins (SalphaNTx) functionally inhibit human muscle-type nAChR, but are markedly more reversible than against rat receptors. salphantx 55-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 29619740-6 2018 In this regard, nicotine, which has been associated with relevant neuroprotective effects mainly through activation of the nicotinic acetylcholine receptor (nAChR), exerts its effects at least in part by acting directly on mitochondrial physiology and morphology. Nicotine 16-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 29619740-6 2018 In this regard, nicotine, which has been associated with relevant neuroprotective effects mainly through activation of the nicotinic acetylcholine receptor (nAChR), exerts its effects at least in part by acting directly on mitochondrial physiology and morphology. Nicotine 16-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 29619740-7 2018 Additionally, a recent description of mitochondrial nAChR localization suggests a nicotine-dependent mitochondrial function. Nicotine 82-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 30607728-4 2018 The affinity of the synthesized oligoarginines for nAChR depended on the number of amino acid residues in the chain. oligoarginines 32-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 30248622-3 2018 METHODS: In a four-way cross-over study, eyes-closed rest EEG was recorded in 28 healthy subjects receiving mecamylamine-a nicotinic acetylcholine receptor (nAChR) antagonist, which induces temporary cognitive dysfunction in healthy subjects-with co-administration of placebo, nicotine or galantamine. mecamylamine-a 108-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 30248622-4 2018 RESULTS: Using machine learning to optimally contrast the effects of 30 mg of mecamylamine and placebo on the brain, we developed a nAChR index that consists of 10 EEG biomarkers and shows high classification accuracy (~95% non-cross-validated, ~70% cross-validated). Mecamylamine 78-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 30248622-5 2018 Importantly, using the nAChR index, we demonstrate reversal of mecamylamine-induced neurophysiological effects due to 16 mg of galantamine as well as administering 21 mg of nicotine transdermally. Mecamylamine 63-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30248622-5 2018 Importantly, using the nAChR index, we demonstrate reversal of mecamylamine-induced neurophysiological effects due to 16 mg of galantamine as well as administering 21 mg of nicotine transdermally. Galantamine 127-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30248622-5 2018 Importantly, using the nAChR index, we demonstrate reversal of mecamylamine-induced neurophysiological effects due to 16 mg of galantamine as well as administering 21 mg of nicotine transdermally. Nicotine 173-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 30243424-1 2018 Mecamylamine is a nicotinic acetylcholine receptor (nAChR) antagonist that was recently used in a clinical trial to treat alcohol use disorder (AUD) in both smokers and non-smokers. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-50 30243424-1 2018 Mecamylamine is a nicotinic acetylcholine receptor (nAChR) antagonist that was recently used in a clinical trial to treat alcohol use disorder (AUD) in both smokers and non-smokers. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 30243424-1 2018 Mecamylamine is a nicotinic acetylcholine receptor (nAChR) antagonist that was recently used in a clinical trial to treat alcohol use disorder (AUD) in both smokers and non-smokers. Alcohols 122-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-50 30243424-1 2018 Mecamylamine is a nicotinic acetylcholine receptor (nAChR) antagonist that was recently used in a clinical trial to treat alcohol use disorder (AUD) in both smokers and non-smokers. Alcohols 122-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 30302403-3 2018 Here, using molecular dynamics simulations and single channel recordings, we show that ethanol interacts with a negatively charged amino acid within an extracellular region of the neuromuscular nicotinic acetylcholine receptor (nAChR), thereby altering its global conformation and reducing the single channel current amplitude. Ethanol 87-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-226 30302403-3 2018 Here, using molecular dynamics simulations and single channel recordings, we show that ethanol interacts with a negatively charged amino acid within an extracellular region of the neuromuscular nicotinic acetylcholine receptor (nAChR), thereby altering its global conformation and reducing the single channel current amplitude. Ethanol 87-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 228-233 30302403-4 2018 Charge reversal of the negatively charged amino acid abolishes the nAChR-ethanol interaction. Ethanol 73-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 30704714-2 2018 Electrophysiological and molecular approaches have demonstrated the presence of several nAChR subtypes with different affinities for neonicotinoid insecticides. Neonicotinoids 133-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 30704714-6 2018 In this review, we discuss findings concerning the number of nAChR binding sites against neonicotinoid insecticides from radioligand binding studies on native tissues. Neonicotinoids 89-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 30704714-8 2018 Finally, we demonstrate that neonicotinoid-nAChR binding sites are also linked to biological samples used and insect species. Neonicotinoids 29-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 28942487-0 2018 Erratum to: The crystal structure of Ac-AChBP in complex with alpha-conotoxin LvIA reveals the mechanism of its selectivity towards different nAChR subtypes. ac-achbp 37-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 29980822-1 2018 RATIONALE AND OBJECTIVE: Two mechanisms underlie smoking cessation efficacies of alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. Nicotine 216-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 29980822-4 2018 Agonist activity is comprised of nAChR activation and desensitization, which were expressed as percentages of desensitization and activation by nicotine from smoking. Nicotine 144-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 29980822-5 2018 Antagonist activity was expressed as the reduction in nAChR occupancy by nicotine during smoking in the presence of an agonist. Nicotine 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 29980822-8 2018 Other discontinued nAChR agonists have lower agonist and antagonist activities at alpha4beta2 nAChRs and are inactive or less efficacious than NRT (dianicline, ABT-089, CP-601927, CP-601932). dianicline 148-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 29980822-8 2018 Other discontinued nAChR agonists have lower agonist and antagonist activities at alpha4beta2 nAChRs and are inactive or less efficacious than NRT (dianicline, ABT-089, CP-601927, CP-601932). 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 160-163 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 30072754-1 2018 Nicotine and acetylcholine cause immunosuppresion by signaling to the alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) on immune cells. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 30072754-1 2018 Nicotine and acetylcholine cause immunosuppresion by signaling to the alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) on immune cells. Acetylcholine 13-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 30072754-2 2018 Neonicotinoids are nAChR agonists and widly used insecticides. Neonicotinoids 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 29759142-3 2018 Fab35 partially inhibited nAChR downmodulation, blocked EAMG serum-induced binding of polyclonal antibodies and complement deposition in vitro. fab35 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 29784663-1 2018 Evidence suggests that the alpha4beta2, but not the alpha7, subtype of the nicotinic acetylcholine receptor (nAChR) plays a key role in mediating the behavioral effects of nicotine and related drugs. Nicotine 172-180 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-107 29784663-1 2018 Evidence suggests that the alpha4beta2, but not the alpha7, subtype of the nicotinic acetylcholine receptor (nAChR) plays a key role in mediating the behavioral effects of nicotine and related drugs. Nicotine 172-180 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 28726253-2 2018 The aim of this study was to identify molecularly, biochemically and pharmacologically which nAChR subtypes are expressed and functionally activated by nicotine in lung cancer cell lines. Nicotine 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 28726253-4 2018 KEY RESULTS: The two adenocarcinoma cell lines express distinctive nAChR subtypes, and this affects their nicotine-induced proliferation. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 29681847-9 2018 Reduced nAChR-mediated anti-inflammation due to the loss of nicotinic innervation might lead to the transformation of glial cells and release of inflammatory mediators, lowering the buffering of extracellular potassium and glutamate metabolism. Potassium 209-218 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 8-13 29672680-7 2018 Therefore, using the recently developed alpha4beta2-nAChR-specific radioligand (-)-18F-flubatine and PET, we aimed to quantify the alpha4beta2-nAChR availability and its relationship to specific cognitive dysfunction in mild Alzheimer"s dementia. 18f-flubatine 83-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 29672680-7 2018 Therefore, using the recently developed alpha4beta2-nAChR-specific radioligand (-)-18F-flubatine and PET, we aimed to quantify the alpha4beta2-nAChR availability and its relationship to specific cognitive dysfunction in mild Alzheimer"s dementia. 18f-flubatine 83-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 29672680-15 2018 Using (-)-18F-flubatine PET in patients with mild Alzheimer"s dementia, we show for the first time a cholinergic alpha4beta2-nAChR deficiency mainly present within the basal forebrain-cortical and septohippocampal cholinergic projections and a relationship between lower alpha4beta2-nAChR availability and impairment of distinct cognitive domains, notably episodic memory and executive function/working memory. fluoronorchloroepibatidine 14-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 29672680-16 2018 This shows the potential of (-)-18F-flubatine as PET biomarker of cholinergic alpha4beta2-nAChR dysfunction and specific cognitive decline. fluoronorchloroepibatidine 35-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 29588343-4 2018 Both influx of calcium through the alpha7 nicotinic acetylcholine receptor (nAChR) channel as well as the binding of intracellular G proteins were involved in the effect of PNU120596 on intracellular calcium. Calcium 15-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 29588343-4 2018 Both influx of calcium through the alpha7 nicotinic acetylcholine receptor (nAChR) channel as well as the binding of intracellular G proteins were involved in the effect of PNU120596 on intracellular calcium. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 173-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 29588343-4 2018 Both influx of calcium through the alpha7 nicotinic acetylcholine receptor (nAChR) channel as well as the binding of intracellular G proteins were involved in the effect of PNU120596 on intracellular calcium. Calcium 200-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 29588343-7 2018 From the model, allosteric modulation of the receptor activates CICR locally via ryanodine receptors and augments IICR through enhanced calcium influx due to prolonged alpha7 nAChR opening. Calcium 136-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 175-180 29791835-5 2018 Electrophysiology, coupled with two-photon microscopy and laser flash photolysis of photoactivatable nicotine, was used to demonstrate nAChR functional activity in the somatodendritic subcellular compartment of VTA VGLUT2+ neurons. Nicotine 101-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 29215705-8 2018 Moreover, nicotine induced expressions of CTGF, and TGF-beta in fibroblasts as identified through alpha7 nicotinic acetylcholine receptor (nAChR)-dependent activation of the AKT/TAZ signaling mechanism. Nicotine 10-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 29572431-3 2018 Efferent activation inhibits OHC active amplification within the mammalian cochlea, through the activation of a calcium-permeable alpha9alpha10 ionotropic cholinergic nicotinic receptor (nAChR), functionally coupled to calcium activated SK2 potassium channels. Calcium 112-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 29681847-9 2018 Reduced nAChR-mediated anti-inflammation due to the loss of nicotinic innervation might lead to the transformation of glial cells and release of inflammatory mediators, lowering the buffering of extracellular potassium and glutamate metabolism. Glutamic Acid 223-232 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 8-13 20301348-15 1993 Individuals with ADNFLE associated with the CHRNA4 pathogenic variant p.Ser284Leu are more responsive to zonisamide than carbamazepine. Zonisamide 105-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-50 29428175-1 2018 The alpha7 nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel (LGIC) that plays an important role in cellular calcium signaling and contributes to several neurological diseases. Calcium 130-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 29428175-2 2018 Agonist binding to the alpha7 nAChR induces fast channel activation followed by inactivation and prolonged desensitization while triggering long-lasting calcium signaling. Calcium 153-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 29621993-1 2018 BACKGROUND: The identification of variants in the nicotinic acetylcholine receptor (nAChR) subunit genes associated with smoking phenotypes are increasingly important for prevention and treatment of nicotine dependence. Nicotine 199-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-82 29621993-1 2018 BACKGROUND: The identification of variants in the nicotinic acetylcholine receptor (nAChR) subunit genes associated with smoking phenotypes are increasingly important for prevention and treatment of nicotine dependence. Nicotine 199-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 28778837-2 2018 Nicotinic acetylcholine receptors (nAChR) have been shown to modulate ethanol behaviors in adult humans and in animal models; however, the role of these receptors in adolescent ethanol behaviors has not been explored. Ethanol 70-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 28778837-2 2018 Nicotinic acetylcholine receptors (nAChR) have been shown to modulate ethanol behaviors in adult humans and in animal models; however, the role of these receptors in adolescent ethanol behaviors has not been explored. Ethanol 70-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 20301348-15 1993 Individuals with ADNFLE associated with the CHRNA4 pathogenic variant p.Ser284Leu are more responsive to zonisamide than carbamazepine. Carbamazepine 121-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-50 29510587-7 2018 On the other hand, the nAChR antagonist mecamylamine strongly inhibited the growth and differentiation of organoids, suggesting the involvement of nAChRs in the regulation of proliferation and differentiation of Lgr5-positive stem cells. Mecamylamine 40-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 28762314-2 2018 Many nAChR subunits have been identified and shown to be involved in signal transduction on binding to them of either the neurotransmitter acetylcholine or exogenous ligands such as nicotine. Acetylcholine 139-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 29497086-5 2018 Human muscle nAChR is sensitive to mutations at position 418, with the Cys-to-Trp mutation resulting in a 16-fold potentiation in function that leads to a congenital myasthenic syndrome. Cysteine 71-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 29497086-5 2018 Human muscle nAChR is sensitive to mutations at position 418, with the Cys-to-Trp mutation resulting in a 16-fold potentiation in function that leads to a congenital myasthenic syndrome. Tryptophan 78-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 29495549-9 2018 In conclusion, this is the first study to show that prorocentrolide-A acts on both muscle and neuronal nAChRs, but with higher affinity on the muscle-type nAChR. prorocentrolide-a 52-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 28825423-1 2018 The aim of the trial was to assess whether extending plasma levels of the alpha7-nicotinic acetylcholine receptor (nAChR) agonist 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXB-A) over time enhances its cognitive effects in schizophrenia. 3-(2,4-dimethoxybenzylidene)anabaseine 130-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-113 28825423-1 2018 The aim of the trial was to assess whether extending plasma levels of the alpha7-nicotinic acetylcholine receptor (nAChR) agonist 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXB-A) over time enhances its cognitive effects in schizophrenia. 3-(2,4-dimethoxybenzylidene)anabaseine 130-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 28825423-1 2018 The aim of the trial was to assess whether extending plasma levels of the alpha7-nicotinic acetylcholine receptor (nAChR) agonist 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXB-A) over time enhances its cognitive effects in schizophrenia. 3-(2,4-dimethoxybenzylidene)anabaseine 171-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-113 28825423-1 2018 The aim of the trial was to assess whether extending plasma levels of the alpha7-nicotinic acetylcholine receptor (nAChR) agonist 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXB-A) over time enhances its cognitive effects in schizophrenia. 3-(2,4-dimethoxybenzylidene)anabaseine 171-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 29324040-5 2018 The structurally related sulfoximine sulfoxaflor and butenolide flupyradifurone are also nAChR agonists, and the mesoionic triflumezopyrim is a nAChR competitive modulator with little or no target-site cross-resistance. sulfoximine sulfoxaflor 25-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 29324040-5 2018 The structurally related sulfoximine sulfoxaflor and butenolide flupyradifurone are also nAChR agonists, and the mesoionic triflumezopyrim is a nAChR competitive modulator with little or no target-site cross-resistance. butenolide flupyradifurone 53-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 29324040-5 2018 The structurally related sulfoximine sulfoxaflor and butenolide flupyradifurone are also nAChR agonists, and the mesoionic triflumezopyrim is a nAChR competitive modulator with little or no target-site cross-resistance. triflumezopyrim 123-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 29095106-8 2018 Such a fitness cost could explain why target site resistances to neonicotinoids in pest insect populations have been associated specific amino acid replacement mutations in nAChR subunits, rather than loss of function. Neonicotinoids 65-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 29370396-2 2018 Although alpha4beta2 nicotinic acetylcholine receptor (alpha4beta2 nAChR) in the dorsal raphe nucleus plays a key role in the ketamine-induced prefrontal serotonin release, the source of cholinergic afferents, and its role is unclear. Ketamine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 29370396-2 2018 Although alpha4beta2 nicotinic acetylcholine receptor (alpha4beta2 nAChR) in the dorsal raphe nucleus plays a key role in the ketamine-induced prefrontal serotonin release, the source of cholinergic afferents, and its role is unclear. Serotonin 154-163 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 29370396-7 2018 This increase was attenuated by intra-dorsal raphe nucleus injection of dihydro-beta-erythroidine, an alpha4beta2 nAChR antagonist, or NBQX, an AMPA receptor antagonist. Dihydro-beta-Erythroidine 72-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 29352227-2 2018 In this study, we characterize the pharmacological interactions of the nAChRs PAM, LY2087101, with the alpha4beta2 nAChR using mutational and computational analyses. LY 2087101 83-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 29110618-6 2018 Recent studies have demonstrated that the alpha4, beta2, and alpha7 subunits of the nicotinic acetylcholine receptor (nAChR) participate in the cognitive-enhancing effects of nicotine. Nicotine 175-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 28762314-2 2018 Many nAChR subunits have been identified and shown to be involved in signal transduction on binding to them of either the neurotransmitter acetylcholine or exogenous ligands such as nicotine. Nicotine 182-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 28762314-5 2018 This review intends to provide insights into recent advances in nAChR signaling, considering the subtypes and subunits of nAChRs and their roles in nicotinic cholinergic systems, including structure, diversity, functional allosteric modulation, targeted knockout mutations, and rare variations of specific subunits, and the potency and functional effects of mutations by focusing on their effects on nicotine addiction (NA) and smoking cessation (SC). Nicotine 400-408 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 29129316-4 2017 Unexpectedly, both deletions and duplications lead to decreased alpha7 nAChR-associated calcium flux. Calcium 88-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 28859996-2 2018 Nicotinic acetylcholine receptor (nAChR) agonists such as nicotine may serve as a novel therapeutic approach for this population. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 28859996-2 2018 Nicotinic acetylcholine receptor (nAChR) agonists such as nicotine may serve as a novel therapeutic approach for this population. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 29058146-9 2018 Finally, we have also investigated the effect of nAChR-targeted tobacco cessation drugs on catecholamine release in chromaffin cells. Catecholamines 91-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 29058146-9 2018 Finally, we have also investigated the effect of nAChR-targeted tobacco cessation drugs on catecholamine release in chromaffin cells. chromaffin 116-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 29074617-9 2017 Moreover, nicotine altered nAChR assembly in the ER, resulting in increased production of the receptor isoform that traffics more efficiently to the cell surface. Nicotine 10-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 29074617-10 2017 We conclude that the combined effects of the increased assembly of one nAChR stoichiometry and its preferential trafficking likely drive the up-regulation of nAChRs on the cell surface upon nicotine exposure. Nicotine 190-198 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 28875553-3 2018 Nifene had subnanomolar affinities for halpha2beta2 (0.34 nM), halpha3beta2 (0.80 nM) and halpha4beta2 (0.83 nM) nAChR but weaker (27-219 nM) for hbeta4 nAChR subtypes and 169 nM for halpha7 nAChR. nifene 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 28875553-3 2018 Nifene had subnanomolar affinities for halpha2beta2 (0.34 nM), halpha3beta2 (0.80 nM) and halpha4beta2 (0.83 nM) nAChR but weaker (27-219 nM) for hbeta4 nAChR subtypes and 169 nM for halpha7 nAChR. nifene 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 28875553-3 2018 Nifene had subnanomolar affinities for halpha2beta2 (0.34 nM), halpha3beta2 (0.80 nM) and halpha4beta2 (0.83 nM) nAChR but weaker (27-219 nM) for hbeta4 nAChR subtypes and 169 nM for halpha7 nAChR. nifene 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 29618714-7 2018 T-REx293 cells expressed the nicotinic acetylcholine receptor (nAchR) and tubocurarine, an nAChR antagonist, completely blocked the effects of nicotine. Tubocurarine 74-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 29618714-7 2018 T-REx293 cells expressed the nicotinic acetylcholine receptor (nAchR) and tubocurarine, an nAChR antagonist, completely blocked the effects of nicotine. Nicotine 143-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-61 29618714-7 2018 T-REx293 cells expressed the nicotinic acetylcholine receptor (nAchR) and tubocurarine, an nAChR antagonist, completely blocked the effects of nicotine. Nicotine 143-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 29618714-7 2018 T-REx293 cells expressed the nicotinic acetylcholine receptor (nAchR) and tubocurarine, an nAChR antagonist, completely blocked the effects of nicotine. Nicotine 143-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 29129316-5 2017 For deletions, this decrease in alpha7 nAChR-dependent calcium flux is expected due to haploinsufficiency of CHRNA7. Calcium 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 29129316-8 2017 Here, we showed that alpha7 nAChR-dependent calcium signal cascades are downregulated in both 15q13.3 deletion and duplication NPCs. Calcium 44-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 28416445-8 2017 GeXIVA is therefore a unique ligand that might prove useful for further probing of binding sites on the alpha9alpha10 nAChR. gexiva 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 28494312-5 2017 The selective ganglionic nAChR agonist DMPP used as a positive control, was a potent activator and desensitizer of nAChR expressed by SH-SY5Y cells. Dimethylphenylpiperazinium Iodide 39-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 28963927-0 2017 Human biodistribution and dosimetry of [18F]nifene, an alpha4beta2* nicotinic acetylcholine receptor PET tracer. nifene 39-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-100 28963927-2 2017 [18F]Nifene is a positron emission tomography (PET) ligand that has shown promise for in vivo imaging of the alpha4beta2* nAChR system in preclinical models and humans. nifene 5-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 28963927-10 2017 CONCLUSIONS: [18F]Nifene is a safe PET radioligand for imaging the alpha4beta2* nAChR system in humans. nifene 18-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 28963927-12 2017 These results facilitate safe development of future [18F]nifene studies to image the alpha4beta2* nAChR system in humans. nifene 57-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 28494312-3 2017 The objective of this study was to test the hypothesis that anagyrine but not lupanine or sparteine can directly, without metabolism, desensitize nicotinic acetylcholine receptors (nAChR) in a cell culture model. anagyrine 60-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-179 28494312-3 2017 The objective of this study was to test the hypothesis that anagyrine but not lupanine or sparteine can directly, without metabolism, desensitize nicotinic acetylcholine receptors (nAChR) in a cell culture model. anagyrine 60-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 28494312-5 2017 The selective ganglionic nAChR agonist DMPP used as a positive control, was a potent activator and desensitizer of nAChR expressed by SH-SY5Y cells. Dimethylphenylpiperazinium Iodide 39-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 28494312-8 2017 Anagyrine was a desensitizer of nAChR with DC50 values of 6.9 and 139muM in SH-SY5Y and TE-671 cells, respectively. anagyrine 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 29196725-2 2017 There is growing evidence that genetic variations in nicotinic acetylcholine receptor (nAChR) subunits influence the risk of nicotine dependence and the ability to quit smoking. Nicotine 125-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-85 28494312-9 2017 These results confirm the hypothesis that anagyrine is a potent and effective desensitizer of nAChR, and that anagyrine can directly, without metabolism, desensitize nAChR. anagyrine 42-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 29196725-2 2017 There is growing evidence that genetic variations in nicotinic acetylcholine receptor (nAChR) subunits influence the risk of nicotine dependence and the ability to quit smoking. Nicotine 125-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 29196725-3 2017 To investigate the role of polymorphisms in nAChR genes on smoking quantity and the outcome of smoking-cessation therapies, we carried out an association study on 337 smokers who underwent pharmacotherapy with varenicline, bupropion, nicotine replacement therapy (NRT) alone, or NRT plus bupropion. Varenicline 210-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28494312-9 2017 These results confirm the hypothesis that anagyrine is a potent and effective desensitizer of nAChR, and that anagyrine can directly, without metabolism, desensitize nAChR. anagyrine 110-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 29196725-3 2017 To investigate the role of polymorphisms in nAChR genes on smoking quantity and the outcome of smoking-cessation therapies, we carried out an association study on 337 smokers who underwent pharmacotherapy with varenicline, bupropion, nicotine replacement therapy (NRT) alone, or NRT plus bupropion. Bupropion 223-232 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28602809-10 2017 They are suggested to mediate the deleterious effects of the major tobacco component, nicotine, a nAChR agonist. Nicotine 86-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 29196725-3 2017 To investigate the role of polymorphisms in nAChR genes on smoking quantity and the outcome of smoking-cessation therapies, we carried out an association study on 337 smokers who underwent pharmacotherapy with varenicline, bupropion, nicotine replacement therapy (NRT) alone, or NRT plus bupropion. Nicotine 234-242 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 29196725-3 2017 To investigate the role of polymorphisms in nAChR genes on smoking quantity and the outcome of smoking-cessation therapies, we carried out an association study on 337 smokers who underwent pharmacotherapy with varenicline, bupropion, nicotine replacement therapy (NRT) alone, or NRT plus bupropion. Bupropion 288-297 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28586306-3 2017 Nicotine is an exogenous agonist of nicotinic acetylcholine receptors (nAChRs) and acts as a pharmacological chaperone in the regulation of nAChR expression, potentially intervening in age-related changes in diverse molecular pathways leading to pathology. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 29040265-1 2017 The majority of patients with myasthenia gravis (MG), an organ-specific autoimmune disease, harbor autoantibodies that attack the nicotinic acetylcholine receptor (nAChR-Abs) at the neuromuscular junction of skeletal muscles, resulting in muscle weakness. Acetylcholine 140-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 28878016-0 2017 Enantiomeric barbiturates bind distinct inter- and intrasubunit binding sites in a nicotinic acetylcholine receptor (nAChR). Barbiturates 13-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-115 28878016-0 2017 Enantiomeric barbiturates bind distinct inter- and intrasubunit binding sites in a nicotinic acetylcholine receptor (nAChR). Barbiturates 13-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 28878016-9 2017 Propofol, a general anesthetic that binds to GABAAR intersubunit sites, inhibited [3H]S-mTFD-MPPB photolabeling of these nAChR intrasubunit binding sites. Propofol 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 28878016-9 2017 Propofol, a general anesthetic that binds to GABAAR intersubunit sites, inhibited [3H]S-mTFD-MPPB photolabeling of these nAChR intrasubunit binding sites. Tritium 83-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 28878016-9 2017 Propofol, a general anesthetic that binds to GABAAR intersubunit sites, inhibited [3H]S-mTFD-MPPB photolabeling of these nAChR intrasubunit binding sites. mtfd-mppb 88-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 29062606-4 2017 Using choline as a nicotinic acetylcholine receptor (nAChR) agonist, we found that nAChR stimulation was sufficient to protect SH-SY5Y cells against cell death from MPP+. Choline 6-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-51 29062606-4 2017 Using choline as a nicotinic acetylcholine receptor (nAChR) agonist, we found that nAChR stimulation was sufficient to protect SH-SY5Y cells against cell death from MPP+. Choline 6-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 29062606-4 2017 Using choline as a nicotinic acetylcholine receptor (nAChR) agonist, we found that nAChR stimulation was sufficient to protect SH-SY5Y cells against cell death from MPP+. Choline 6-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 29062606-5 2017 Blocking alpha7 nAChR with methyllycaconitine (MLA) prevented the protective effects of nicotine, demonstrating that these receptors are necessary for the neuroprotective effects of nicotine. methyllycaconitine 27-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 29062606-5 2017 Blocking alpha7 nAChR with methyllycaconitine (MLA) prevented the protective effects of nicotine, demonstrating that these receptors are necessary for the neuroprotective effects of nicotine. methyllycaconitine 47-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 29062606-5 2017 Blocking alpha7 nAChR with methyllycaconitine (MLA) prevented the protective effects of nicotine, demonstrating that these receptors are necessary for the neuroprotective effects of nicotine. Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 29062606-5 2017 Blocking alpha7 nAChR with methyllycaconitine (MLA) prevented the protective effects of nicotine, demonstrating that these receptors are necessary for the neuroprotective effects of nicotine. Nicotine 182-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 29062606-8 2017 In conclusion, our data indicate that nicotine likely exerts neuroprotective effects in PD through the alpha7 nAChR and downstream pathways including PARP-1 and caspase-3. Nicotine 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 28851841-1 2017 Conotoxin GeXIVA inhibits the alpha9alpha10 nicotinic acetylcholine receptor (nAChR) and is analgesic in animal models of pain. gexiva 10-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 28874590-3 2017 We addressed these challenges in the context of the alpha4beta2 nAChR, a widespread ligand-gated ion channel in the brain and a target for nicotine addiction therapy, and the 19-residue conotoxin alpha-GID that antagonizes it. Nicotine 139-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 28815595-6 2017 Escitalopram and fluvoxamine (100 nM to 1 muM) reversibly inhibited nAChR currents. Citalopram 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 28815595-6 2017 Escitalopram and fluvoxamine (100 nM to 1 muM) reversibly inhibited nAChR currents. Fluvoxamine 17-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 28815595-7 2017 The sigma-1 receptor antagonists NE-100 and BD-1047 also blocked nAChR currents ( 50% block at 100 nM) as did PRE-084, a sigma-1 receptor agonist. N-(2-(3,4-Dichlorphenyl)ethyl)-N,N',N'-trimethyl-1,2-ethandiamin 44-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 28815595-8 2017 Block of nAChR currents by fluvoxamine and NE-100 was not additive suggesting a common site of action. Fluvoxamine 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 28815595-8 2017 Block of nAChR currents by fluvoxamine and NE-100 was not additive suggesting a common site of action. N,N-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride 43-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 28877969-11 2017 These findings connect CHRNA4 genotype, CO network activation, and sustained alertness, providing insights into how genetics shapes individuals" cognitive control abilities.SIGNIFICANCE STATEMENT The nicotinic acetylcholine system plays a central role in neuromodulatory regulation of cognitive control processes and is dysregulated in several neuropsychiatric disorders. Acetylcholine 210-223 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-29 28766701-4 2017 Fenofibrate, a common lipid-regulating drug, is an agonist at peroxisome proliferator-activated receptor alpha (PPARalpha) that is a ligand-activated transcription factor, which negatively modulates the function of beta2-containing nAChR. Fenofibrate 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 232-237 28935799-3 2017 Among them is epibatidine, a nicotinic acetylcholine receptor (nAChR) agonist that is lethal at microgram doses. epibatidine 14-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-61 28935799-3 2017 Among them is epibatidine, a nicotinic acetylcholine receptor (nAChR) agonist that is lethal at microgram doses. epibatidine 14-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 28935799-4 2017 Epibatidine shares a highly conserved binding site with acetylcholine, making it difficult to evolve resistance yet maintain nAChR function. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 28935799-5 2017 Electrophysiological assays of human and frog nAChR revealed that one amino acid replacement, which evolved three times in poison frogs, decreased epibatidine sensitivity but at a cost of acetylcholine sensitivity. epibatidine 147-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 28606760-1 2017 The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), gamma-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Cysteine 15-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 28878681-2 2017 Our previous studies suggested that alpha5-nAChR mediates nicotine-induced lung cancer cell proliferation, migration, and invasion in vitro. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 28878681-6 2017 In vivo, alpha5-nAChR silencing inhibited the growth of lung tumors, especially in the context of nicotine exposure. Nicotine 98-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 28878681-8 2017 These results reveal that alpha5-nAChR silencing inhibits the progression of nicotine-related NSCLC, making this receptor a potential pharmacological target for the treatment of nicotine-related lung carcinogenesis. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 28878681-8 2017 These results reveal that alpha5-nAChR silencing inhibits the progression of nicotine-related NSCLC, making this receptor a potential pharmacological target for the treatment of nicotine-related lung carcinogenesis. Nicotine 178-186 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 28718646-3 2017 Taking advantage of more than 100 AChBP crystal structures in the Protein DataBank (PDB), we explored the relationship between the size, efficiency, and efficacy of nAChR ligands and the C-loop movement. achbp 34-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 28718646-4 2017 We found that the size of the ligand is correlated with the opening of the C-loop, which can be used in selecting AChBP crystal structures with appropriate C-loop opening to be used for nAChR ligand docking. achbp 114-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 28791704-6 2017 Granulocyte abundance, nAChR expression, and nAChR upregulation following chronic nicotine administration makes granulocytes interesting models for identifying protein markers of nicotine exposure. Nicotine 82-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 28791704-7 2017 Nicotinic receptor subunits and several non-nAChR proteins have been identified as protein markers of granulocyte nicotine exposure. Nicotine 114-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28420041-8 2017 CONCLUSION: The binding profile and tracer kinetics of [18 F]nifene make it a promising alpha4beta2* nAChR radiotracer for scientific research in humans, with reliable DVR test-retest reproducibility. nifene 61-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 28585699-9 2017 Use of the beta2-selective nAChR antagonist, dihydro-beta-erythroidine, suggests that loss of cholinergic efficacy may also be the result of an age-related subunit switch from high affinity beta2-containing nAChRs to low affinity beta4-containing nAChRs, in addition to the loss of total nAChR number. Dihydro-beta-Erythroidine 45-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 28585699-9 2017 Use of the beta2-selective nAChR antagonist, dihydro-beta-erythroidine, suggests that loss of cholinergic efficacy may also be the result of an age-related subunit switch from high affinity beta2-containing nAChRs to low affinity beta4-containing nAChRs, in addition to the loss of total nAChR number. Dihydro-beta-Erythroidine 45-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 207-212 28750889-0 2017 Reciprocal activation of alpha5-nAChR and STAT3 in nicotine-induced human lung cancer cell proliferation. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 28750889-6 2017 Nicotine increased the levels of alpha5-nAChR mRNA and protein in NSCLC cell lines and activated the JAK2/STAT3 signaling cascade. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 28750889-7 2017 Nicotine-induced activation of JAK2/STAT3 signaling was inhibited by the silencing of alpha5-nAChR. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 28750889-10 2017 By silencing STAT3 expression, nicotine-induced upregulation of alpha5-nAChR was suppressed. Nicotine 31-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 28750889-11 2017 Downregulation of alpha5-nAChR and/or STAT3 expression inhibited nicotine-induced lung cancer cell proliferation. Nicotine 65-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 28750889-12 2017 These results suggest that there is a feedback loop between alpha5-nAChR and STAT3 that contributes to the nicotine-induced tumor cell proliferation, which indicates that alpha5-nAChR is an important therapeutic target involved in tobacco-associated lung carcinogenesis. Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 28750889-12 2017 These results suggest that there is a feedback loop between alpha5-nAChR and STAT3 that contributes to the nicotine-induced tumor cell proliferation, which indicates that alpha5-nAChR is an important therapeutic target involved in tobacco-associated lung carcinogenesis. Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 27581650-2 2017 Despite varying reports in the literature as to which receptor is ultimately responsible for interaction of RVG with the nervous system, there is a strong argument for major nicotinic acetylcholine receptor (nAChR) involvement. Acetylcholine 184-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 28725182-2 2017 Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. Phosphorylcholine 27-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 28725182-2 2017 Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. Phosphorylcholine 43-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 28725182-2 2017 Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. 1,2-Dipalmitoylphosphatidylcholine 51-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 28725182-2 2017 Furthermore, we identified phosphocholine (PC) and dipalmitoylphosphatidylcholine (DPPC) as novel nicotinic agonists that elicit metabotropic activity at monocytic nAChR. 1,2-Dipalmitoylphosphatidylcholine 83-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 28319594-5 2017 During the follow-up, the reduction of anti-nAChR antibodies produced by immunoadsorption was associated with a diminished orthostatic hypotension, a restored capability to increase LF/HF, LFSAP and norepinephrine in upright position, a decline in the intensity of autonomic symptoms and an improvement of life quality. Norepinephrine 199-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28583088-10 2017 Finally, we found that liver-specific CHRNA4 transcription was highly correlated with genes involved in the nicotine metabolism, including CYP2A6, UGT2B7, and FMO3. Nicotine 108-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-44 27421773-8 2017 In addition, drastic variation in the binding stability of Mongoose nAChR-alpha-Bungarotoxin (alpha-BTX) and human nAChR-alpha-BTX complexes were found at specific phase of MDS. alpha-btx 94-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 23-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 23-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-3 2017 Varenicline has been associated with adverse cardiovascular (CV) events, including myocardial infarction, which may be caused by activation of the alpha7 nAChR receptor that in turn stimulates parasympathetic output from the brainstem to the heart, release of catecholamines, and has a prothrombotic effect. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 28268112-3 2017 Varenicline has been associated with adverse cardiovascular (CV) events, including myocardial infarction, which may be caused by activation of the alpha7 nAChR receptor that in turn stimulates parasympathetic output from the brainstem to the heart, release of catecholamines, and has a prothrombotic effect. Catecholamines 260-274 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 28298165-3 2017 The alpha6beta2beta3 nAChR subtype is expressed in terminals of dopaminergic neurons that project to the nucleus accumbens and striatum and modulate dopamine release in brain regions involved in nicotine addiction. Dopamine 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 28298165-3 2017 The alpha6beta2beta3 nAChR subtype is expressed in terminals of dopaminergic neurons that project to the nucleus accumbens and striatum and modulate dopamine release in brain regions involved in nicotine addiction. Nicotine 195-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 27581650-5 2017 It is possible that nAChR-mediated uptake of RVG-derived peptides may serve as an attractive new approach for targeting drug delivery to the brain. rvg 45-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 27613895-4 2017 We have manually curated a set of genes believed to play a role in nicotine-induced nAChR upregulation. Nicotine 67-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 28212459-1 2017 Nicotinoids are agonists of the acetylcholine receptor (nAChR) and play important biochemical and pharmacological roles. nicotinoids 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 28499726-6 2017 This reduction was inhibited not only by mecamylamine, a nAChR antagonist, but also by PI3K and Akt inhibitors. Mecamylamine 41-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 28499726-8 2017 These results suggest that donepezil inhibits the inflammatory response induced by bradykinin via nAChR and PI3K-Akt pathway in astrocytes. Donepezil 27-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 28450546-10 2017 The data may also help to explain why genetic insults to alpha4 subunits are associated with working memory and attentional deficits and why alpha4beta2-nAChR agonists may have therapeutic potential.SIGNIFICANCE STATEMENT The acetylcholine (ACh) arousal system in the brain is needed for robust attention and working memory functions, but the receptor and cellular bases for its beneficial effects are poorly understood in the newly evolved primate brain. Acetylcholine 226-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 28450546-11 2017 The current study found that ACh stimulation of nicotinic receptors comprised of alpha4 and beta2 subunits (alpha4beta2-nAChR) enhanced the firing of neurons in the primate prefrontal cortex that subserve top-down attentional control and working memory. Acetylcholine 29-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 28100642-7 2017 Lynx1 is expressed in the habenulopeduncular tract, where alpha3beta4*-alpha5*-nAChR subtypes are critical contributors to the balance between nicotine aversion and reward. Nicotine 143-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 28221788-0 2017 Substituted 2-Aminopyrimidines Selective for alpha7-Nicotinic Acetylcholine Receptor Activation and Association with Acetylcholine Binding Proteins. 2-aminopyrimidine 12-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 28361878-4 2017 This study provides novel structural insights into the molecular basis for alpha-conotoxin activity at alpha3beta4 nAChR, a therapeutic target where subtype specific antagonists have potential to treat nicotine addiction and lung cancer. Nicotine 202-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 28221788-1 2017 Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. Acetylcholine 43-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-236 28221788-1 2017 Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. Acetylcholine 43-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 238-243 28221788-1 2017 Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. 4,6-substituted 2-aminopyrimidines 119-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-236 28221788-1 2017 Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. 4,6-substituted 2-aminopyrimidines 119-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 238-243 28221788-3 2017 Initial screening of a series of over 50 newly characterized 2-aminopyrimidines with affinity for AChBP showed only two to be agonists on the alpha7-nAChR below 10 muM concentration. 2-aminopyrimidine 61-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 28025040-7 2017 Mecamylamine, a nAChR inhibitor, suppressed not only these [Ca2+]i transients, but also IL-2 release and T cell proliferation. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 28293176-11 2017 Activation of nicotinic acetylcholine receptors (nAChRs) with nAChR agonist nicotine or DMPP had no effect on the excitability of RA PNs, and the nAChR antagonist mecamylamine failed to inhibit the effects of carbachol. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 28293176-11 2017 Activation of nicotinic acetylcholine receptors (nAChRs) with nAChR agonist nicotine or DMPP had no effect on the excitability of RA PNs, and the nAChR antagonist mecamylamine failed to inhibit the effects of carbachol. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 28293176-11 2017 Activation of nicotinic acetylcholine receptors (nAChRs) with nAChR agonist nicotine or DMPP had no effect on the excitability of RA PNs, and the nAChR antagonist mecamylamine failed to inhibit the effects of carbachol. Dimethylphenylpiperazinium Iodide 88-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 27531501-3 2017 Our results show that blockade of the alpha3beta4 nAChR in the MHb, but not the IPN prevented increases in locomotor responding as well as increases in accumbal dopamine overflow in sensitized animals. Dopamine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 27871840-4 2017 The measured Kd for acetylcholine binding to the uncoupled nAChR is similar to that for the resting state, confirming that the agonist binding site adopts a resting-state like conformation. Acetylcholine 20-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 27993517-1 2017 We describe the synthesis of quinuclidine-containing spiroguanidines and their utility as alpha7 neuronal nicotinic acetylcholine receptor (nAChR) partial agonists. Quinuclidines 29-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 27993517-1 2017 We describe the synthesis of quinuclidine-containing spiroguanidines and their utility as alpha7 neuronal nicotinic acetylcholine receptor (nAChR) partial agonists. spiroguanidines 53-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 27856558-3 2017 The neuronal alpha5 nicotinic acetylcholine receptor (nAChR) subunit is critically involved in nicotine dependence. Nicotine 95-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 27917874-4 2017 Since acetylcholine-binding protein (AChBP) from Lymnaea stagnalis is most closely related to the alpha-subunit of nAChRs, it has been used as a template for the N-terminal domain of alpha-subunit of nAChR to study the molecular recognition process of nAChR-ligand interactions, and to identify ligands with potential nAChR-like activities.Here we report the discovery and optimization of novel acetylcholine-binding protein ligands through screening, structure-activity relationships and structure-based design. Acetylcholine 6-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 27917874-4 2017 Since acetylcholine-binding protein (AChBP) from Lymnaea stagnalis is most closely related to the alpha-subunit of nAChRs, it has been used as a template for the N-terminal domain of alpha-subunit of nAChR to study the molecular recognition process of nAChR-ligand interactions, and to identify ligands with potential nAChR-like activities.Here we report the discovery and optimization of novel acetylcholine-binding protein ligands through screening, structure-activity relationships and structure-based design. Acetylcholine 6-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 27917874-4 2017 Since acetylcholine-binding protein (AChBP) from Lymnaea stagnalis is most closely related to the alpha-subunit of nAChRs, it has been used as a template for the N-terminal domain of alpha-subunit of nAChR to study the molecular recognition process of nAChR-ligand interactions, and to identify ligands with potential nAChR-like activities.Here we report the discovery and optimization of novel acetylcholine-binding protein ligands through screening, structure-activity relationships and structure-based design. Acetylcholine 6-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 28372298-12 2017 The functional activity of alpha7 nAChR was evaluated by calcium (Ca2+) influx mediated by nicotine using the Fluo-4 NW Calcium assay. Calcium 57-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 28372298-12 2017 The functional activity of alpha7 nAChR was evaluated by calcium (Ca2+) influx mediated by nicotine using the Fluo-4 NW Calcium assay. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 28372298-12 2017 The functional activity of alpha7 nAChR was evaluated by calcium (Ca2+) influx mediated by nicotine using the Fluo-4 NW Calcium assay. Fluo 4 110-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 28372298-12 2017 The functional activity of alpha7 nAChR was evaluated by calcium (Ca2+) influx mediated by nicotine using the Fluo-4 NW Calcium assay. Calcium 120-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 28372298-18 2017 CONCLUSIONS: At the concentration used, nicotine had an adverse effect on the proliferation and chondrogenic differentiation of hWJ-MSCs which was probably impaired through a alpha7 nAChR mediation. Nicotine 40-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 27678550-3 2017 OBJECTIVES: The aim was to test whether low doses of the nAChR antagonist mecamylamine would benefit performance in human volunteers. Mecamylamine 74-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 28176635-8 2017 Co-crystallisation of neonicotinoids with the acetylcholine binding protein (AChBP), a surrogate for the nAChR ligand binding domain, has proved instructive. Neonicotinoids 22-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 27805736-1 2017 Varenicline is a nicotinic acetylcholine receptor (nAChR) agonist used to treat nicotine addiction, but a live debate persists concerning its mechanism of action in reducing nicotine consumption. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-49 27805736-1 2017 Varenicline is a nicotinic acetylcholine receptor (nAChR) agonist used to treat nicotine addiction, but a live debate persists concerning its mechanism of action in reducing nicotine consumption. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 27805736-1 2017 Varenicline is a nicotinic acetylcholine receptor (nAChR) agonist used to treat nicotine addiction, but a live debate persists concerning its mechanism of action in reducing nicotine consumption. Nicotine 80-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 27805736-2 2017 Although initially reported as alpha4beta2 selective, varenicline was subsequently shown to activate other nAChR subtypes implicated in nicotine addiction including alpha3beta4. Varenicline 54-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 27805736-2 2017 Although initially reported as alpha4beta2 selective, varenicline was subsequently shown to activate other nAChR subtypes implicated in nicotine addiction including alpha3beta4. Nicotine 136-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 27573666-1 2017 BACKGROUND: The nicotinic acetylcholine receptor (nAChR) gene family encodes for subunits of acetylcholine gated ion channels. Acetylcholine 26-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 28863823-1 2017 Cholesterol is a potent modulator of the nicotinic acetylcholine receptor (nAChR) from Torpedo. Cholesterol 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 28863823-1 2017 Cholesterol is a potent modulator of the nicotinic acetylcholine receptor (nAChR) from Torpedo. Cholesterol 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 28863823-2 2017 Here, we review current understanding of the mechanisms underlying cholesterol-nAChR interactions in the context of increasingly available high-resolution structural and functional data. Cholesterol 67-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 28863823-4 2017 In the absence of cholesterol and anionic lipids, the nAChR adopts an uncoupled conformation that binds agonist but does not undergo agonist-induced conformational transitions-unless the nAChR is located in a relatively thick lipid bilayer, such as that found in cholesterol-rich lipid rafts. Lipid Bilayers 226-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 28863823-4 2017 In the absence of cholesterol and anionic lipids, the nAChR adopts an uncoupled conformation that binds agonist but does not undergo agonist-induced conformational transitions-unless the nAChR is located in a relatively thick lipid bilayer, such as that found in cholesterol-rich lipid rafts. Lipid Bilayers 226-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 28863823-4 2017 In the absence of cholesterol and anionic lipids, the nAChR adopts an uncoupled conformation that binds agonist but does not undergo agonist-induced conformational transitions-unless the nAChR is located in a relatively thick lipid bilayer, such as that found in cholesterol-rich lipid rafts. Cholesterol 263-274 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 28863823-8 2017 We evaluate the nature of cholesterol-nAChR interactions, considering the evidence supporting the roles of both direct binding to allosteric sites and cholesterol-induced changes in bulk membrane physical properties. Cholesterol 26-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 27645992-11 2016 Agonists or antagonists for these unorthodox sites might be selective and effective drugs for modulating nAChR function to treat nicotine addiction and other disorders. Nicotine 129-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 28105289-1 2017 We describe the synthesis of quinuclidine-containing spiroimidates and their utility as alpha7 nicotinic acetylcholine receptor (nAChR) partial agonists. Quinuclidines 29-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 28105289-1 2017 We describe the synthesis of quinuclidine-containing spiroimidates and their utility as alpha7 nicotinic acetylcholine receptor (nAChR) partial agonists. spiroimidates 53-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 27907022-14 2016 nAChR antagonists significantly suppressed the effects of nicotine on podocyte. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 27613505-3 2016 Varenicline is a nAChR partial agonist that may improve cognitive deficits in both smokers and non-smokers with schizophrenia; however, the mechanism by which varenicline alters cognition in schizophrenia remains unclear. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. glutathione thiyl radical 91-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-48 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. glutathione thiyl radical 91-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. glutathione thiyl radical 91-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. glutathione thiyl radical 91-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. beta-Cyclodextrins 129-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-48 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. beta-Cyclodextrins 129-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. beta-Cyclodextrins 129-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. beta-Cyclodextrins 129-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 263-287 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-48 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 263-287 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 263-287 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 263-287 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 289-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-48 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 289-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 289-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. Superoxides 289-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. OOH 308-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-48 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. OOH 308-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. OOH 308-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27941944-5 2016 We present EPR spin-trapping proof that: (i) EBN is an efficient probe for the analysis of glutathione thiyl radical (GS ); (ii) beta-cyclodextrins increase the kinetic stability of the spin-adduct EBN/ SG; and (iii) in aqueous solutions, EBN does not react with superoxide anion radical (O2- ) to form EBN/ OOH to any significant extent. OOH 308-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-201 27846263-5 2016 Exposing STC-1 cells to nicotine acutely (24h) or chronically (4 days) induced a differential increase in the expression of nAChR subunit mRNA and protein in a dose- and time-dependent fashion. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 27846263-7 2016 Exposing STC-1 cells to nicotine increased intracellular Ca2+ in a dose-dependent manner that was inhibited in the presence of mecamylamine or dihydro-beta-erythroidine, a alpha4beta2 nAChR antagonist. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 27846263-7 2016 Exposing STC-1 cells to nicotine increased intracellular Ca2+ in a dose-dependent manner that was inhibited in the presence of mecamylamine or dihydro-beta-erythroidine, a alpha4beta2 nAChR antagonist. Mecamylamine 127-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 27846263-7 2016 Exposing STC-1 cells to nicotine increased intracellular Ca2+ in a dose-dependent manner that was inhibited in the presence of mecamylamine or dihydro-beta-erythroidine, a alpha4beta2 nAChR antagonist. Dihydro-beta-Erythroidine 143-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 27846263-13 2016 In STC-1 cells nAChR expression is modulated by exposure to nicotine in a dose- and time-dependent manner. Nicotine 60-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 27190210-3 2016 nAChR agonists elicit a transient ion flux response that is further sustained by the release of calcium from intracellular sources. Calcium 96-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 27545666-1 2016 The neuromodulator acetylcholine (ACh) is considered to have a crucial effect on sensory inputs in the process of learning and memory, and ACh activates muscarinic (mAChR) and nicotinic (nAChR) acetylcholine receptors. Acetylcholine 19-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 27545666-1 2016 The neuromodulator acetylcholine (ACh) is considered to have a crucial effect on sensory inputs in the process of learning and memory, and ACh activates muscarinic (mAChR) and nicotinic (nAChR) acetylcholine receptors. Acetylcholine 34-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 27545666-1 2016 The neuromodulator acetylcholine (ACh) is considered to have a crucial effect on sensory inputs in the process of learning and memory, and ACh activates muscarinic (mAChR) and nicotinic (nAChR) acetylcholine receptors. Acetylcholine 139-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 27545666-4 2016 However, the responsibility of mAChR and nAChR on pyramidal neuron and interneuron on STDP induction is still unclear. stdp 86-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 27128144-4 2016 In turn, acetylcholine interacts with members of the nicotinic acetylcholine receptor (nAChR) family, particularly with the alpha7 nicotinic acetylcholine receptor (alpha7nAChR), which is expressed by macrophages and other cytokine-producing cells. Acetylcholine 9-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-85 27128144-4 2016 In turn, acetylcholine interacts with members of the nicotinic acetylcholine receptor (nAChR) family, particularly with the alpha7 nicotinic acetylcholine receptor (alpha7nAChR), which is expressed by macrophages and other cytokine-producing cells. Acetylcholine 9-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 27128144-4 2016 In turn, acetylcholine interacts with members of the nicotinic acetylcholine receptor (nAChR) family, particularly with the alpha7 nicotinic acetylcholine receptor (alpha7nAChR), which is expressed by macrophages and other cytokine-producing cells. Acetylcholine 9-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 27424921-8 2016 We also found that nicotine induced phosphatidylinositol 3-kinase (PI3K) signal activation, and a specific inhibitor of the nicotine acetylcholine receptor (nAChR) as well as knockdown of nAChR prevented nicotine-mediated Akt phosphorylation and aPKC activation. Nicotine 19-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-155 27424921-8 2016 We also found that nicotine induced phosphatidylinositol 3-kinase (PI3K) signal activation, and a specific inhibitor of the nicotine acetylcholine receptor (nAChR) as well as knockdown of nAChR prevented nicotine-mediated Akt phosphorylation and aPKC activation. Nicotine 19-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 27424921-8 2016 We also found that nicotine induced phosphatidylinositol 3-kinase (PI3K) signal activation, and a specific inhibitor of the nicotine acetylcholine receptor (nAChR) as well as knockdown of nAChR prevented nicotine-mediated Akt phosphorylation and aPKC activation. Nicotine 19-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 27424921-8 2016 We also found that nicotine induced phosphatidylinositol 3-kinase (PI3K) signal activation, and a specific inhibitor of the nicotine acetylcholine receptor (nAChR) as well as knockdown of nAChR prevented nicotine-mediated Akt phosphorylation and aPKC activation. Nicotine 124-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 27424921-11 2016 CONCLUSIONS AND GENERAL SIGNIFICANCE: Nicotine induces aberrant activation of aPKC via nAChR/PI3K signaling in PC cells, resulting in enhancement of cellular proliferation, migration and invasion. Nicotine 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 26790437-7 2016 Our study found that A7-nAChR knockdown (A7-nAChR-KD) AGS cells were more sensitive to ixabepilone administration than scrambled control AGS cells. ixabepilone 87-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 27559543-4 2016 We observed significant effects of nicotine exposure on the beta2*-nAChR-associated proteome in human and mouse cortex, particularly in the abundance of the nAChR subunits themselves, as well as putative interacting proteins that make up core components of neuronal excitability (Na/K ATPase subunits), presynaptic neurotransmitter release (syntaxins, SNAP25, synaptotagmin), and a member of a known nAChR protein chaperone family (14-3-3zeta). Nicotine 35-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 27559543-4 2016 We observed significant effects of nicotine exposure on the beta2*-nAChR-associated proteome in human and mouse cortex, particularly in the abundance of the nAChR subunits themselves, as well as putative interacting proteins that make up core components of neuronal excitability (Na/K ATPase subunits), presynaptic neurotransmitter release (syntaxins, SNAP25, synaptotagmin), and a member of a known nAChR protein chaperone family (14-3-3zeta). Nicotine 35-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 27284006-7 2016 Exposure of cytokine-stimulated NK cells to PNU-282987, a specific alpha7 nAChR agonist, increases intracellular calcium concentration ([Ca(2+)]i) mainly released from intracellular stores, indicating that alpha7 nAChR is functional. N-neopentyl-N-nitrosourea 44-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 27284006-7 2016 Exposure of cytokine-stimulated NK cells to PNU-282987, a specific alpha7 nAChR agonist, increases intracellular calcium concentration ([Ca(2+)]i) mainly released from intracellular stores, indicating that alpha7 nAChR is functional. N-neopentyl-N-nitrosourea 44-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 27284006-7 2016 Exposure of cytokine-stimulated NK cells to PNU-282987, a specific alpha7 nAChR agonist, increases intracellular calcium concentration ([Ca(2+)]i) mainly released from intracellular stores, indicating that alpha7 nAChR is functional. Calcium 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 27284006-7 2016 Exposure of cytokine-stimulated NK cells to PNU-282987, a specific alpha7 nAChR agonist, increases intracellular calcium concentration ([Ca(2+)]i) mainly released from intracellular stores, indicating that alpha7 nAChR is functional. Calcium 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 26790437-0 2016 Silencing A7-nAChR levels increases the sensitivity of gastric cancer cells to ixabepilone treatment. ixabepilone 79-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 26790437-3 2016 Alpha-7 nicotine acetylcholine receptor (A7-nAChR) is the key molecule that mediates gastric cancer progression, metastasis, and therapy responses; however, the role of A7-nAChR in the therapeutic efficacy of ixabepilone remains unclear. ixabepilone 209-220 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 26790437-3 2016 Alpha-7 nicotine acetylcholine receptor (A7-nAChR) is the key molecule that mediates gastric cancer progression, metastasis, and therapy responses; however, the role of A7-nAChR in the therapeutic efficacy of ixabepilone remains unclear. ixabepilone 209-220 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 27493220-1 2016 In this study we report the X-ray crystal structure of the extracellular domain (ECD) of the human neuronal alpha2 nicotinic acetylcholine receptor (nAChR) subunit in complex with the agonist epibatidine at 3.2 A. Interestingly, alpha2 was crystallized as a pentamer, revealing the intersubunit interactions in a wild type neuronal nAChR ECD and the full ligand binding pocket conferred by two adjacent alpha subunits. epibatidine 192-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 27493220-1 2016 In this study we report the X-ray crystal structure of the extracellular domain (ECD) of the human neuronal alpha2 nicotinic acetylcholine receptor (nAChR) subunit in complex with the agonist epibatidine at 3.2 A. Interestingly, alpha2 was crystallized as a pentamer, revealing the intersubunit interactions in a wild type neuronal nAChR ECD and the full ligand binding pocket conferred by two adjacent alpha subunits. epibatidine 192-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 332-337 27774124-2 2016 The binding studies revealed that the stereochemistry at the C3 position of the quinuclidine scaffold plays an important role in the nAChR subtype selectivity. Quinuclidines 80-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 26790437-7 2016 Our study found that A7-nAChR knockdown (A7-nAChR-KD) AGS cells were more sensitive to ixabepilone administration than scrambled control AGS cells. ixabepilone 87-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 26790437-8 2016 We found that A7-nAChR knockdown enhanced ixabepilone-induced cell death as evidenced by the increased number of annexin V-positive (apoptotic) cells. ixabepilone 42-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 26790437-9 2016 After scrambled control and A7-nAChR-KD cells were treated with ixabepilone, we found that pAKT and AKT levels were significantly reduced in both groups of cells. ixabepilone 64-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 26790437-11 2016 Bad and Bax levels did not change between the treatment group and vehicle group in both A7-nAChR-KD and scrambled control cells, whereas cleaved PARP levels dramatically increased in ixabepilone-treated A7-nAChR-KD cells. ixabepilone 183-194 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 26790437-11 2016 Bad and Bax levels did not change between the treatment group and vehicle group in both A7-nAChR-KD and scrambled control cells, whereas cleaved PARP levels dramatically increased in ixabepilone-treated A7-nAChR-KD cells. ixabepilone 183-194 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 26790437-12 2016 Our results demonstrated that knockdown of A7-nAChR enhanced the sensitivity of gastric cancer cells to ixabepilone administration. ixabepilone 104-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 26790437-13 2016 Thus, the A7-nAChR expression level in patients with gastric cancer may be a good indicator of ixabepilone sensitivity. ixabepilone 95-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 27035276-2 2016 We report the synthesis and biological characterization of novel derivatives of 3-[(1-methyl-2(S)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine (4a-f and 5) as potent and highly selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) full or partial agonists. 3-[(1-methyl-2(s)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine 80-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-230 27349288-5 2016 In this study, we demonstrate that phosphocholine inhibits ion-channel function of ATP receptor P2X7 in monocytic cells via nAChR containing alpha9 and alpha10 subunits. Phosphorylcholine 35-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 27349288-8 2016 We conclude that phophocholine activates immuno-modulatory nAChR expressed by monocytes but does not stimulate canonical ionotropic receptor functions. phophocholine 17-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 27035276-2 2016 We report the synthesis and biological characterization of novel derivatives of 3-[(1-methyl-2(S)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine (4a-f and 5) as potent and highly selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) full or partial agonists. 3-[(1-methyl-2(s)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine 80-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 232-237 27035276-0 2016 Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective alpha4beta2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Cyclopropanes 43-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-114 27035276-2 2016 We report the synthesis and biological characterization of novel derivatives of 3-[(1-methyl-2(S)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine (4a-f and 5) as potent and highly selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) full or partial agonists. 4a-f 143-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-230 27035276-2 2016 We report the synthesis and biological characterization of novel derivatives of 3-[(1-methyl-2(S)-pyrrolidinyl)methoxy]-5-cyclopropylpyridine (4a-f and 5) as potent and highly selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) full or partial agonists. 4a-f 143-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 232-237 26061781-7 2016 Rather, we found that nAChR activation tonically enhanced evoked and spontaneous presynaptic release of GABA in the embryonic spinal cord. gamma-Aminobutyric Acid 104-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 27304486-10 2016 E. coli expressed AChBP bound nAChR agonists and antagonists with affinities matching those previously reported. achbp 18-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 27059649-9 2016 We propose that nicotinic acetylcholine receptor activation induces an increase in intracellular calcium (Ca(2+) ) concentration. Calcium 97-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-48 26952864-1 2016 Using Icelandic whole-genome sequence data and an imputation approach we searched for rare sequence variants in CHRNA4 and tested them for association with nicotine dependence. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-118 26952864-2 2016 We show that carriers of a rare missense variant (allele frequency=0.24%) within CHRNA4, encoding an R336C substitution, have greater risk of nicotine addiction than non-carriers as assessed by the Fagerstrom Test for Nicotine Dependence (P=1.2 x 10(-4)). Nicotine 142-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-87 26952864-2 2016 We show that carriers of a rare missense variant (allele frequency=0.24%) within CHRNA4, encoding an R336C substitution, have greater risk of nicotine addiction than non-carriers as assessed by the Fagerstrom Test for Nicotine Dependence (P=1.2 x 10(-4)). Nicotine 218-226 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-87 27028298-0 2016 Neuronal Nicotinic Acetylcholine Receptor Modulators Reduce Sugar Intake. Sugars 60-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-41 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Varenicline 15-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-76 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Varenicline 15-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Dopamine 116-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Sucrose 194-201 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-76 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Sucrose 194-201 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 27028298-4 2016 Similar results were observed with other nAChR drugs, namely mecamylamine and cytisine. Mecamylamine 61-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 27028298-4 2016 Similar results were observed with other nAChR drugs, namely mecamylamine and cytisine. cytisine 78-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 27028298-6 2016 Taken together, our results suggest that nAChR drugs such as varenicline may represent a novel treatment strategy for reducing sugar consumption. Varenicline 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 27028298-6 2016 Taken together, our results suggest that nAChR drugs such as varenicline may represent a novel treatment strategy for reducing sugar consumption. Sugars 127-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 26994846-0 2016 Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists. indolizine 39-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 26994846-2 2016 Herein, we report the synthesis and agonistic activities of a series of indolizine derivatives targeting to alpha7 nAChR. indolizine 72-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 26418512-4 2016 Augmented IL-8 secretion by Ca9-22 cells was blocked by the NF-kappaB inhibitor L-1-4"-tosylamino-phenylethyl-chloromethyl ketone (TPCK) and the nicotinic acetylcholine receptor (nAChR)-specific inhibitor alpha-bungarotoxin (alphaBtx). Tosylphenylalanyl Chloromethyl Ketone 131-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-177 26418512-4 2016 Augmented IL-8 secretion by Ca9-22 cells was blocked by the NF-kappaB inhibitor L-1-4"-tosylamino-phenylethyl-chloromethyl ketone (TPCK) and the nicotinic acetylcholine receptor (nAChR)-specific inhibitor alpha-bungarotoxin (alphaBtx). Tosylphenylalanyl Chloromethyl Ketone 131-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 26418512-10 2016 The results from this study indicate that the binding of nicotine to nAChR induces Ca(2+) influx, which results in the activation and phosphorylation of CaMK II and NF-kappaB p65, respectively. Nicotine 57-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 26764897-4 2016 Using a combination of conventional mutagenesis, unnatural amino acid incorporation, immunohistochemistry and MD simulations, we demonstrate the crucial contributions of these two Trp residues to receptor expression and function in two prototypical Cys-loop receptors, the anion-selective GlyR alpha1 and the cation-selective nAChR alpha7. Tryptophan 180-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 326-331 26764897-4 2016 Using a combination of conventional mutagenesis, unnatural amino acid incorporation, immunohistochemistry and MD simulations, we demonstrate the crucial contributions of these two Trp residues to receptor expression and function in two prototypical Cys-loop receptors, the anion-selective GlyR alpha1 and the cation-selective nAChR alpha7. Cysteine 249-252 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 326-331 26861354-4 2016 The objective was to evaluate whether propofol or AZD3043 interact with the alpha1beta1deltaepsilon, alpha3beta2, or alpha7 nAChR subtypes that can be found in the neuromuscular junction and if there are any differences in affinity for those subtypes between propofol and AZD3043. Propofol 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 26803692-0 2016 nAChR dysfunction as a common substrate for schizophrenia and comorbid nicotine addiction: Current trends and perspectives. Nicotine 71-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 26774337-9 2016 These nicotine effects were blocked by treatment with mecamylamine, a nonselective nAChR antagonist. Nicotine 6-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 26774337-9 2016 These nicotine effects were blocked by treatment with mecamylamine, a nonselective nAChR antagonist. Mecamylamine 54-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 26774337-10 2016 These data suggest that nicotine degrades mitofusin in NT2/D1 cells and thus induces mitochondrial dysfunction and cell growth inhibition in a nAChR-dependent manner. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 26925840-0 2016 From crystal structure of alpha-conotoxin GIC in complex with Ac-AChBP to molecular determinants of its high selectivity for alpha3beta2 nAChR. ac-achbp 62-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 26861354-4 2016 The objective was to evaluate whether propofol or AZD3043 interact with the alpha1beta1deltaepsilon, alpha3beta2, or alpha7 nAChR subtypes that can be found in the neuromuscular junction and if there are any differences in affinity for those subtypes between propofol and AZD3043. AZD-3043 50-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 26861354-7 2016 AZD3043 was a more potent inhibitor at the adult muscle nAChR subtype compared to propofol. AZD-3043 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 26861354-8 2016 Propofol and AZD3043 inhibit nAChR subtypes that can be found in the adult NMJ in concentrations higher than needed for general anaesthesia. Propofol 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 26861354-8 2016 Propofol and AZD3043 inhibit nAChR subtypes that can be found in the adult NMJ in concentrations higher than needed for general anaesthesia. AZD-3043 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Dimethylphenylpiperazinium Iodide 77-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-146 26608528-2 2016 Delineation of nAChR subtypes and their responses to nicotine stimulation in bronchial epithelium may provide information for therapeutic targeting in smoking-related inflammation in the airway. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 26608528-4 2016 Seven human bronchial epithelial cell lines (HBECs) were exposed to nicotine in vitro for their response in nAChR subunit gene expression to nicotine exposure and removal. Nicotine 68-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 26608528-4 2016 Seven human bronchial epithelial cell lines (HBECs) were exposed to nicotine in vitro for their response in nAChR subunit gene expression to nicotine exposure and removal. Nicotine 141-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 26608528-6 2016 Nicotine stimulation in HBECs resulted in transient increase in the levels of nAChR alpha5 and alpha6 but more sustained increase in nAChR alpha7 expression. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 26608528-6 2016 Nicotine stimulation in HBECs resulted in transient increase in the levels of nAChR alpha5 and alpha6 but more sustained increase in nAChR alpha7 expression. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 26608528-8 2016 Nicotine exposure in HBECs resulted in both short and longer term responses in nAChR subunit gene expression. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 26707847-7 2016 Two-electrode voltage clamping of the human alpha7 nAChR expressed in Xenopus oocytes revealed that it was possible to tune the behavior of compounds to show enhanced desensitization without corresponding partial agonist activity such that trifluoromethyl and carboxamide aryl substituents showed 33 to 46-fold larger PAM-dependent net-charge responses, indicating selective partitioning of the ligand receptor complexes into the desensitized state. carboxamide 260-271 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Dimethylphenylpiperazinium Iodide 77-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Dimethylphenylpiperazinium Iodide 105-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-146 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Dimethylphenylpiperazinium Iodide 105-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Atracurium 186-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-146 26575950-7 2016 A second NNMB, Vecuronium, also induced GSC astrocytic differentiation while Dimethylphenylpiperazinium (DMPP), a nicotinic acetylcholine receptor (nAChR) agonist, significantly blocked Atracurium Besylate pro-differentiation activity. Atracurium 186-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 26818858-4 2016 SEN12333 represents a novel chemotype for the development of alpha7 nAChR agonists, and exploration of this scaffold has produced structurally diverse ligands with promising pharmacological properties. 5-morpholin-4-ylpentanoic acid (4-pyridin-3-ylphenyl)amide 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 26818867-2 2016 The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Acetylcholine 48-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-140 26818867-2 2016 The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Acetylcholine 48-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 26818867-2 2016 The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Acetylcholine 63-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-140 26818867-2 2016 The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Acetylcholine 63-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 26845123-5 2016 Most of these effects are a result of nicotine binding and activation of cell-surface neuronal nicotinic acetylcholine receptors (nAChRs) and downstream intracellular signalling cascades, and many are blocked by nAChR subtype-selective antagonists. Nicotine 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 26845123-6 2016 Recent genome-wide association studies have revealed single nucleotide polymorphisms of nAChR subunits that influence nicotine dependence and lung cancer. Nicotine 118-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 26810002-7 2016 Here, we review recent insights into the rewarding effects of alcohol, as they pertain to different nAChR subtypes, associated signaling molecules, and pathways that contribute to the molecular mechanisms of alcoholism and/or comorbid brain disorders. Alcohols 62-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 26318101-2 2015 SNPs in the putative promoter region of CHRNB3, the gene that encodes the beta3 subunit of the nicotinic acetylcholine receptor (nAChR), have been repeatedly associated with nicotine behaviors. Nicotine 174-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 26440997-0 2015 Postnatal nicotine effects on the expression of nicotinic acetylcholine receptors in the developing piglet hippocampus and brainstem. Nicotine 10-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-81 26440997-3 2015 Nicotine, the major neurotoxic component of cigarette smoke, induces its actions by binding to nicotinic acetylcholine receptors (nAChR). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-128 26440997-3 2015 Nicotine, the major neurotoxic component of cigarette smoke, induces its actions by binding to nicotinic acetylcholine receptors (nAChR). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 26440997-8 2015 This is the first demonstration that non-classical nAChR subunits are affected by postnatal nicotine in the developing brain, and the implications are discussed. Nicotine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Donepezil 85-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-172 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Donepezil 85-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Mecamylamine 192-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-172 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Mecamylamine 192-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Scopolamine 266-277 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-172 26315944-6 2015 We also found that the increase in the number of oligodendrocytes observed following donepezil treatment was significantly inhibited by the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine, but not by the muscarinic acetylcholine receptor antagonist scopolamine. Scopolamine 266-277 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 26429939-2 2015 nAChRs in the medial habenula (MHb) have recently been shown to play a role in nicotine dependence, but it is not clear which nAChR subtypes or MHb neuron types are most important. Nicotine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 26429939-6 2015 The latter result was correlated with a differing ability of nicotine to induce nAChR desensitization. Nicotine 61-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 26429939-7 2015 Chronic nicotine caused functional upregulation of nAChRs selectively in MHbVI cells, but did not change nAChR function in MHbVL. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 26429939-11 2015 Together, these results suggest that acute and chronic nicotine differentially affect nAChR function and output of cells in MHb subregions. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 26438212-2 2015 The alpha3beta2 and alpha3beta4 nAChR subtypes are expressed in the central and peripheral nervous systems and play a critical role in various pathophysiological conditions ranging from nicotine addiction to the development and progression of lung cancer. Nicotine 186-194 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 26432642-3 2015 This compound increases acetylcholine-evoked responses of alpha2* and alpha4* nAChRs but is without effect on alpha3* or alpha6* nAChRs (* indicates the presence of other nAChR subunits). Acetylcholine 24-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 26432642-6 2015 Like 17beta-estradiol, the non-steroid Br-PBTC only requires one alpha4 subunit to potentiate nAChR function, and its potentiation is stronger with more alpha4 subunits. Steroids 31-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 26432642-6 2015 Like 17beta-estradiol, the non-steroid Br-PBTC only requires one alpha4 subunit to potentiate nAChR function, and its potentiation is stronger with more alpha4 subunits. Br-PBTC 39-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 26473809-5 2015 Based on in vitro binding affinity and selectivity, assessed by radioligand displacement studies at different rat and human nAChR subtypes and at the structurally related human 5-HT3 receptor, we selected the compound 7-(1,4-diazabicyclo[3.2.2]nonan-4-yl)-2-fluorodibenzo-[b,d]thiophene 5,5-dioxide (10a) for radiolabeling and further evaluation in vivo. DBT-10 218-298 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 26272810-7 2015 RESULTS: Thalamic nAChR alpha4beta2* availability was significantly reduced in slow nicotine metabolizers (P = 0.04). Nicotine 84-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 26272810-9 2015 CONCLUSION: The rate of nicotine metabolism is associated with thalamic nAChR availability. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 26272810-10 2015 Additional studies could examine whether altered nAChR availability underlies the differences in treatment response between slow and normal metabolizers of nicotine. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 26354438-5 2015 Our findings support the hypothesis that a cholesterol-sensitive nAChR might reside in specialized membrane microdomains that upon cholesterol depletion become disrupted and release the cholesterol-sensitive nAChRs to the pool of activable receptors. Cholesterol 43-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 26354438-5 2015 Our findings support the hypothesis that a cholesterol-sensitive nAChR might reside in specialized membrane microdomains that upon cholesterol depletion become disrupted and release the cholesterol-sensitive nAChRs to the pool of activable receptors. Cholesterol 131-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 26354438-5 2015 Our findings support the hypothesis that a cholesterol-sensitive nAChR might reside in specialized membrane microdomains that upon cholesterol depletion become disrupted and release the cholesterol-sensitive nAChRs to the pool of activable receptors. Cholesterol 131-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 26354438-7 2015 The current work suggests that the interplay between cholesterol and CAV-1 provides the molecular basis for modulating the function and dynamics of the cholesterol-sensitive alphaC418W nAChR. Cholesterol 53-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 26354438-7 2015 The current work suggests that the interplay between cholesterol and CAV-1 provides the molecular basis for modulating the function and dynamics of the cholesterol-sensitive alphaC418W nAChR. Cholesterol 152-163 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 26231943-2 2015 Acetylcholine binds in the receptor extracellular domain at the interface between two subunits and research has identified a large number of nAChR-selective ligands, including agonists and competitive antagonists, that bind at the same site as acetylcholine (commonly referred to as the orthosteric binding site). Acetylcholine 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 26231943-2 2015 Acetylcholine binds in the receptor extracellular domain at the interface between two subunits and research has identified a large number of nAChR-selective ligands, including agonists and competitive antagonists, that bind at the same site as acetylcholine (commonly referred to as the orthosteric binding site). Acetylcholine 244-257 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 26231943-3 2015 In addition, more recent research has identified ligands that are able to modulate nAChR function by binding to sites that are distinct from the binding site for acetylcholine, including sites located in the transmembrane domain. Acetylcholine 162-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 26283025-3 2015 In this study, using a two-electrode voltage-clamp and patch-clamp techniques and live cellular calcium imaging, we have investigated the effect of bisabolol on the function of human alpha7 subunit of nicotinic acetylcholine receptor (nAChR) in Xenopus oocytes, interneurons of rat hippocampal slices. bisabolol 148-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 26355753-1 2015 The insertion and function of the muscle-type nicotinic acetylcholine receptor (nAChR) in Au(111)-supported thiolipid self-assembled monolayers have been studied by atomic force microscopy (AFM), surface plasmon resonance (SPR), and electrochemical techniques. Gold 90-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 26355753-1 2015 The insertion and function of the muscle-type nicotinic acetylcholine receptor (nAChR) in Au(111)-supported thiolipid self-assembled monolayers have been studied by atomic force microscopy (AFM), surface plasmon resonance (SPR), and electrochemical techniques. thiolipid 108-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 26355753-4 2015 Addition of the full agonist carbamoylcholine activated and opened the nAChR ion channel, as revealed by the increase in capacitance relative to that of the nAChR-thiolipid system under basal conditions. Carbachol 29-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 26355753-4 2015 Addition of the full agonist carbamoylcholine activated and opened the nAChR ion channel, as revealed by the increase in capacitance relative to that of the nAChR-thiolipid system under basal conditions. Carbachol 29-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 26354438-2 2015 The novel nicotinic acetylcholine receptor (nAChR) mutation alphaC418W, the first lipid-exposed mutation identified in a patient that causes slow channel congenital myasthenia syndrome was shown to be cholesterol-sensitive and to accumulate in microdomains rich in the membrane raft marker protein caveolin-1. Cholesterol 201-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 10-42 26354438-2 2015 The novel nicotinic acetylcholine receptor (nAChR) mutation alphaC418W, the first lipid-exposed mutation identified in a patient that causes slow channel congenital myasthenia syndrome was shown to be cholesterol-sensitive and to accumulate in microdomains rich in the membrane raft marker protein caveolin-1. Cholesterol 201-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 26473809-9 2015 Our initial evaluation revealed that the dibenzothiophene-based PET radioligand [18F]10a ([18F]DBT-10) has high potential to provide clinically relevant information about the expression and availability of alpha7 nAChR in the brain. dibenzothiophene 41-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 26473809-9 2015 Our initial evaluation revealed that the dibenzothiophene-based PET radioligand [18F]10a ([18F]DBT-10) has high potential to provide clinically relevant information about the expression and availability of alpha7 nAChR in the brain. di-n-butyltin 95-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 26269589-3 2015 The effect of cotinine, the primary metabolite of nicotine, on nAChR trafficking and assembly has not been extensively investigated. Cotinine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 26440539-0 2015 Genome-wide meta-analysis reveals common splice site acceptor variant in CHRNA4 associated with nicotine dependence. Nicotine 96-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-79 26440539-6 2015 Using criteria for smoking behavior that encompass more than the single "cigarettes per day" item, we identified a common CHRNA4 variant with important regulatory properties that contributes to nicotine dependence and smoking-related consequences. Nicotine 194-202 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-128 26269589-3 2015 The effect of cotinine, the primary metabolite of nicotine, on nAChR trafficking and assembly has not been extensively investigated. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 26265067-3 2015 Here, we present the first large-scale analysis of the proteomic and phosphoproteomic alterations in pancreatic stellate cells following treatment with two nicotinic acetylcholine receptor (nAChR) ligands: nicotine and alpha-bungarotoxin. Nicotine 206-214 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-188 26265067-3 2015 Here, we present the first large-scale analysis of the proteomic and phosphoproteomic alterations in pancreatic stellate cells following treatment with two nicotinic acetylcholine receptor (nAChR) ligands: nicotine and alpha-bungarotoxin. Nicotine 206-214 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 26441658-9 2015 At higher concentrations of nicotine, NNK always inhibited the alpha4beta2 nAChR. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 26441658-10 2015 In contrast, NNN was a pure inhibitor of this nAChR subtype, with IC50 of approximately 1 nM in the presence of 10 muM nicotine. Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 25498233-1 2015 Recent human genetic studies have identified genetic variants in multiple nicotinic acetylcholine receptor (nAChR) subunit genes that are associated with risk for nicotine dependence and other smoking-related measures. Nicotine 163-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-106 26205096-0 2015 alpha5-nAChR modulates nicotine-induced cell migration and invasion in A549 lung cancer cells. Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 7-12 26205096-4 2015 Recently studies have indicated that alpha5-nAChR is highly associated with lung cancer risk and nicotine dependence. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 26205096-10 2015 Nicotine can induce activation of alpha5-nAChR in association with increased migration and invasion of human lung cancer A549 cell. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 26205096-11 2015 Treatment of cells with alpha5-nAChR specific siRNA blocks nicotine-stimulated activation of alpha5-nAChR and suppresses A549 cell migration and invasion. Nicotine 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 26205096-11 2015 Treatment of cells with alpha5-nAChR specific siRNA blocks nicotine-stimulated activation of alpha5-nAChR and suppresses A549 cell migration and invasion. Nicotine 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 26205096-13 2015 These findings suggest that nicotine-induced migration and invasion may occur in a mechanism through activation of alpha5-nAChR, which can contribute to metastasis or development of human lung cancer. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 26038197-7 2015 Using the nucleoside analogue EdU (5-ethynyl-2"-deoxyuridine) as a marker of cell proliferation, application of alpha7*nAChR modulators in spinal cord cultures or in vivo induced proliferation in the CC region, producing Sox-2 expressing ependymal cells. Nucleosides 10-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-124 26038197-7 2015 Using the nucleoside analogue EdU (5-ethynyl-2"-deoxyuridine) as a marker of cell proliferation, application of alpha7*nAChR modulators in spinal cord cultures or in vivo induced proliferation in the CC region, producing Sox-2 expressing ependymal cells. 5-ethynyl-2'-deoxyuridine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-124 26038197-7 2015 Using the nucleoside analogue EdU (5-ethynyl-2"-deoxyuridine) as a marker of cell proliferation, application of alpha7*nAChR modulators in spinal cord cultures or in vivo induced proliferation in the CC region, producing Sox-2 expressing ependymal cells. 5-ethynyl-2'-deoxyuridine 35-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-124 26175091-4 2015 Starting from classical homology and docking approaches, binding mode hypotheses are created for five agonists of the nAChR, covering insecticides in the main group 4 of the Insecticide Resistance Action Committee (IRAC) mode of action (MoA) classification, namely, neonicotinoids, nicotine, sulfoxaflor, and butenolides. Neonicotinoids 266-280 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 26175091-4 2015 Starting from classical homology and docking approaches, binding mode hypotheses are created for five agonists of the nAChR, covering insecticides in the main group 4 of the Insecticide Resistance Action Committee (IRAC) mode of action (MoA) classification, namely, neonicotinoids, nicotine, sulfoxaflor, and butenolides. Nicotine 282-290 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 26175091-4 2015 Starting from classical homology and docking approaches, binding mode hypotheses are created for five agonists of the nAChR, covering insecticides in the main group 4 of the Insecticide Resistance Action Committee (IRAC) mode of action (MoA) classification, namely, neonicotinoids, nicotine, sulfoxaflor, and butenolides. sulfoxaflor 292-303 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 26175091-4 2015 Starting from classical homology and docking approaches, binding mode hypotheses are created for five agonists of the nAChR, covering insecticides in the main group 4 of the Insecticide Resistance Action Committee (IRAC) mode of action (MoA) classification, namely, neonicotinoids, nicotine, sulfoxaflor, and butenolides. butenolide 309-320 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 26037057-3 2015 Following on from promising preclinical results, the aim of the present study was to evaluate for the first time in humans the novel PET radioligand (-)-[(18)F]Flubatine, formerly known as (-)-[(18)F]NCFHEB, as a tool for alpha4beta2* nAChR imaging and in vivo quantification. (-)-[(18)f]flubatine 149-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 25498233-1 2015 Recent human genetic studies have identified genetic variants in multiple nicotinic acetylcholine receptor (nAChR) subunit genes that are associated with risk for nicotine dependence and other smoking-related measures. Nicotine 163-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 25529272-0 2015 The nicotinic acetylcholine receptor and its prokaryotic homologues: Structure, conformational transitions & allosteric modulation. Adenosine Monophosphate 108-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 25963024-7 2015 Several amino acid residues, such as B/Tyr-93, B/Lys-143, B/Trp-147, B/Tyr-188, B/Tyr-195, A/Trp-55 and A/Leu-118 played a major role in the alpha7 nAChR-antagonist recognition processes, in particular, residues B/Tyr-93, B/Trp-147 and B/Tyr-188 are the most important. Tryptophan 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 25963024-7 2015 Several amino acid residues, such as B/Tyr-93, B/Lys-143, B/Trp-147, B/Tyr-188, B/Tyr-195, A/Trp-55 and A/Leu-118 played a major role in the alpha7 nAChR-antagonist recognition processes, in particular, residues B/Tyr-93, B/Trp-147 and B/Tyr-188 are the most important. Leucine 106-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 25963024-4 2015 In the context of this manuscript, our primary objective was to comprehensively analyze the recognition patterns and the critical interaction descriptors between target alpha7 nAChR and a series of the novel compounds with potentially antagonistic activity by means of virtual screening, molecular docking and molecular dynamics simulation, and meanwhile these recognition reactions were also compared with the biointeraction of alpha7 nAChR with a commercially natural antagonist - methyllycaconitine. methyllycaconitine 483-501 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 176-181 25963024-7 2015 Several amino acid residues, such as B/Tyr-93, B/Lys-143, B/Trp-147, B/Tyr-188, B/Tyr-195, A/Trp-55 and A/Leu-118 played a major role in the alpha7 nAChR-antagonist recognition processes, in particular, residues B/Tyr-93, B/Trp-147 and B/Tyr-188 are the most important. Tryptophan 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 26225816-1 2015 Some unichiral analogues of 2R,2"S-2-(1"-methyl-2"-pyrrolidinyl)-7-hydroxy-1,4-benzodioxane, a potent and selective alpha4beta2-nAChR partial agonist, were designed by opening dioxane and replacing hydroxyl carbon with nitrogen. 2r,2"s-2-(1"-methyl-2"-pyrrolidinyl)-7-hydroxy-1,4-benzodioxane 28-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 26063663-3 2015 In order to further characterize the pharmacological profiles of these phycotoxins on various nicotinic acetylcholine receptor (nAChR) subtypes and to examine whether they act on muscarinic receptors (mAChRs), functional electrophysiological studies and competition binding experiments have been performed. phycotoxins 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 26063663-3 2015 In order to further characterize the pharmacological profiles of these phycotoxins on various nicotinic acetylcholine receptor (nAChR) subtypes and to examine whether they act on muscarinic receptors (mAChRs), functional electrophysiological studies and competition binding experiments have been performed. phycotoxins 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 26225816-1 2015 Some unichiral analogues of 2R,2"S-2-(1"-methyl-2"-pyrrolidinyl)-7-hydroxy-1,4-benzodioxane, a potent and selective alpha4beta2-nAChR partial agonist, were designed by opening dioxane and replacing hydroxyl carbon with nitrogen. 1,4-dioxane 84-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 26247203-3 2015 We found that antagonizing the alpha4beta2 nAChR locally in the lateral hypothalamus with di-hydro-ss-erythroidine (DHbetaE), an alpha4 nAChR antagonist with moderate affinity, caused an increase in food intake following free access to food after a 12 hour fast, compared to saline-infused animals. di-hydro-ss-erythroidine 90-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 26138153-7 2015 Tribendimidine is a selective cholinergic nematode B-subtype nAChR agonist, producing muscle depolarization and contraction. tribendimidine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 25990637-8 2015 Serine 365 in the M3-M4 cytoplasmic loop of the alpha7 nAChR is a phosphorylation site for protein kinase A (PKA). Serine 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 26247203-3 2015 We found that antagonizing the alpha4beta2 nAChR locally in the lateral hypothalamus with di-hydro-ss-erythroidine (DHbetaE), an alpha4 nAChR antagonist with moderate affinity, caused an increase in food intake following free access to food after a 12 hour fast, compared to saline-infused animals. di-hydro-ss-erythroidine 90-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 26247203-3 2015 We found that antagonizing the alpha4beta2 nAChR locally in the lateral hypothalamus with di-hydro-ss-erythroidine (DHbetaE), an alpha4 nAChR antagonist with moderate affinity, caused an increase in food intake following free access to food after a 12 hour fast, compared to saline-infused animals. Dihydro-beta-Erythroidine 116-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 26247203-3 2015 We found that antagonizing the alpha4beta2 nAChR locally in the lateral hypothalamus with di-hydro-ss-erythroidine (DHbetaE), an alpha4 nAChR antagonist with moderate affinity, caused an increase in food intake following free access to food after a 12 hour fast, compared to saline-infused animals. Dihydro-beta-Erythroidine 116-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 26247203-3 2015 We found that antagonizing the alpha4beta2 nAChR locally in the lateral hypothalamus with di-hydro-ss-erythroidine (DHbetaE), an alpha4 nAChR antagonist with moderate affinity, caused an increase in food intake following free access to food after a 12 hour fast, compared to saline-infused animals. Sodium Chloride 275-281 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 26244344-4 2015 In the present work, using docking and molecular dynamics methodologies, we established the most probable binding sites of SB-206553, a drug originally described as a competitive antagonist of serotonin type 2B/2C metabotropic receptors (5-HT2B/2CRs) and more recently as a positive allosteric modulator of the ionotropic alpha7 nicotinic acetylcholine receptor (nAChR). SB 206553 123-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 363-368 26247203-4 2015 Immunocytochemical analysis revealed that orexin/hypocretin (HO), oxytocin, and tyrosine hydroxylase (TH)-containing neurons in the A13 and A12 of the hypothalamus expressed the nAChR alpha4 subunit in varying amounts (34%, 42%, 50%, and 51%, respectively) whereas melanin concentrating hormone (MCH) neurons did not, suggesting that DHbetaE-mediated increases in food intake may be due to a direct activation of specific hypothalamic circuits. Dihydro-beta-Erythroidine 334-341 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 26244344-5 2015 To this end, we employed the crystal structures of the 5-HT2BR and acetylcholine binding protein as templates to build homology models of the 5-HT2CR and alpha7 nAChR, respectively. Acetylcholine 67-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 25964258-2 2015 The nAChR subtype transduces the irritant effects of nicotine in tobacco smoke and, in certain brain areas, may be involved in nicotine addiction and/or withdrawal. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 26244344-7 2015 Our analysis showed that the most plausible binding sites for SB-206553 at 5-HT2Rs and alpha7 nAChR are remarkably similar, both in size and chemical nature of the amino acid residues lining these pockets, thus providing a rationale to explain its affinity towards both receptor types. Antimony 62-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 26142318-3 2015 In this compound series, the nAChR ligand N,N-dimethyl-2-(pyridin-3-yloxy)ethan-1-amine 9 served as one pharmacological entity and it was initially kept constant as one part of the "twin" compound. n,n-dimethyl-2-(pyridin-3-yloxy)ethan-1-amine 42-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Acetylcysteine 0-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Hexamethonium 37-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Hexamethonium 37-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Reactive Oxygen Species 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Reactive Oxygen Species 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. nachrs 244-250 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. nachrs 244-250 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Reactive Oxygen Species 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 25503516-5 2015 N-acetyl-cysteine (ROS scavenger) or hexamethonium [nicotinic acetylcholine receptor (nAChR) antagonist] attenuated the CSE-induced increase in intracellular ROS, activation of AMPK and NF-kappaB, as well as IL-8 induction, which suggests that nAChRs and ROS are important. Reactive Oxygen Species 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 25964258-2 2015 The nAChR subtype transduces the irritant effects of nicotine in tobacco smoke and, in certain brain areas, may be involved in nicotine addiction and/or withdrawal. Nicotine 127-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 25964258-5 2015 Menthol markedly decreased nAChR activity as assessed by Ca(2+) imaging, (86)Rb(+) efflux, and voltage-clamp measurements. Menthol 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 25964258-5 2015 Menthol markedly decreased nAChR activity as assessed by Ca(2+) imaging, (86)Rb(+) efflux, and voltage-clamp measurements. Rubidium 77-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 25885699-5 2015 RESULTS: We demonstrated that the growth-promoting effect of nicotine mediated by activation of alpha7 cm-nAChR synergizes mainly with that of epidermal growth factor (EGF), alpha3 - vascular endothelial growth factor (VEGF), alpha4 - insulin-like growth factor I (IGF-I) and VEGF, whereas alpha9 with EGF, IGF-I and VEGF. Nicotine 61-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 25647695-0 2015 Modulation of nicotine effects on selective attention by DRD2 and CHRNA4 gene polymorphisms. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-72 25647695-4 2015 OBJECTIVE: We aimed to investigate whether CHRNA4 and DRD2 genotypes alter the effects of nicotine on distractor interference. Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-49 26080439-6 2015 We also show that M2/M4 mAChRs depress the nAChR-dependent mechanism of DA release in the striatum. Dopamine 72-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 26004441-5 2015 Uniquely, however, the bulky bridged EF-ketal ring specific to the pinnatoxins extends radially from the interfacial-binding pocket to interact with the sequence-variable loop F and govern nAChR subtype selectivity and central neurotoxicity. pinnatoxins 67-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 26008231-4 2015 Among the low-molecular weight compounds are alkaloids pibocin, varacin and makaluvamines C and G. 6-Bromohypaphorine from the mollusk Hermissenda crassicornis does not bind to Torpedo nAChR but behaves as an agonist on human alpha7 nAChR. L-6-bromohypaporphine 99-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 25670150-0 2015 Nicotine induces resistance to erlotinib via cross-talk between alpha 1 nAChR and EGFR in the non-small cell lung cancer xenograft model. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 25670150-0 2015 Nicotine induces resistance to erlotinib via cross-talk between alpha 1 nAChR and EGFR in the non-small cell lung cancer xenograft model. Erlotinib Hydrochloride 31-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 25670150-1 2015 OBJECTIVES: Given our previously published study, alpha 1 nicotinic acetylcholine receptor (nAChR) plays an essential role in nicotine-induced cell signaling and nicotine-induced resistance to epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) in non-small cell lung cancer (NSCLC) PC9 cells. Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 25670150-1 2015 OBJECTIVES: Given our previously published study, alpha 1 nicotinic acetylcholine receptor (nAChR) plays an essential role in nicotine-induced cell signaling and nicotine-induced resistance to epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) in non-small cell lung cancer (NSCLC) PC9 cells. Nicotine 162-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 25670150-2 2015 The aim of this study was to investigate the potential mechanism between nAChR and EGFR for nicotine-induced resistance to EGFR-TKI erlotinib in the NSCLC xenograft model. Nicotine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 25670150-2 2015 The aim of this study was to investigate the potential mechanism between nAChR and EGFR for nicotine-induced resistance to EGFR-TKI erlotinib in the NSCLC xenograft model. Erlotinib Hydrochloride 132-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 25536046-6 2015 In addition, cell-attached, single-channel recording shows that both acetylcholine-activated alpha4beta2chi- and alpha4beta4chi-nAChR have a significantly lower mean open probability, shorter mean open-time, and a longer mean closed-time than their fully wild-type counterparts while not having different conductance amplitudes. Acetylcholine 69-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 26096691-1 2015 Performance improvements in cognitive tasks requiring executive functions are evident with nicotinic acetylcholine receptor (nAChR) agonists, and activation of the underlying neural circuitry supporting these cognitive effects is thought to involve dopamine neurotransmission. Dopamine 249-257 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 25870334-5 2015 Upon irradiation at 312 nm, [(3)H]dFBr photoincorporated into amino acids within the Torpedo nAChR ion channel with the efficiency of photoincorporation enhanced in the presence of agonist and the agonist-enhanced photolabeling inhibitable by phencyclidine. [(3)h]dfbr 28-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 25870334-5 2015 Upon irradiation at 312 nm, [(3)H]dFBr photoincorporated into amino acids within the Torpedo nAChR ion channel with the efficiency of photoincorporation enhanced in the presence of agonist and the agonist-enhanced photolabeling inhibitable by phencyclidine. Phencyclidine 243-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 25870334-6 2015 In the presence of agonist, [(3)H]dFBr also photolabeled amino acids in the nAChR extracellular domain within binding pockets identified previously for the nonselective nAChR PAMs galantamine and physostigmine at the canonical alpha-gamma interface containing the transmitter binding sites and at the noncanonical delta-beta subunit interface. Galantamine 180-191 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 25870334-6 2015 In the presence of agonist, [(3)H]dFBr also photolabeled amino acids in the nAChR extracellular domain within binding pockets identified previously for the nonselective nAChR PAMs galantamine and physostigmine at the canonical alpha-gamma interface containing the transmitter binding sites and at the noncanonical delta-beta subunit interface. Physostigmine 196-209 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 26273406-3 2015 In the present study, we investigated the mechanisms by which PGE2 increases non-small cell lung cancer (NSCLC) proliferation via alpha7 nAChR induction. Dinoprostone 62-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 26273406-4 2015 METHODS: The effects of PGE2 on alpha7 nAChR expression, promoter activity, and cell signaling pathways were detected by Western blot analysis, real time reverse transcriptase polymerase chain reaction, and transient transfection assay. Dinoprostone 24-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 26273406-6 2015 RESULTS: We found that PGE2 induced alpha7 nAChR expression and its promoter activity in NSCLC cells. Dinoprostone 23-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 26273406-7 2015 The stimulatory role of PGE2 on cell proliferation was attenuated by alpha7 nAChR small interfering ribonucleic acids (siRNA) or acetylcholinesterase. Dinoprostone 24-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 26273406-8 2015 PGE2-induced alpha7 nAChR expression was blocked by an antagonist of the PGE2 receptor subtype EP4 and by EP4 siRNA. Dinoprostone 0-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 26273406-9 2015 Furthermore, PGE2 enhanced alpha7 nAChR expression via activation of c-Jun N-terminal kinase (JNK), phosphatidylinositol 3-kinase (PI3-K), and protein kinase A (PKA) pathways followed by increased c-Jun expression, a critical transcription factor. Dinoprostone 13-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 26273406-10 2015 Blockade of c-Jun diminished the effects of PGE2 on alpha7 nAChR promoter activity and protein expression, and cell growth. Dinoprostone 44-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 26273406-11 2015 CONCLUSION: Our results demonstrate that PGE2 promotes NSCLC cell growth through increased alpha7 nAChR expression. Dinoprostone 41-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 26079805-6 2015 On behavioural level, the strongest benefits of nicotine in invalid trials were observed in participants carrying both, the DRD2 T- and CHRNA4 C+ variant. Nicotine 48-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-142 26079805-7 2015 Neurally, we were able to demonstrate that different DRD2/CHRNA4 groups can be decoded from the pattern of brain activity in invalid trials under nicotine. Nicotine 146-154 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-64 26079805-9 2015 Our findings suggest that polymorphisms in the CHRNA4 and DRD2 genes are a relevant source of individual variability in pharmacological studies with nicotine. Nicotine 149-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-53 25934188-5 2015 RESULTS: Using voltage clamp experiments we were able to show that the CHRNA4 haplotype alleles differ with respect to their functional effects on receptor sensitivity including reversal of receptor sensitivity between low and high acetylcholine concentrations. Acetylcholine 232-245 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-77 25699474-2 2015 Given that ACh levels are affected in pre-eclampsia, it has been suggested that compensatory changes in nAChR expression may ensue. Acetylcholine 11-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 25699474-8 2015 Given the absence of cigarette smoking, the changes in expression are hypothesised to be due to the hypoxic environment resulting from the pathophysiology of pre-eclampsia, which subsequently affects endogenous ACh levels, yielding compensatory increases in alpha2, alpha7, alpha9, beta1, beta2, and delta nAChR subunits. Acetylcholine 211-214 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 306-311 25388292-9 2015 CONCLUSIONS: Although replicating nicotine-induced upregulation of nAChRs in human smokers and demonstrating NVHL validity in terms of schizophrenia-associated nAChR density patterns, these findings do not support hypotheses explaining increased nicotine use in schizophrenia as reflecting illness-specific effects of nicotine to therapeutically alter cognition or nAChR densities. Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 25770198-4 2015 Upon finding a missense mutation in CHRNA2, we measured whole-cell currents in human embryonic kidney cells in both wild-type and mutant alpha2beta4 and alpha2beta2 nAChR subtypes stimulated with nicotine. Nicotine 196-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 25670150-8 2015 injection of nicotine through activating alpha 1 nAChR and EGFR pathways. Nicotine 13-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 25670150-9 2015 CONCLUSIONS: These results suggest that nicotine contributes to the progression and erlotinib-resistance of the NSCLC xenograft model via the cooperation between nAChR and EGFR. Nicotine 40-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 25670150-9 2015 CONCLUSIONS: These results suggest that nicotine contributes to the progression and erlotinib-resistance of the NSCLC xenograft model via the cooperation between nAChR and EGFR. Erlotinib Hydrochloride 84-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 25716861-4 2015 We sought to identify the nAChR subunits that underlie the rapid excitation of CD afferents and whether they differ from alpha9alpha10 nAChRs on type II hair cells that drive efferent-mediated inhibition in adjacent bouton afferents. Cadmium 79-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 25775422-2 2015 For the nudibranch mollusk Hermissenda crassicornis no endogenous compounds were known, and here we describe the isolation of 6-BHP from this mollusk and its effects on different nicotinic acetylcholine receptors (nAChR). L-6-bromohypaporphine 126-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 25775422-4 2015 However, in radioligand analysis, 6-BHP competed with radioiodinated alpha-bungarotoxin for binding to human alpha7 nAChR expressed in GH4C1 cells (IC50 23 +- 1 muM), but showed no competition on muscle-type nAChR from Torpedo californica. L-6-bromohypaporphine 34-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-121 25775422-5 2015 In Ca2+-imaging experiments on the human alpha7 nAChR expressed in the Neuro2a cells, 6-BHP in the presence of PNU120596 behaved as an agonist (EC50 ~80 muM). L-6-bromohypaporphine 86-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25775422-6 2015 To the best of our knowledge, 6-BHP is the first low-molecular weight compound from marine source which is an agonist of the nAChR subtype. L-6-bromohypaporphine 30-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 25601486-11 2015 In contrast, alpha7 nAChR was a repressor of proliferation in tumour cells isolated from well differentiated NSCLC but mediated the pro-proliferative activity of nicotine in cells isolated from poorly differentiated NSCLC. Nicotine 162-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 25180076-1 2015 INTRODUCTION: Genome-wide association studies linking the alpha3, beta4, and alpha5 nicotinic acetylcholine receptor (nAChR) subunits to nicotine dependence suggest that alpha3beta4* nAChR may be targets for smoking cessation pharmacotherapies. Nicotine 137-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 25180076-1 2015 INTRODUCTION: Genome-wide association studies linking the alpha3, beta4, and alpha5 nicotinic acetylcholine receptor (nAChR) subunits to nicotine dependence suggest that alpha3beta4* nAChR may be targets for smoking cessation pharmacotherapies. Nicotine 137-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 25180076-2 2015 We previously reported that AT-1001, a selective alpha3beta4* nAChR ligand binds with high affinity to rat alpha3beta4 and human alpha3beta4alpha5 nAChR, antagonizes epibatidine-induced activation of rat alpha3beta4 nAChR in HEK cells and potently inhibits nicotine self-administration in rats. larazotide acetate 28-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 25180076-2 2015 We previously reported that AT-1001, a selective alpha3beta4* nAChR ligand binds with high affinity to rat alpha3beta4 and human alpha3beta4alpha5 nAChR, antagonizes epibatidine-induced activation of rat alpha3beta4 nAChR in HEK cells and potently inhibits nicotine self-administration in rats. epibatidine 166-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 25180076-4 2015 RESULTS: Concentration-response curves show that AT-1001 is a partial agonist at human alpha3beta4 nAChR, evoking up to 35% of the maximal acetylcholine (ACh) response (50% effective concentration [EC50] = 0.37 muM). Astatine 49-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 25180076-6 2015 Pre- and co-application of various concentrations of AT-1001 with 50 muM ACh revealed a complex pattern of activation-inhibition by AT-1001 at alpha3beta4 nAChR, which was best fitted by a 2-site equation. Astatine 53-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 25180076-6 2015 Pre- and co-application of various concentrations of AT-1001 with 50 muM ACh revealed a complex pattern of activation-inhibition by AT-1001 at alpha3beta4 nAChR, which was best fitted by a 2-site equation. Acetylcholine 73-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 25180076-6 2015 Pre- and co-application of various concentrations of AT-1001 with 50 muM ACh revealed a complex pattern of activation-inhibition by AT-1001 at alpha3beta4 nAChR, which was best fitted by a 2-site equation. Astatine 132-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 25180076-7 2015 At alpha4beta2 nAChR, co-exposure of AT-1001 with ACh only showed inhibition of ACh current with a shallower curve. Acetylcholine 50-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 25180076-8 2015 CONCLUSIONS: AT-1001 is a partial agonist at the human alpha3beta4 nAChR and causes desensitization at concentrations at which it evokes an inward current, resulting in an overall functional antagonism of alpha3beta4 nAChR. Astatine 13-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 25180076-8 2015 CONCLUSIONS: AT-1001 is a partial agonist at the human alpha3beta4 nAChR and causes desensitization at concentrations at which it evokes an inward current, resulting in an overall functional antagonism of alpha3beta4 nAChR. Astatine 13-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 217-222 25774163-0 2015 CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy. Varenicline 57-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-6 25774163-10 2015 CONCLUSION: The CHRNA4 rs1044396 is associated with smoking cessation in individuals on varenicline therapy. Varenicline 88-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-22 25716861-6 2015 The alpha9alpha10 nAChR antagonists, alpha-bungarotoxin and alpha-conotoxin RgIA, blocked efferent-mediated inhibition in bouton afferents while leaving efferent-mediated excitation in CD units largely intact. Cadmium 185-187 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Acetylcholine 21-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-155 25618596-1 2015 In the present study, nitromethylene neonicotinoid derivatives possessing substituents that contain a sulfur atom, oxygen atom or aromatic ring at position 5 on the imidazolidine ring were synthesized to evaluate their affinity for the nicotinic acetylcholine receptor (nAChR) and their insecticidal activity against adult female houseflies. nitromethylene neonicotinoid 22-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 236-268 25618596-1 2015 In the present study, nitromethylene neonicotinoid derivatives possessing substituents that contain a sulfur atom, oxygen atom or aromatic ring at position 5 on the imidazolidine ring were synthesized to evaluate their affinity for the nicotinic acetylcholine receptor (nAChR) and their insecticidal activity against adult female houseflies. nitromethylene neonicotinoid 22-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 270-275 25618596-1 2015 In the present study, nitromethylene neonicotinoid derivatives possessing substituents that contain a sulfur atom, oxygen atom or aromatic ring at position 5 on the imidazolidine ring were synthesized to evaluate their affinity for the nicotinic acetylcholine receptor (nAChR) and their insecticidal activity against adult female houseflies. Imidazolidines 165-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 236-268 25475645-5 2015 The allosteric sites found at the extracellular domain (EXD) of halpha3beta4 and halpha4beta2 nAChRs could explain the partial agonistic activity of varenicline on these nAChR subtypes. Varenicline 149-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 25475645-6 2015 Molecular dynamics simulations show that the interaction of varenicline to each allosteric site decreases the capping of Loop C at the halpha4beta2 nAChR, suggesting that these allosteric interactions limit the initial step in the gating process. Varenicline 60-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Acetylcholine 21-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Acetylcholine 36-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-155 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Acetylcholine 36-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Cysteine 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-155 25639674-1 2015 The neurotransmitter acetylcholine (ACh) can regulate neuronal excitability by acting on the cys-loop cation-conducting ligand-gated nicotinic ACh receptor (nAChR) channels. Cysteine 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 25642160-6 2014 Here, we review preclinical and clinical evidence involving a number of nAChR ligands that target different nAChR subtypes in alcohol and nicotine addiction. Alcohols 126-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Phosphatidylcholines 81-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Phosphatidylcholines 81-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Phosphatidylcholines 102-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Phosphatidylcholines 102-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Cholesterol 124-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 25519904-1 2015 Although the Torpedo nicotinic acetylcholine receptor (nAChR) reconstituted into phosphatidylcholine (PC) membranes lacking cholesterol and anionic lipids adopts a conformation where agonist binding is uncoupled from channel gating, the underlying mechanism remains to be defined. Cholesterol 124-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25642160-6 2014 Here, we review preclinical and clinical evidence involving a number of nAChR ligands that target different nAChR subtypes in alcohol and nicotine addiction. Alcohols 126-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 25642160-6 2014 Here, we review preclinical and clinical evidence involving a number of nAChR ligands that target different nAChR subtypes in alcohol and nicotine addiction. Nicotine 138-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 25642160-6 2014 Here, we review preclinical and clinical evidence involving a number of nAChR ligands that target different nAChR subtypes in alcohol and nicotine addiction. Nicotine 138-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 25642160-7 2014 The important ligands include cytisine, lobeline, mecamylamine, varenicline, sazetidine A and others that target alpha4beta2(*) nAChR subtypes as small molecule modulators of the brain nicotinic cholinergic system are also discussed. cytisine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 25642160-8 2014 Taken together, both preclinical and clinical data exist that support nAChR-based ligands as promising therapeutic agents for the treatment of alcohol and drug dependence. Alcohols 143-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 25451094-0 2014 Contribution of alpha4beta2 nAChR in nicotine-induced intracellular calcium response and excitability of MSDB neurons. Nicotine 37-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 25492812-3 2015 GABA differentially activates nAChR subtypes. gamma-Aminobutyric Acid 0-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 25492812-8 2015 Interestingly, single-channel activity elicited by GABA is similar to that elicited by ACh in gain-of-function nAChR mutants associated to congenital myasthenic syndromes, which could be important in the progression of the disorders due to steady exposure to serum GABA. gamma-Aminobutyric Acid 51-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 25492812-8 2015 Interestingly, single-channel activity elicited by GABA is similar to that elicited by ACh in gain-of-function nAChR mutants associated to congenital myasthenic syndromes, which could be important in the progression of the disorders due to steady exposure to serum GABA. Acetylcholine 87-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 25492812-8 2015 Interestingly, single-channel activity elicited by GABA is similar to that elicited by ACh in gain-of-function nAChR mutants associated to congenital myasthenic syndromes, which could be important in the progression of the disorders due to steady exposure to serum GABA. gamma-Aminobutyric Acid 265-269 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 25464883-3 2014 Homology modeling, molecular docking and molecular dynamics of ligand-receptor complexes in POPC membrane are used to find the mode of interactions of N-alkylated dextromethorphan derivatives with alpha3beta4 nAChR. n-alkylated dextromethorphan 151-179 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 25464883-4 2014 The compounds, similarly as dextromethorphan, interact with the middle portion of alpha3beta4 nAChR ion channel. Dextromethorphan 28-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 25921743-5 2015 In this review, the pharmacological efficacy of nAChR ligands, such as mecamylamine, lobeline, cytisine, sazetidine-A, and others will be discussed. Mecamylamine 71-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25921743-5 2015 In this review, the pharmacological efficacy of nAChR ligands, such as mecamylamine, lobeline, cytisine, sazetidine-A, and others will be discussed. Lobeline 85-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25921743-5 2015 In this review, the pharmacological efficacy of nAChR ligands, such as mecamylamine, lobeline, cytisine, sazetidine-A, and others will be discussed. cytisine 95-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25921743-5 2015 In this review, the pharmacological efficacy of nAChR ligands, such as mecamylamine, lobeline, cytisine, sazetidine-A, and others will be discussed. sazetidine-A 105-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25921743-6 2015 Overall, findings from preclinical and clinical studies included here suggest that the nAChR ligands may be of potential benefit in reducing MDD symptoms and that may aid in the prevention and treatment of MDD and co-morbid alcohol or nicotine use disorder. Alcohols 224-231 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 25921743-6 2015 Overall, findings from preclinical and clinical studies included here suggest that the nAChR ligands may be of potential benefit in reducing MDD symptoms and that may aid in the prevention and treatment of MDD and co-morbid alcohol or nicotine use disorder. Nicotine 235-243 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 25655889-3 2015 Attention-enhancing effects of the nonselective nAChR agonist nicotine can be observed in human nonsmokers and in laboratory animals, suggesting that benefits go beyond a reversal of withdrawal deficits in smokers. Nicotine 62-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 25655889-8 2015 Thus, attention-enhancing nAChR agents could spare the system central to nicotine dependence. Nicotine 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 25451094-2 2014 Nicotinic acetylcholine receptor (nAChR) subunits, alpha4beta2 and alpha7 nAChRs, are expressed in MSDB neurons and permeable to calcium ions, which may modulate the function of MSDB neurons. Calcium 129-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 25451094-2 2014 Nicotinic acetylcholine receptor (nAChR) subunits, alpha4beta2 and alpha7 nAChRs, are expressed in MSDB neurons and permeable to calcium ions, which may modulate the function of MSDB neurons. Calcium 129-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 25451094-3 2014 The aims of this study are to determine the roles of selective nAChR activation on the calcium responses and membrane currents in MSDB neurons. Calcium 87-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 25451094-4 2014 Our results showed that nicotine increased calcium responses in the majority of MSDB neurons, pre-treatment of MSDB slices with a alpha4beta2 nAChR antagonist, DhbetaE but not a alpha7 nAChR antagonist, MLA prevented nicotine-induced calcium responses. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 25451094-6 2014 Surprisingly, post-treatment of alpha4beta2 or alpha7 nAChR antagonists failed to block nicotine s role, they increased calcium responses instead. Calcium 120-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 25451094-8 2014 These results suggest that there was a subtype specific modulation of nAChRs on calcium signaling and membrane currents in MSDB neurons and nAChR antagonists were also able to induce calcium responses involving a distinct mechanism. Calcium 80-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 25451094-8 2014 These results suggest that there was a subtype specific modulation of nAChRs on calcium signaling and membrane currents in MSDB neurons and nAChR antagonists were also able to induce calcium responses involving a distinct mechanism. Calcium 183-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Varenicline 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Varenicline 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 25344397-2 2014 Chronic nicotine exposure alters the expression of various nAChR subtypes, which likely contributes to nicotine dependence; however, the underlying mechanisms regulating these changes remain unclear. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Alcohols 130-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Ethanol 139-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Ethanol 148-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 25581658-5 2014 In addition, effects of varenicline on acute stimulation and/or on the acquisition of sensitization would suggest a role for nAChR involvement in these effects of EtOH. Ethanol 163-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 25387119-1 2014 The alpha4beta2* nicotinic acetylcholine receptors (alpha4beta2*-nAChR) are highly abundant in the human brain. Acetylcholine 27-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 25387119-5 2014 Furthermore, recent developments of novel alpha4beta2*-nAChR-specific PET radioligands, such as (-)[18F]Flubatine or [18F]AZAN are summarized. fluoronorchloroepibatidine 104-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25387119-5 2014 Furthermore, recent developments of novel alpha4beta2*-nAChR-specific PET radioligands, such as (-)[18F]Flubatine or [18F]AZAN are summarized. Azaguanine 122-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25315828-2 2014 Choline is a selective alpha7 nAChR agonist and the aim of this study was to determine whether cytidine 5"-diphosphocholine (CDP-choline), or citicoline, a dietary source of choline, increases sensory gating and cognition in healthy volunteers stratified for gating level. Choline 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 25344397-2 2014 Chronic nicotine exposure alters the expression of various nAChR subtypes, which likely contributes to nicotine dependence; however, the underlying mechanisms regulating these changes remain unclear. Nicotine 103-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 25344397-11 2014 Our results provide evidence for a novel mode of nicotine-mediated regulation of the mammalian nAChR gene family. Nicotine 49-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 24836728-4 2014 The general nAChR agonist nicotine, as well as several nAChR agonists (varenicline, ABT-089 and ABT-894), reduces l-dopa-induced abnormal involuntary movements or dyskinesias up to 60% in parkinsonian nonhuman primates and rodents. Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 25450372-4 2014 The changes in the inhibitory activities of its Ala mutants, the NMR structure, and molecular simulation results based on other conotoxins targeting nAChR alpha4beta2, all demonstrated that the residues Ile(6) and Leu(14) were the main hydrophobic pharmacophores. Isoleucine 203-206 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 25450372-4 2014 The changes in the inhibitory activities of its Ala mutants, the NMR structure, and molecular simulation results based on other conotoxins targeting nAChR alpha4beta2, all demonstrated that the residues Ile(6) and Leu(14) were the main hydrophobic pharmacophores. Leucine 214-217 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 25282151-1 2014 We determined the X-ray crystal structures of the extracellular domain (ECD) of the monomeric state of human neuronal alpha9 nicotinic acetylcholine receptor (nAChR) and of its complexes with the antagonists methyllycaconitine and alpha-bungarotoxin at resolutions of 1.8 A, 1.7 A and 2.7 A, respectively. methyllycaconitine 208-226 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 25122874-15 2014 Similar to muscle injury, CSDS-treated fibroblasts disrupted nAChR clusters and hypersensitized myotube contraction, while ALDS-treated fibroblasts aggregated nAChRs in large clusters, which may have important clinical implications. csds 26-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 24950454-1 2014 There occur two rare variations, Asp(D)478Asn(N) and Asp(D)478Glu(E), in the putative cytoplasmic amphipathic alpha-helices of human nicotinic acetylcholine receptor (nAChR) alpha2 subunit as a result of mutation in the 1st (G A: rs141072985) and 3rd (C A: rs56344740) nucleotide of its 478th triplet codon (GAC). Aspartic Acid 33-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-165 24950454-1 2014 There occur two rare variations, Asp(D)478Asn(N) and Asp(D)478Glu(E), in the putative cytoplasmic amphipathic alpha-helices of human nicotinic acetylcholine receptor (nAChR) alpha2 subunit as a result of mutation in the 1st (G A: rs141072985) and 3rd (C A: rs56344740) nucleotide of its 478th triplet codon (GAC). Aspartic Acid 33-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 24950454-4 2014 Two-electrode voltage clamp analyses indicate that the agonist (ACh or nicotine) induced peak current responses (Imax) of alpha2beta2-nAChR isoforms and those of alpha2beta4-nAChR isoforms are increased (1.3-4.7-fold) as a result of D478E variation. Acetylcholine 64-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 24950454-4 2014 Two-electrode voltage clamp analyses indicate that the agonist (ACh or nicotine) induced peak current responses (Imax) of alpha2beta2-nAChR isoforms and those of alpha2beta4-nAChR isoforms are increased (1.3-4.7-fold) as a result of D478E variation. Acetylcholine 64-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 24950454-4 2014 Two-electrode voltage clamp analyses indicate that the agonist (ACh or nicotine) induced peak current responses (Imax) of alpha2beta2-nAChR isoforms and those of alpha2beta4-nAChR isoforms are increased (1.3-4.7-fold) as a result of D478E variation. Nicotine 71-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 24950454-4 2014 Two-electrode voltage clamp analyses indicate that the agonist (ACh or nicotine) induced peak current responses (Imax) of alpha2beta2-nAChR isoforms and those of alpha2beta4-nAChR isoforms are increased (1.3-4.7-fold) as a result of D478E variation. Nicotine 71-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 25360085-9 2014 This might be a general feature in different brain areas since a similar nAChR-mediated bolstering of NMDA-induced ([(3)H]D-Asp) overflow was also observed in hippocampal synaptosomes. N-Methylaspartate 102-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 25360085-9 2014 This might be a general feature in different brain areas since a similar nAChR-mediated bolstering of NMDA-induced ([(3)H]D-Asp) overflow was also observed in hippocampal synaptosomes. Aspartic Acid 124-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 24836728-4 2014 The general nAChR agonist nicotine, as well as several nAChR agonists (varenicline, ABT-089 and ABT-894), reduces l-dopa-induced abnormal involuntary movements or dyskinesias up to 60% in parkinsonian nonhuman primates and rodents. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 84-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 24836728-4 2014 The general nAChR agonist nicotine, as well as several nAChR agonists (varenicline, ABT-089 and ABT-894), reduces l-dopa-induced abnormal involuntary movements or dyskinesias up to 60% in parkinsonian nonhuman primates and rodents. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 96-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 24836728-4 2014 The general nAChR agonist nicotine, as well as several nAChR agonists (varenicline, ABT-089 and ABT-894), reduces l-dopa-induced abnormal involuntary movements or dyskinesias up to 60% in parkinsonian nonhuman primates and rodents. Levodopa 114-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 24836728-8 2014 Preclinical and clinical studies also show that the nAChR agonist varenicline improves balance and coordination in various ataxias. Varenicline 66-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 24836728-10 2014 Several nAChR subtypes appear to be involved in these beneficial effects of nicotine and nAChR drugs including alpha4beta2*, alpha6beta2* and alpha7 nAChRs (the asterisk indicates the possible presence of other subunits in the receptor). Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 8-13 24836728-11 2014 Overall, the above findings, coupled with nicotine"s neuroprotective effects, suggest that nAChR drugs have potential for future drug development for movement disorders. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 25237305-2 2014 Since cocaine is a weak nAChR inhibitor, we hypothesized that cocaine may alter DA release by inhibiting the nAChRs in DA terminals in the striatum and thus contribute to cocaine"s reinforcing properties primarily associated with the inhibition of DA transporters. Cocaine 6-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 25237305-2 2014 Since cocaine is a weak nAChR inhibitor, we hypothesized that cocaine may alter DA release by inhibiting the nAChRs in DA terminals in the striatum and thus contribute to cocaine"s reinforcing properties primarily associated with the inhibition of DA transporters. Cocaine 62-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 25237305-3 2014 We found that biologically relevant concentrations of cocaine can mildly inhibit nAChR-mediated currents in midbrain DA neurons and consequently alter DA release in the dorsal and ventral striatum. Cocaine 54-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 24762290-7 2014 CONCLUSIONS: These significant correlations between the results of the CERAD subtests and the cerebral alpha4beta2 nAchR density, as assessed by 5-I-A-85380 SPECT, indicate that cerebral cholinergic pathways are relevant to cognitive processing in IPD. 5-i-a 145-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 24966348-10 2014 Experiments with the nAChR channel blocker mecamylamine on P2X2-alpha6beta4 oocytes point to the loss of P2X2 channel activity during the crosstalk, whereas the ion channel pores of the P2X receptors were fully functional and unaltered by the receptor interaction for P2X2-alpha6beta4beta3, P2X2/3-alpha6beta4, and P2X2/3-alpha6beta4beta3. Mecamylamine 43-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 24990939-1 2014 The minimum pharmacophore for activation of the human alpha7 nicotinic acetylcholine receptor (nAChR) is the tetramethylammonium cation. tetramethylammonium 109-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 24990939-4 2014 We synthesized several panels of quaternary ammonium nAChR ligands that systematically varied the size of the substituents bonded to the central positively charged nitrogen atom. Nitrogen 164-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 24793809-2 2014 Previous studies have indicated that alpha5-nAChR is highly associated with lung cancer risk and nicotine dependence. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 24965900-0 2014 Sofinicline: a novel nicotinic acetylcholine receptor agonist in the treatment of attention-deficit/hyperactivity disorder. 3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo(3.2.0)heptane 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 24965900-3 2014 AREAS COVERED: This article reviews Phase I and Phase II trials of sofinicline (ABT-894), an agonist of the nAChR alpha4beta2 subtype, as a potential non-stimulant treatment for ADHD. 3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo(3.2.0)heptane 67-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 24965900-3 2014 AREAS COVERED: This article reviews Phase I and Phase II trials of sofinicline (ABT-894), an agonist of the nAChR alpha4beta2 subtype, as a potential non-stimulant treatment for ADHD. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 80-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 24177919-0 2014 A mutation in the extracellular domain of the alpha7 nAChR reduces calcium permeability. Calcium 67-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 24177919-1 2014 The alpha7 neuronal nicotinic acetylcholine receptor (nAChR) displays the highest calcium permeability among the different subtypes of nAChRs expressed in the mammalian brain and can impact cellular events including neurotransmitter release, second messenger cascades, cell survival, and apoptosis. Calcium 82-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 24177919-5 2014 In the alpha7 nAChR, it has been found that the ECD contains a ring of ten aspartates (two per subunit) that is believed to face the lumen of the pore and could attract cations for permeation. Aspartic Acid 75-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-19 24177919-6 2014 Using mutagenesis and a combination of electrophysiology and imaging techniques, we tested the possible involvement of these aspartate residues in the calcium permeability of the rat alpha7 nAChR. Aspartic Acid 125-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 24177919-6 2014 Using mutagenesis and a combination of electrophysiology and imaging techniques, we tested the possible involvement of these aspartate residues in the calcium permeability of the rat alpha7 nAChR. Calcium 151-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 24177919-7 2014 We found that one of these residues (the aspartate at position 44) appears to be essential since mutating it to alanine resulted in a decrease in amplitude for both whole cell and single-channel responses and in the complete disappearance of detectable calcium changes in most cells, which indicates that the ECD of the alpha7 nAChR plays a key role in calcium permeation. Aspartic Acid 41-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 327-332 24177919-7 2014 We found that one of these residues (the aspartate at position 44) appears to be essential since mutating it to alanine resulted in a decrease in amplitude for both whole cell and single-channel responses and in the complete disappearance of detectable calcium changes in most cells, which indicates that the ECD of the alpha7 nAChR plays a key role in calcium permeation. Alanine 112-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 327-332 24793809-12 2014 These results show that the alpha5-nAChR/HIF-1alpha/VEGF axis is involved in nicotine-induced tumor cell proliferation, which suggests that alpha5-nAChR may serve as a potential anticancer target in nicotine-associated lung cancer. Nicotine 199-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 24793809-12 2014 These results show that the alpha5-nAChR/HIF-1alpha/VEGF axis is involved in nicotine-induced tumor cell proliferation, which suggests that alpha5-nAChR may serve as a potential anticancer target in nicotine-associated lung cancer. Nicotine 199-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 24793809-4 2014 In the present study, we investigated the roles of alpha5-nAChR in the nicotine-induced expression of hypoxia-inducible factor-1alpha (HIF-1alpha) and vascular endothelial growth factor (VEGF). Nicotine 71-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 24793809-10 2014 In the A549 cell line, alpha5-nAChR and HIF-1alpha were found to be expressed under normal conditions, and their expression levels were significantly increased in response to nicotine treatment. Nicotine 175-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 24793809-11 2014 The silencing of alpha5-nAChR significantly inhibited the nicotine-induced cell proliferation compared with the control group and attenuated the nicotine-induced upregulation of HIF-1alpha and VEGF, and these effects required the cooperation of the ERK1/2 and PI3K/Akt signaling pathways. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 24793809-11 2014 The silencing of alpha5-nAChR significantly inhibited the nicotine-induced cell proliferation compared with the control group and attenuated the nicotine-induced upregulation of HIF-1alpha and VEGF, and these effects required the cooperation of the ERK1/2 and PI3K/Akt signaling pathways. Nicotine 145-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 24793809-12 2014 These results show that the alpha5-nAChR/HIF-1alpha/VEGF axis is involved in nicotine-induced tumor cell proliferation, which suggests that alpha5-nAChR may serve as a potential anticancer target in nicotine-associated lung cancer. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 24793809-12 2014 These results show that the alpha5-nAChR/HIF-1alpha/VEGF axis is involved in nicotine-induced tumor cell proliferation, which suggests that alpha5-nAChR may serve as a potential anticancer target in nicotine-associated lung cancer. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 24827506-5 2014 There is also growing evidence that the unique genetic makeup of an individual, such as polymorphisms in genes encoding nAChR subunits, might influence the susceptibility of that individual to the pathobiological effects of nicotine. Nicotine 224-232 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 24628360-1 2014 BACKGROUND AND PURPOSE: Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. Varenicline 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 24628360-1 2014 BACKGROUND AND PURPOSE: Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. Varenicline 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24628360-1 2014 BACKGROUND AND PURPOSE: Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. Ethanol 110-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24661093-3 2014 Previous studies have demonstrated that alpha6beta2*-nAChR are down-regulated following chronic nicotine exposure (unlike other subtypes that have been investigated - most prominently alpha4beta2* nAChR). Nicotine 96-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 24661093-3 2014 Previous studies have demonstrated that alpha6beta2*-nAChR are down-regulated following chronic nicotine exposure (unlike other subtypes that have been investigated - most prominently alpha4beta2* nAChR). Nicotine 96-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 24661093-5 2014 Chronic nicotine dose-responses and quantitative ligand-binding autoradiography were used to define nicotine sensitivity of changes in alpha4beta2*-nAChR and alpha6beta2*-nAChR expression. Nicotine 100-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 24661093-5 2014 Chronic nicotine dose-responses and quantitative ligand-binding autoradiography were used to define nicotine sensitivity of changes in alpha4beta2*-nAChR and alpha6beta2*-nAChR expression. Nicotine 100-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 171-176 24661093-6 2014 alpha6beta2*-nAChR down-regulation by chronic nicotine exposure in dopaminergic and optic-tract nuclei was three-fold more sensitive than up-regulation of alpha4beta2*-nAChR. Nicotine 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 24661093-7 2014 In contrast, nAChR-mediated [(3) H]-dopamine release from dopamine-terminal region synaptosomal preparations changed only in response to chronic treatment with high nicotine doses, whereas dopaminergic parameters (transporter expression and activity, dopamine receptor expression) were largely unchanged. Dopamine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 24661093-7 2014 In contrast, nAChR-mediated [(3) H]-dopamine release from dopamine-terminal region synaptosomal preparations changed only in response to chronic treatment with high nicotine doses, whereas dopaminergic parameters (transporter expression and activity, dopamine receptor expression) were largely unchanged. Nicotine 165-173 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 24661093-12 2014 Chronic nicotine treatment altered alpha6beta2*- and alpha4beta2*-nAChR-mediated [(3) H]-dopamine release from striatal and olfactory tubercle synaptosomes, but dopaminergic parameters were largely unaffected. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 24661093-12 2014 Chronic nicotine treatment altered alpha6beta2*- and alpha4beta2*-nAChR-mediated [(3) H]-dopamine release from striatal and olfactory tubercle synaptosomes, but dopaminergic parameters were largely unaffected. Dopamine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 24813183-8 2014 The catecholamine (CA) secretion induced by nAChR agonist (NCT") was significantly inhibited by the pyrilamine pretreatment. Catecholamines 4-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 24813183-8 2014 The catecholamine (CA) secretion induced by nAChR agonist (NCT") was significantly inhibited by the pyrilamine pretreatment. Pyrilamine 100-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 24813183-12 2014 Overall, these data suggest that pyrilamine directly docks into the ligand binding site of nAChRs and specifically inhibits the nAChR-mediated effects thereby causing inhibition of CA secretion. Pyrilamine 33-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 25265849-2 2014 It has been shown that in human umbilical vein endothelial cells (HUVECs) alpha7 nAChR agonists increase the intracellular calcium concentration ([Ca2+]i), thus inducing proliferation and vessel formation which are important stages of angiogenesis. Calcium 123-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 25265849-5 2014 The increase in [Ca2+]i induced by 1 mM choline was inhibited significantly (p = 0.014) in cells which had been pre-incubated for 15 min with methyllycaconitine (MLA), a selective alpha7 nAChR antagonist. Choline 40-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 25265849-5 2014 The increase in [Ca2+]i induced by 1 mM choline was inhibited significantly (p = 0.014) in cells which had been pre-incubated for 15 min with methyllycaconitine (MLA), a selective alpha7 nAChR antagonist. methyllycaconitine 142-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 25265849-5 2014 The increase in [Ca2+]i induced by 1 mM choline was inhibited significantly (p = 0.014) in cells which had been pre-incubated for 15 min with methyllycaconitine (MLA), a selective alpha7 nAChR antagonist. methyllycaconitine 162-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 187-192 25265849-8 2014 The increase in [Ca2+]i induced by compound 1 was significantly inhibited by MLA (p = 0.013) and completely inhibited by mecamylamine, a non-selective nAChR antagonist, indicating that the isoxazolic compound 1 acts as an alpha7 nAChR agonist. Mecamylamine 121-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-156 24886653-2 2014 Here we wanted to investigate the role of N-terminal domain (NTD) residues of human (h) nAChR alpha6 subunit in the functional expression of halpha6*-nAChRs. halpha6 141-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 24406270-0 2014 Functional interactions of varenicline and nicotine with nAChR subtypes implicated in cardiovascular control. Varenicline 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 24406270-0 2014 Functional interactions of varenicline and nicotine with nAChR subtypes implicated in cardiovascular control. Nicotine 43-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 24406270-5 2014 and of nicotine in smokers was derived from activation-inhibition curves for each nAChR subtype. Nicotine 7-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24886653-5 2014 While variations at residues Ser43 or Asn46 (both in N-terminal alpha-helix) in halpha6 subunit reduce halpha6hbeta2*-nAChRs function those at residues Arg96 (beta2-beta3 loop), Asp199 (loop F) or Ser233 (beta10-strand) increase halpha6hbeta2*-nAChR function. halpha6 80-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 24886653-5 2014 While variations at residues Ser43 or Asn46 (both in N-terminal alpha-helix) in halpha6 subunit reduce halpha6hbeta2*-nAChRs function those at residues Arg96 (beta2-beta3 loop), Asp199 (loop F) or Ser233 (beta10-strand) increase halpha6hbeta2*-nAChR function. halpha6hbeta2 103-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 24886653-8 2014 Incorporation of nAChR hbeta3 subunits always increase the function of wild-type or variant halpha6hbeta4-nAChRs except for those of halpha6(D57N, S156R, R87C or N171K)hbeta4-nAChRs. halpha6hbeta4-nachrs 92-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24886653-8 2014 Incorporation of nAChR hbeta3 subunits always increase the function of wild-type or variant halpha6hbeta4-nAChRs except for those of halpha6(D57N, S156R, R87C or N171K)hbeta4-nAChRs. halpha6 92-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24886653-8 2014 Incorporation of nAChR hbeta3 subunits always increase the function of wild-type or variant halpha6hbeta4-nAChRs except for those of halpha6(D57N, S156R, R87C or N171K)hbeta4-nAChRs. nachrs 106-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24886653-12 2014 Variations (Asp57Asn, Arg87Cys, Asp92Glu, Ser156Arg or Asn171Lys) in halpha6 subunit that compromise halpha6*-nAChR function are expected to contribute to individual differences in responses to smoked nicotine. halpha6 69-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 24886653-12 2014 Variations (Asp57Asn, Arg87Cys, Asp92Glu, Ser156Arg or Asn171Lys) in halpha6 subunit that compromise halpha6*-nAChR function are expected to contribute to individual differences in responses to smoked nicotine. halpha6 101-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 24832553-7 2014 This MoA is considered not relevant to humans, given fundamental qualitative differences in sulfoxaflor agonism on the rat versus the human muscle nAChR. sulfoxaflor 92-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 24703234-1 2014 N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. n-substituted amino-2(5h)-oxazolones a 0-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-115 24703234-1 2014 N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. n-substituted amino-2(5h)-oxazolones a 0-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 24569419-2 2014 Genetic variants in the nicotinic acetylcholine receptor (nAChR) genes have been associated with nicotine dependence, and are likely to influence renal function and related traits. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-56 24569419-2 2014 Genetic variants in the nicotinic acetylcholine receptor (nAChR) genes have been associated with nicotine dependence, and are likely to influence renal function and related traits. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 24569419-8 2014 In contrast, a gene-family analysis considering the joint impact of all 61 SNPs reveals significant associations of the nAChR gene family with kidney function variables including estimated glomerular filtration rate, urinary albumin/creatinine ratio, and albuminuria (all Ps <= 0.0001) after adjusting for established risk factors including cigarette smoking. Creatinine 233-243 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 24428733-5 2014 RESULTS: Frequency of binge drinking and other correlated alcohol consumption measures were significantly associated with SNPs in CHRNA4 (p-values ranged from 0.0003 to 0.02), but not with SNPs in other CHRNs. Alcohols 58-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-136 24627467-1 2014 Although nicotine mediates its effects through several nicotinic acetylcholine receptor (nAChR) subtypes, it remains to be determined which nAChR subtypes directly mediate heightened anxiety during withdrawal. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 24627467-1 2014 Although nicotine mediates its effects through several nicotinic acetylcholine receptor (nAChR) subtypes, it remains to be determined which nAChR subtypes directly mediate heightened anxiety during withdrawal. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 24627467-2 2014 Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Varenicline 77-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 24627467-2 2014 Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Varenicline 90-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 24412748-8 2014 Collectively, these results demonstrate that GW1929 not only inhibits but also antagonizes Ach-induced NSCLC cell growth by inhibition of alpha7 nAChR expression through PPARgamma-independent signals that are associated with activation of p38 MPAK and inactivation of PI3-K/mTOR, followed by inducing Egr-1 protein and Egr-1 binding activity in the alpha7 nAChR gene promoter. GW 1929 45-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 356-361 24412748-0 2014 GW1929 inhibits alpha7 nAChR expression through PPARgamma-independent activation of p38 MAPK and inactivation of PI3-K/mTOR: The role of Egr-1. GW 1929 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 24412748-1 2014 Studies demonstrated that peroxisome proliferator-activated receptor gamma (PPARgamma) ligands reduce nicotine-induced non small cell lung carcinoma (NSCLC) cell growth through inhibition of nicotinic acetylcholine receptor (nAChR) mediated signaling pathways. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-223 24412748-1 2014 Studies demonstrated that peroxisome proliferator-activated receptor gamma (PPARgamma) ligands reduce nicotine-induced non small cell lung carcinoma (NSCLC) cell growth through inhibition of nicotinic acetylcholine receptor (nAChR) mediated signaling pathways. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-230 24412748-4 2014 Interestingly, GW1929 inhibited alpha7 nAChR expression, which was not blocked by GW9662, an antagonist of PPARgamma, or by PPARgamma siRNA, but was abrogated by the p38 MPAK inhibitor SB239063. GW 1929 15-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 24412748-8 2014 Collectively, these results demonstrate that GW1929 not only inhibits but also antagonizes Ach-induced NSCLC cell growth by inhibition of alpha7 nAChR expression through PPARgamma-independent signals that are associated with activation of p38 MPAK and inactivation of PI3-K/mTOR, followed by inducing Egr-1 protein and Egr-1 binding activity in the alpha7 nAChR gene promoter. GW 1929 45-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 24412748-8 2014 Collectively, these results demonstrate that GW1929 not only inhibits but also antagonizes Ach-induced NSCLC cell growth by inhibition of alpha7 nAChR expression through PPARgamma-independent signals that are associated with activation of p38 MPAK and inactivation of PI3-K/mTOR, followed by inducing Egr-1 protein and Egr-1 binding activity in the alpha7 nAChR gene promoter. Acetylcholine 91-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 24412748-8 2014 Collectively, these results demonstrate that GW1929 not only inhibits but also antagonizes Ach-induced NSCLC cell growth by inhibition of alpha7 nAChR expression through PPARgamma-independent signals that are associated with activation of p38 MPAK and inactivation of PI3-K/mTOR, followed by inducing Egr-1 protein and Egr-1 binding activity in the alpha7 nAChR gene promoter. Acetylcholine 91-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 356-361 24412748-9 2014 By downregulation of the alpha7 nAchR, GW1929 blocks cholinergic signaling and inhibits NSCLC cell growth. GW 1929 39-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 24515328-16 2014 ABT-894 and ABT-089 appear to be good candidate nAChR drugs for the management of LIDs in Parkinson"s disease. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 24515328-16 2014 ABT-894 and ABT-089 appear to be good candidate nAChR drugs for the management of LIDs in Parkinson"s disease. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 12-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 24326163-8 2014 Our findings thus identify specific loss of synaptic NMDARs and their coagonist, d-serine, as well as glutamatergic synaptic deficits in alpha7 nAChR gene deletion models of cortical dysfunction, thereby implicating alpha7 nAChR-mediated control of synaptic NMDARs and serine racemase/d-serine pathways in cortical dysfunction underlying many neuropsychiatric and neurodevelopmental disorders, particularly those associated with deletion of human CHRNA7. Deuterium 7-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 223-228 24467848-0 2014 A signal peptide missense mutation associated with nicotine dependence alters alpha2*-nicotinic acetylcholine receptor function. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-118 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Cytosine 2-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Cytosine 2-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Thymidine 14-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Thymidine 14-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Threonine 172-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Threonine 172-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Nicotine 238-246 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 24467848-1 2014 A cytosine to thymidine (C T) missense mutation in the signal peptide (SP) sequence (rs2472553) of the nicotinic acetylcholine receptor (nAChR) alpha2 subunit produces a threonine-to-isoleucine substitution (T22I) often associated with nicotine dependence (ND). Nicotine 238-246 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 24467848-2 2014 We assessed effects on function of alpha2*-nAChR ("*"indicates presence of additional subunits) of this mutation, which could alter SP cleavage, RNA/protein secondary structure, and/or efficiency of transcription, translation, subunit assembly, receptor trafficking or cell surface expression. Protein Sorting Signals 132-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 24467848-6 2014 We hypothesize that lower sensitivity of human alpha2*-nAChR to nicotine could contribute to increased susceptibility to ND. Nicotine 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 24633083-5 2014 Similar changes in nAChR-mediated neurotransmitter production were identified as the cause of NSCLC stimulation in vitro and in xenograft models by chronic nicotine. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 24190916-3 2014 Unlike previously studied agonists, desensitization by the highly selective agonists A-85380 [3-(2(S)-azetidinylmethoxy)pyridine] and sazetidine-A (Saz-A) preferentially reduced alpha4beta2-nAChR HS-phase versus LS-phase responses. A 85380 94-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 24385388-9 2014 Taken together, these experiments suggest that genetic variation at CHRNA4 alters the assembly and expression of human alpha4beta2 nAChRs, resulting in receptors that are more sensitive to nicotine exposure than those assembled with the common alpha4 variant. Nicotine 189-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-74 24385388-10 2014 The changes in nAChR pharmacology could contribute to differences in responses to smoked nicotine in individuals harboring these rare variants. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 24616704-6 2014 These include sites at locations associated with the well-known cholesterol binding motif CRAC and its reversed form CARC in nAChR, BK, and TRPV, as well as novel cholesterol binding regions in Kir channels. Cholesterol 64-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 24362025-3 2014 Direct activation is sensitive to alpha7 nAChR antagonist methyllycaconitine, although the primed potentiation is not. methyllycaconitine 58-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 24469431-6 2014 A nicotinic acetylcholine receptor (nAChR) labeled with a fluorescein derivative was used to develop this assay. Fluorescein 58-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 2-34 24469431-6 2014 A nicotinic acetylcholine receptor (nAChR) labeled with a fluorescein derivative was used to develop this assay. Fluorescein 58-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 24369841-1 2014 Both enantiomers of the epibatidine analogue flubatine display high affinity towards the alpha4beta2 nicotinic acetylcholine receptor (nAChR) in vitro, accompanied by negligible interactions with diverse off-target proteins. epibatidine 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 24369841-1 2014 Both enantiomers of the epibatidine analogue flubatine display high affinity towards the alpha4beta2 nicotinic acetylcholine receptor (nAChR) in vitro, accompanied by negligible interactions with diverse off-target proteins. fluoronorchloroepibatidine 45-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 24117996-8 2014 In addition, nicotine exerted full spine-enlarging response in the post-synaptic neuron whose beta2 nAChR expression was knocked down. Nicotine 13-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 24616704-3 2014 The first major insight that comes from growing number of studies that based on the sterol specificity of cholesterol effects, show that several types of ion channels (nAChR, Kir, BK, TRPV) are regulated by specific sterol-protein interactions. Cholesterol 106-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 24362025-0 2014 The activity of GAT107, an allosteric activator and positive modulator of alpha7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface. Amino Acids, Aromatic 140-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-121 24362025-1 2014 GAT107, the (+)-enantiomer of racemic 4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide, is a strong positive allosteric modulator (PAM) of alpha7 nicotinic acetylcholine receptor (nAChR) activation by orthosteric agonists with intrinsic allosteric agonist activities. 4-(4-bromophenyl)-3a,4,5,9b 38-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 210-215 24057800-6 2014 In application to a real dataset, we detected one significant tetragenic interaction among CHRNA4, CHRNB2, BDNF, and NTRK2 associated with nicotine dependence in the Study of Addiction: Genetics and Environment sample, suggesting the biological role of these genes in nicotine dependence development. Nicotine 139-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-97 24057800-6 2014 In application to a real dataset, we detected one significant tetragenic interaction among CHRNA4, CHRNB2, BDNF, and NTRK2 associated with nicotine dependence in the Study of Addiction: Genetics and Environment sample, suggesting the biological role of these genes in nicotine dependence development. Nicotine 268-276 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-97 23990377-1 2014 Through linkage analysis, candidate gene approach, and genome-wide association studies (GWAS), many genetic susceptibility factors for substance dependence have been discovered such as the alcohol dehydrogenase gene (ALDH2) for alcohol dependence (AD) and nicotinic acetylcholine receptor (nAChR) subunit variants on chromosomes 8 and 15 for nicotine dependence (ND). Nicotine 342-350 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 256-288 23990377-1 2014 Through linkage analysis, candidate gene approach, and genome-wide association studies (GWAS), many genetic susceptibility factors for substance dependence have been discovered such as the alcohol dehydrogenase gene (ALDH2) for alcohol dependence (AD) and nicotinic acetylcholine receptor (nAChR) subunit variants on chromosomes 8 and 15 for nicotine dependence (ND). Nicotine 342-350 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 290-295 24498031-4 2014 Alpha4 nicotinic acetylcholine receptor (nAChR) subunit-related phenotypes were assessed by the Fagerstrom Test for Nicotine Dependence (FTND), exhaled carbon monoxide (CO) measurements, the Minnesota Nicotine Withdrawal Scale (MNWS) and the Zung Self-Rating Depression Scale (ZSDS). Nicotine 116-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 25324001-4 2014 The ionic events (Ca(+2) influx) are generated by the ACh-opening of nAChR channels, while the metabolic events by ACh-binding to G-proteincoupled mAChR. Acetylcholine 54-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 25324001-10 2014 Inhibition of M3 by antisense or antagonists (Darifenacin, Tiotropium) reduces lung or colon cancer proliferation, as well as inhibition of alpha9- nAChR [polyphenol (-)-epigallocatechin-3-gallate] diminishes breast cancer cells growth. polyphenol (-)-epigallocatechin-3-gallate 155-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 24190916-4 2014 The concatenated-nAChR experiments confirmed that approximately 20% of LS-isoform acetylcholine-induced function occurs in an HS-like phase, which is abolished by Saz-A preincubation. Acetylcholine 82-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24190916-3 2014 Unlike previously studied agonists, desensitization by the highly selective agonists A-85380 [3-(2(S)-azetidinylmethoxy)pyridine] and sazetidine-A (Saz-A) preferentially reduced alpha4beta2-nAChR HS-phase versus LS-phase responses. sazetidine-A 134-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 24882143-1 2014 Nicotine (NIC) is an exogenous ligand of the nicotinic acetylcholine receptor (nAChR), and it influences various functions in the central nervous system. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-77 24882143-1 2014 Nicotine (NIC) is an exogenous ligand of the nicotinic acetylcholine receptor (nAChR), and it influences various functions in the central nervous system. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 24190916-4 2014 The concatenated-nAChR experiments confirmed that approximately 20% of LS-isoform acetylcholine-induced function occurs in an HS-like phase, which is abolished by Saz-A preincubation. leucylserine 71-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24882143-1 2014 Nicotine (NIC) is an exogenous ligand of the nicotinic acetylcholine receptor (nAChR), and it influences various functions in the central nervous system. Nicotine 10-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-77 24882143-1 2014 Nicotine (NIC) is an exogenous ligand of the nicotinic acetylcholine receptor (nAChR), and it influences various functions in the central nervous system. Nicotine 10-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 24882143-10 2014 Taken together, these findings suggest that NIC-induced antinociception and the development of physical dependence are mediated by the endogenous opioid system, via the alpha7 nAChR. Nicotine 44-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 176-181 24190916-4 2014 The concatenated-nAChR experiments confirmed that approximately 20% of LS-isoform acetylcholine-induced function occurs in an HS-like phase, which is abolished by Saz-A preincubation. sazetidine-A 163-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 24190916-10 2014 These studies elucidate the receptor-level differences underlying the differential pharmacology of the two alpha4beta2-nAChR isoforms, and demonstrate that HS versus LS alpha4beta2-nAChR activity can be selectively manipulated using pharmacological approaches. hassio 156-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 24190916-10 2014 These studies elucidate the receptor-level differences underlying the differential pharmacology of the two alpha4beta2-nAChR isoforms, and demonstrate that HS versus LS alpha4beta2-nAChR activity can be selectively manipulated using pharmacological approaches. leucylserine 166-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 24376846-1 2013 We describe the expression of the extracellular domain of the human alpha1 nicotinic acetylcholine receptor (nAChR) in lepidopteran insect cells (i-alpha1-ECD) and its suitability for use in antigen-specific therapies for Myasthenia Gravis (MG). Acetylcholine 85-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 24274400-1 2013 Nicotine binds to nicotinic acetylcholine receptors (nAChR), which can exist as many different subtypes. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-51 24274400-1 2013 Nicotine binds to nicotinic acetylcholine receptors (nAChR), which can exist as many different subtypes. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 24274400-2 2013 The alpha4beta2 nAChR is the most prevalent subtype in the brain and possesses the most evidence linking it to nicotine seeking behavior. Nicotine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 24012499-2 2013 The effect of nAChR agonists and antagonists on SR activity and expression was examined by following concentration-dependent changes in intracellular d-Ser levels and SR protein expression. D-serine 150-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-19 24194515-3 2013 Here we show that in contrast to the alpha7 nAChR, the alpha7beta2 nAChR is highly susceptible to inhibition by the volatile anesthetic isoflurane in electrophysiology measurements. Isoflurane 136-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 24145137-0 2013 The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. 3,7-diazabicyclo(3.3.1)nonane 4-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-97 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. 3,7-diazabicyclo(3.3.1)nonane 0-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. 3,7-diazabicyclo(3.3.1)nonane 0-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. bispidine 31-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. bispidine 31-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. nachrs 137-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 24145137-2 2013 3,7-Diazabicyclo[3.3.1]nonane (bispidine) based nicotinic acetylcholine receptor (nAChR) ligands have been synthesized and evaluated for nAChRs interaction. nachrs 137-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24358207-12 2013 Nicotine was sensed by nAChR and the signal was transduced by Sp1 which bound to the R3 region of LDLR gene. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 24012499-10 2013 We propose that nAChR-associated changes in Ca(2+) flux affect SR activity, but not expression, and that MLA and (R,S)-dehydronorketamine bind to allosteric sites on the alpha7-nAChR and promote multiple signaling cascades that converge at mTOR to increase m-SR levels. (r,s)-dehydronorketamine 113-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 24012499-3 2013 Incubation with (S)-nicotine increased d-Ser levels, which were attenuated by the alpha7-nAChR antagonist methyllycaconitine (MLA). Nicotine 16-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 24012499-3 2013 Incubation with (S)-nicotine increased d-Ser levels, which were attenuated by the alpha7-nAChR antagonist methyllycaconitine (MLA). D-serine 39-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 24012499-3 2013 Incubation with (S)-nicotine increased d-Ser levels, which were attenuated by the alpha7-nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 106-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 24012499-3 2013 Incubation with (S)-nicotine increased d-Ser levels, which were attenuated by the alpha7-nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 126-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 24012499-4 2013 Treatment of PC-12 cells with mecamylamine (MEC) produced a bimodal reduction of d-Ser reflecting MEC inhibition of homomeric and heteromeric nAChRs, while a unimodal curve was observed with 1321N1 cells, reflecting predominant expression of alpha7-nAChR. Mecamylamine 30-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 24012499-4 2013 Treatment of PC-12 cells with mecamylamine (MEC) produced a bimodal reduction of d-Ser reflecting MEC inhibition of homomeric and heteromeric nAChRs, while a unimodal curve was observed with 1321N1 cells, reflecting predominant expression of alpha7-nAChR. Mecamylamine 44-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 24012499-5 2013 The nAChR subtype selectivity was probed using alpha7-nAChR selective inhibitors MLA and (R,S)-dehydronorketamine and alpha3beta4-nAChR specific inhibitor AT-1001. (r,s)-dehydronorketamine 89-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 24236983-6 2013 Significantly, pretreatment with diCQAs attenuated the neurotoxic effects of Abeta25-35 , a neuroprotective effect in which the upregulation of alpha7 and alpha3 nAChR may be involved. caffeoylquinic acid 33-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 24100032-4 2013 We performed alanine scanning mutagenesis of AuIB and alpha3beta4 nAChR, homology modeling, and molecular dynamics simulations to identify the structural determinants of the AuIB alpha3beta4 nAChR interaction. Alanine 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 24100032-8 2013 Homology modeling and molecular dynamics simulations suggest that Phe-9 of AuIB interacts with a two-residue binding pocket on the beta4 nAChR subunit. Phenylalanine 66-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 24276616-5 2013 In this study, we computationally analyzed the role of this water molecule as a putative hydrogen bond donor/acceptor moiety in the agonist binding site of the three most relevant heteromeric (alpha4beta2, alpha3beta4) and homomeric (alpha7) neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Water 60-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 285-290 24051136-4 2013 Firstly, the signaling evoked by physiologically relevant ACh concentrations through the (alpha4)3(beta2)2 nAChR in HEK293 cells was potentiated by NS9283, consistent with the classification of NS9283 as a PAM. Acetylcholine 58-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 24276616-5 2013 In this study, we computationally analyzed the role of this water molecule as a putative hydrogen bond donor/acceptor moiety in the agonist binding site of the three most relevant heteromeric (alpha4beta2, alpha3beta4) and homomeric (alpha7) neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Hydrogen 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 285-290 23624811-5 2013 RESULTS: The objective of this review is to describe the multiple cellular pathways through which chronic nicotine exposure regulates nAChR expression, and to juxtapose these mechanisms with evidence for altered expression of high-affinity nAChRs in human psychiatric illness. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 24013278-3 2013 In the absence of anionic lipids and cholesterol, the nAChR adopts an uncoupled conformation, which binds agonist with resting state-like affinity but does not usually undergo agonist-induced conformational transitions. Cholesterol 37-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 23902940-4 2013 We first tested the nonselective nAChR agonist 1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine (varenicline), which offers the advantage that it is approved by the U.S. Food and Drug Administration for use in humans. 1, 6,7,8,9-tetrahydro-6,10-methano-6h-pyrazino[2,3-h][3]benzazepine 47-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 23902940-7 2013 We next tested the selective alpha4beta2*/alpha6beta2* nAChR agonist TC-8831 [3-cyclopropylcarbonyl-3,6-diazabicyclo[3.1.1]heptane] on LIDs in the same set of monkeys after a 10-week washout. TC-8831 69-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 23902940-13 2013 These data suggest that nAChR agonists may be useful for the management of dyskinesias in l-DOPA-treated Parkinson"s disease patients. Levodopa 90-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 23830821-3 2013 We review what is known of the processes regulating nAChR assembly, degradation and trafficking, and how nicotine-induced modulation of these processes leads to nAChR up-regulation and changes in downstream neuronal plasticity at molecular, cellular and circuit level. Nicotine 105-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). gamma-Aminobutyric Acid 29-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). gamma-Aminobutyric Acid 29-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). Glutamic Acid 81-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). Glutamic Acid 81-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). gamma-Aminobutyric Acid 161-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 23771165-3 2013 In this study, an open-state GABA(A)R was constructed using the structure of the glutamate-gated chloride channel (GluCl), which has a high sequence identity to GABA(A)R. A closed-state model was constructed using the structure of the nicotinic acetylcholine receptor (nAChR). gamma-Aminobutyric Acid 161-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 23389808-1 2013 About 85 % of patients with generalized myasthenia gravis (MG) have anti-nicotinic acetylcholine receptor (nAChR) antibodies in their sera (seropositive MG; SPMG). Acetylcholine 83-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 23574176-5 2013 This review highlights the important preclinical findings involving nAChR ligands in regulating nicotine, alcohol and other addictive drug-induced neurobiological changes in animal models and humans. Nicotine 96-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 23937977-1 2013 We have carried out computational studies on interactions of diazabicyclic amide analogs with alpha4beta2 nAChR using homology modeling, docking and pharmacophore elucidation techniques. diazabicyclic 61-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 23937977-1 2013 We have carried out computational studies on interactions of diazabicyclic amide analogs with alpha4beta2 nAChR using homology modeling, docking and pharmacophore elucidation techniques. Amides 75-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 23937977-8 2013 These findings could be exploited to design diverse and selective novel chemical libraries for the treatment of diseases and conditions where the alpha4beta2 nAChR is disrupted, such as Alzheimer disease, Parkinson"s disease and l-dopa-induced dyskinesia (LID). Levodopa 229-235 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 23639435-6 2013 Nortriptyline is an exception with a Cu,b that is 2-fold below its IC50, which is comparable to the nAChR antagonist (+-)-mecamylamine, for which Cu,b is 4-fold below its IC50; both drugs will inhibit a substantial fraction of alpha4beta2 nAChRs. Mecamylamine 117-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 23757208-2 2013 We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. benzamide 155-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 23757208-2 2013 We exploited knowledge on nAChR ligands and their binding site that were previously identified by our laboratory through virtual screenings and identified benzamide analogs as a novel chemical class of neuronal nicotinic receptor (nAChR) ligands. benzamide 155-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 231-236 23757208-3 2013 The lead molecule, compound 1 (4-(allyloxy)-N-(6-methylpyridin-2-yl)benzamide) inhibits nAChR activity with an IC50 value of 6.0 (3.4-10.6) muM on human alpha4beta2 nAChRs with a ~5-fold preference against human alpha3beta4 nAChRs. 4-(allyloxy)-n-(6-methylpyridin-2-yl)benzamide 31-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 23757208-3 2013 The lead molecule, compound 1 (4-(allyloxy)-N-(6-methylpyridin-2-yl)benzamide) inhibits nAChR activity with an IC50 value of 6.0 (3.4-10.6) muM on human alpha4beta2 nAChRs with a ~5-fold preference against human alpha3beta4 nAChRs. nachrs 165-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 23604333-2 2013 Moreover, the TT genotype of the nicotinic acetylcholine receptor (nAChR) alpha3-subunit (CHRNA3) rs1051730 polymorphism has previously been associated with diminished PPI and nicotine dependence. Nicotine 176-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-65 23604333-2 2013 Moreover, the TT genotype of the nicotinic acetylcholine receptor (nAChR) alpha3-subunit (CHRNA3) rs1051730 polymorphism has previously been associated with diminished PPI and nicotine dependence. Nicotine 176-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 23604333-8 2013 CONCLUSIONS: The present findings imply that the effect of nicotine on sensorimotor gating is modulated by nAChR alpha3-subunits. Nicotine 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 23574176-5 2013 This review highlights the important preclinical findings involving nAChR ligands in regulating nicotine, alcohol and other addictive drug-induced neurobiological changes in animal models and humans. Alcohols 106-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 23833792-0 2004 5-(6-(5-[(11)C]methylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)pyridazin-3-yl)-1H-indole The nicotinic acetylcholine receptors (nAChR) are pentameric ligand-gated cation channels that are found primarily in the central nervous system of mammals and are composed of alpha and beta subunits arranged in various homomeric or heteromeric stoichiometric arrangements (for details, see dos Santos Coura and Granon (1)). 5-(6-(5-methylhexahydropyrrolo(3,4-c)pyrrol-2(1H)-yl)pyridazin-3-yl)-1H-indole 0-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 23603380-8 2013 The blockade of anabasine and myosmine actions in TE-671 cells by alpha conotoxin GI indicates that they are agonists at fetal muscle-type nAChR. Anabasine 16-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 23603380-8 2013 The blockade of anabasine and myosmine actions in TE-671 cells by alpha conotoxin GI indicates that they are agonists at fetal muscle-type nAChR. myosmine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 23603417-4 2013 Mecamylamine easily traverses the blood-brain barrier to reach the central nervous system (CNS), where it acts as a nicotinic acetylcholine receptor (nAChR) antagonist, inhibiting all known nAChR subtypes. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-148 23603417-4 2013 Mecamylamine easily traverses the blood-brain barrier to reach the central nervous system (CNS), where it acts as a nicotinic acetylcholine receptor (nAChR) antagonist, inhibiting all known nAChR subtypes. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 23603417-4 2013 Mecamylamine easily traverses the blood-brain barrier to reach the central nervous system (CNS), where it acts as a nicotinic acetylcholine receptor (nAChR) antagonist, inhibiting all known nAChR subtypes. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 23801676-3 2013 We also present a receptor blocking study in a nicotine subject dosed with the alpha4beta2-nAChR-selective partial agonist varenicline. Nicotine 47-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 23801676-3 2013 We also present a receptor blocking study in a nicotine subject dosed with the alpha4beta2-nAChR-selective partial agonist varenicline. Varenicline 123-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 23801676-9 2013 CONCLUSION: (18)F-AZAN is a highly specific, safe, and effective PET radioligand for human subjects that requires only 90 min of PET scanning to estimate high-affinity alpha4beta2-nAChR in the living human brain. f-azan 16-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 23884938-2 2013 The prototypical agonist nicotine acts intracellularly to upregulate many nAChR subtypes, a phenomenon that is thought to contribute to the nicotine dependence of cigarette smokers. Nicotine 25-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 23884938-2 2013 The prototypical agonist nicotine acts intracellularly to upregulate many nAChR subtypes, a phenomenon that is thought to contribute to the nicotine dependence of cigarette smokers. Nicotine 140-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 23884938-8 2013 Our findings uncover a novel mechanism of nicotine-induced alpha3beta4 nAChR upregulation that may be relevant also for other nAChR subtypes. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 23884938-8 2013 Our findings uncover a novel mechanism of nicotine-induced alpha3beta4 nAChR upregulation that may be relevant also for other nAChR subtypes. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 23818597-4 2013 Here we explore alpha7-nAChR localization and actions in primate dlPFC and find that they are enriched in glutamate network synapses, where they are essential for dlPFC persistent firing, with permissive effects on NMDA receptor actions. Glutamic Acid 106-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 23818597-8 2013 We additionally show that alpha7-nAChR stimulation is needed for NMDA actions, suggesting that it is key for the engagement of dlPFC circuits. N-Methylaspartate 65-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 23869214-1 2013 Human genetic association studies have shown gene variants in the alpha5 subunit of the neuronal nicotinic receptor (nAChR) influence both ethanol and nicotine dependence. Ethanol 139-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 23869214-1 2013 Human genetic association studies have shown gene variants in the alpha5 subunit of the neuronal nicotinic receptor (nAChR) influence both ethanol and nicotine dependence. Nicotine 151-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 23869214-11 2013 Additionally, the alpha5alpha4* nAChR in VTA dopaminergic neurons regulates the effect of nicotine but not ethanol on currents. Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 23171716-3 2013 We sought to determine if menthol cigarette usage results in greater nAChR up-regulation than non-menthol cigarette usage. Menthol 26-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 23238810-4 2013 The inward current of the epsilon-nAChR was activated by use of 10 mumol/L acetylcholine alone or in combination with different concentrations of sevoflurane, isoflurane, or rocuronium. Acetylcholine 75-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23238810-4 2013 The inward current of the epsilon-nAChR was activated by use of 10 mumol/L acetylcholine alone or in combination with different concentrations of sevoflurane, isoflurane, or rocuronium. Sevoflurane 146-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23238810-4 2013 The inward current of the epsilon-nAChR was activated by use of 10 mumol/L acetylcholine alone or in combination with different concentrations of sevoflurane, isoflurane, or rocuronium. Isoflurane 159-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23238810-4 2013 The inward current of the epsilon-nAChR was activated by use of 10 mumol/L acetylcholine alone or in combination with different concentrations of sevoflurane, isoflurane, or rocuronium. Rocuronium 174-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23238810-9 2013 Sevoflurane or isoflurane (0.5 IC5) with rocuronium at IC5, IC25, and IC50 synergistically inhibited the current amplitude of adult-type muscle epsilon-nAChR. Sevoflurane 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 23238810-9 2013 Sevoflurane or isoflurane (0.5 IC5) with rocuronium at IC5, IC25, and IC50 synergistically inhibited the current amplitude of adult-type muscle epsilon-nAChR. Isoflurane 15-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 23238810-9 2013 Sevoflurane or isoflurane (0.5 IC5) with rocuronium at IC5, IC25, and IC50 synergistically inhibited the current amplitude of adult-type muscle epsilon-nAChR. Rocuronium 41-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 23545348-9 2013 Both toxins inhibited contractile responses to exogenous ACh and CCh, but not KCl, suggesting a post-synaptic mode of action at the nicotinic acetylcholine receptor (nAChR). Acetylcholine 57-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 23414838-1 2013 High throughput screening led to the identification of a novel series of quinolone alpha7 nicotinic acetylcholine receptor (nAChR) agonists. Quinolones 73-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 23700644-8 2004 5-(3"-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine (nifrolidine) is a putative and selective nAChR antagonist with nanomolar affinity. 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 0-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 23700644-8 2004 5-(3"-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine (nifrolidine) is a putative and selective nAChR antagonist with nanomolar affinity. 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 59-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 23700644-11 2004 5-(3"-[(18)F]-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine ([(18)F]nifrolidine) is being developed as a PET agent with faster kinetics than 2-[(18)F]FA and 6-[(18)F]FA for the noninvasive study of nAChR in the brain (6). 5-(3"-[(18)f]-fluoropropyl)-3-(2-(s)-pyrrolidinylmethoxy)pyridine 0-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 23700644-11 2004 5-(3"-[(18)F]-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine ([(18)F]nifrolidine) is being developed as a PET agent with faster kinetics than 2-[(18)F]FA and 6-[(18)F]FA for the noninvasive study of nAChR in the brain (6). 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 74-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 23553665-8 2013 In addition, rs755203 and rs1044397 in CHRNA4 were associated with nicotine dependence in healthy controls. Nicotine 67-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-45 23553665-10 2013 In addition, rs755203 and rs1044397 in CHRNA4 might play a role in the pathophysiology of nicotine dependence in healthy controls in the Japanese population. Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-45 23626818-11 2013 However, treatment with the Rho associated kinase inhibitor Y27632 resulted in a significant increase in alpha3beta4 nAChR levels within N-cadherin-mediated cell-cell contacts. Y 27632 60-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 23479730-5 2013 Sustained exposure of Abeta(1-42) to alpha4beta2 nAChR-transfected cells for several days led to increased Ca(2+) responses on subsequent acute stimulation with Abeta(1-42) or nicotine, paralleled by increased expression levels of alpha4beta2 nAChRs, likely the result of enhanced receptor recycling. Nicotine 176-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 23278456-9 2013 CONCLUSIONS AND IMPLICATIONS: This study demonstrates that NS9283 increases responsiveness of human (alpha4)3(beta2)2 nAChR to ACh with no change in maximum efficacy. 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile 59-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 23278456-11 2013 In summary, the mechanism of action of NS9283 bears high resemblance to that of benzodiazepines at the GABAA receptor and to our knowledge, NS9283 constitutes the first nAChR compound of this class. 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile 39-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 23278456-11 2013 In summary, the mechanism of action of NS9283 bears high resemblance to that of benzodiazepines at the GABAA receptor and to our knowledge, NS9283 constitutes the first nAChR compound of this class. 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile 140-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 26105867-12 2013 CONCLUSION: Nicotine exposure in pregnancy increases nAChR subunit mRNAs that play a role in vasoconstriction and amino acid uptake, possibly contributing to abnormalities in placentas from smoking mothers. Nicotine 12-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 23430468-8 2013 Treatment of non-transfected cells with Abeta elevated the level of malondialdehyde (MDA) and lowered the activities of SOD and GSH-Px and these changes were potentiated by inhibiting expression of alpha7 nAChR. Malondialdehyde 68-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 23430468-8 2013 Treatment of non-transfected cells with Abeta elevated the level of malondialdehyde (MDA) and lowered the activities of SOD and GSH-Px and these changes were potentiated by inhibiting expression of alpha7 nAChR. Glutathione 128-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 23641218-8 2013 In addition, ethanol potentiates distinct nAChR subtype responses to ACh and nicotine in vitro and in DAergic neurons. Ethanol 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 23641218-8 2013 In addition, ethanol potentiates distinct nAChR subtype responses to ACh and nicotine in vitro and in DAergic neurons. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 23641218-9 2013 The smoking cessation therapeutic and nAChR partial agonist, varenicline, reduces alcohol consumption in heavy drinking smokers and rodent models of alcohol consumption. Varenicline 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 23641218-9 2013 The smoking cessation therapeutic and nAChR partial agonist, varenicline, reduces alcohol consumption in heavy drinking smokers and rodent models of alcohol consumption. Alcohols 82-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 23641218-9 2013 The smoking cessation therapeutic and nAChR partial agonist, varenicline, reduces alcohol consumption in heavy drinking smokers and rodent models of alcohol consumption. Alcohols 149-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 23336579-1 2013 alpha-Conotoxin MII (alpha-CTxMII) is a potent and selective peptide antagonist of neuronal nicotinic acetylcholine receptors (nAChR"s). alpha-ctxmii 21-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 23349463-4 2013 This interaction was predicted by studies of ACh-binding proteins and confirmed by functional studies of the neuronal (CNS) nAChR, alpha4beta2. Acetylcholine 45-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 23201359-2 2013 Nicotine - a nonspecific nicotinic acetylcholine receptor (nAChR) agonist - improves vigilance in healthy subjects and schizophrenia patients as measured by continuous performance tests (CPTs), but the nAChR mediating this effect remains unclear. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-57 23201359-2 2013 Nicotine - a nonspecific nicotinic acetylcholine receptor (nAChR) agonist - improves vigilance in healthy subjects and schizophrenia patients as measured by continuous performance tests (CPTs), but the nAChR mediating this effect remains unclear. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 23201359-10 2013 The similarity of nicotine and ABT-418 effects provides support for an alpha4beta2 nAChR mechanism of action for nicotine-induced improvement in attention/vigilance. 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 31-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 23201359-10 2013 The similarity of nicotine and ABT-418 effects provides support for an alpha4beta2 nAChR mechanism of action for nicotine-induced improvement in attention/vigilance. Nicotine 113-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 23300078-2 2013 Here, we characterize propofol binding sites in a muscle-type nAChR by use of a photoreactive analog of propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm). Propofol 22-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 23352509-0 2013 Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the alpha3beta4 nicotinic acetylcholine receptor (nAChR). arylmethylene quinuclidine 57-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 23300078-2 2013 Here, we characterize propofol binding sites in a muscle-type nAChR by use of a photoreactive analog of propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm). Propofol 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 23300078-2 2013 Here, we characterize propofol binding sites in a muscle-type nAChR by use of a photoreactive analog of propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm). 2-isopropyl-5-(3-(trifluoromethyl)-3H-diazirin-3-yl)phenol 114-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 23300078-2 2013 Here, we characterize propofol binding sites in a muscle-type nAChR by use of a photoreactive analog of propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm). azipm 174-179 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 23300078-3 2013 Based upon radioligand binding assays, AziPm stabilized the Torpedo nAChR in the resting state, whereas propofol stabilized the desensitized state. azipm 39-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 23300078-4 2013 nAChR-rich membranes were photolabeled with [(3)H]AziPm, and labeled amino acids were identified by Edman degradation. [(3)h]azipm 44-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 23300078-8 2013 These results identify for the first time a single intrasubunit propofol binding site in the nAChR transmembrane domain and suggest that this is the functionally relevant inhibitory binding site. Propofol 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 23037950-0 2013 Possible association of nicotinic acetylcholine receptor gene (CHRNA4 and CHRNB2) polymorphisms with nicotine dependence in Japanese males: an exploratory study. Nicotine 101-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-69 22751493-2 2013 This nicotine addiction is mediated through the nicotinic acetylcholine receptor (nAChR), expressed on most neurons, and also many other organs in the body. Nicotine 5-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 22751493-2 2013 This nicotine addiction is mediated through the nicotinic acetylcholine receptor (nAChR), expressed on most neurons, and also many other organs in the body. Nicotine 5-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. Codeine 33-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. Codeine 33-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. eseroline 45-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. eseroline 45-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. Galantamine 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 22931533-3 2013 The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development. Galantamine 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22750421-10 2013 These results demonstrate that nicotine and endogenous ACh enhance the excitatory and inhibitory synaptic inputs of IA-AVPNs and cause a postsynaptic excitatory current and that the nicotinic effects are mediated presynaptically by activation of the alpha4beta2 type of nAChR and postsynaptically by activation of multiple nAChRs, including alpha7 and alpha4beta2 types. Nicotine 31-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 270-275 23418390-3 2013 Using pharmacological and behavioral tools, we found that alpha7-nAChR-mediated cholinergic interactions between the pedunculopontine tegmental nucleus and the medial prefrontal cortex modulate the duration of fear-motivated memories, maybe by regulating the activation state of VTA-hippocampus dopamine connections. Dopamine 295-303 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Varenicline 110-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Varenicline 110-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 23710919-1 2013 OBJECTIVE: To investigate the effects of alpha3 neuronal nicotinic acetylcholine receptor (nAChR) on apoptosis and p38 signal transduction pathway in SH-SY5Y cells and to assess the roles of alpha3 nAChR in the pathogenesis of Alzheimer"s disease (AD). Acetylcholine 67-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 23086458-3 2013 In the current study, molecular docking, molecular dynamics simulations and binding energy calculations were performed to theoretically investigate the interactions between the partial agonists, 4-OH-DMXBA and tropisetron with alpha7-nAChR. 4-oh-dmxba 195-205 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 234-239 23086458-3 2013 In the current study, molecular docking, molecular dynamics simulations and binding energy calculations were performed to theoretically investigate the interactions between the partial agonists, 4-OH-DMXBA and tropisetron with alpha7-nAChR. Tropisetron 210-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 234-239 23086458-4 2013 The results suggest that the partial agonists 4-OH-DMXBA and tropisetron bind with alpha7-nAChR in a binding mode similar to that with AChBP. 4-oh-dmxba 46-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 23086458-4 2013 The results suggest that the partial agonists 4-OH-DMXBA and tropisetron bind with alpha7-nAChR in a binding mode similar to that with AChBP. Tropisetron 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 23086458-6 2013 Energy calculation and decomposition using MM-GB/SA suggests that the van der Waals term (DeltaE(VDW)) is the main driving force for the binding of the partial agonists to alpha7-nAChR. 2-chloro-10-(4'(N-beta-hydroxyethyl)piperazinyl-1')acetylphenothiazine 49-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 22291029-11 2013 In LV and LVI, nAChR-induced activation of inhibitory and excitatory neurons results in a net augmentation of output neuron activity. lvi 10-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 22750421-10 2013 These results demonstrate that nicotine and endogenous ACh enhance the excitatory and inhibitory synaptic inputs of IA-AVPNs and cause a postsynaptic excitatory current and that the nicotinic effects are mediated presynaptically by activation of the alpha4beta2 type of nAChR and postsynaptically by activation of multiple nAChRs, including alpha7 and alpha4beta2 types. Acetylcholine 55-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 270-275 23086230-1 2013 Coniine is an optically active toxic piperidine alkaloid and nicotinic acetylcholine receptor (nAChR) agonist found in poison hemlock (Conium maculatum L.). coniine 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 23042213-4 2013 The alpha7 nAChR agonists varenicline and JN403, but not the alpha4beta2 nAChR agonist cytisine, increased the 3H-PIB binding in autopsy tissue homogenates from AD and control frontal cortex. Varenicline 26-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 23042213-4 2013 The alpha7 nAChR agonists varenicline and JN403, but not the alpha4beta2 nAChR agonist cytisine, increased the 3H-PIB binding in autopsy tissue homogenates from AD and control frontal cortex. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 42-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 23042213-4 2013 The alpha7 nAChR agonists varenicline and JN403, but not the alpha4beta2 nAChR agonist cytisine, increased the 3H-PIB binding in autopsy tissue homogenates from AD and control frontal cortex. Tritium 111-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 23042213-5 2013 This effect was blocked in the presence of the alpha7 nAChR antagonists methyllycaconitine, alpha-bungarotoxin, and mecamylamine, but not by the alpha4beta2 nAChR antagonist dihydro-beta-erythroidine. methyllycaconitine 72-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 23042213-5 2013 This effect was blocked in the presence of the alpha7 nAChR antagonists methyllycaconitine, alpha-bungarotoxin, and mecamylamine, but not by the alpha4beta2 nAChR antagonist dihydro-beta-erythroidine. Mecamylamine 116-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 23086230-9 2013 These results provide pharmacological evidence that the piperidine alkaloid coniine is acting at fetal muscle-type nAChR in a concentration-dependent manner. piperidine alkaloid 56-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 23086230-9 2013 These results provide pharmacological evidence that the piperidine alkaloid coniine is acting at fetal muscle-type nAChR in a concentration-dependent manner. coniine 76-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 23010362-1 2013 The interaction of the selective norepinephrine reuptake inhibitor (-)-reboxetine with the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) in different conformational states was studied by several functional and structural approaches. Norepinephrine 33-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 23010362-1 2013 The interaction of the selective norepinephrine reuptake inhibitor (-)-reboxetine with the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) in different conformational states was studied by several functional and structural approaches. Reboxetine 67-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 23468647-6 2013 acr-7 knockout and nAChR antagonists suppress clozapine-induced inhibition of pharyngeal pumping. Clozapine 46-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 23010362-3 2013 Consistently, the results from the electrophysiology-based functional approach suggest that (-)-reboxetine may act via open channel block; therefore, it is capable of producing a use-dependent type of inhibition of the halpha4beta2 nAChR function. Reboxetine 92-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 232-237 23010362-5 2013 The results indicate that, although (-)-reboxetine binds with low affinity to this site, it discriminates between the resting and desensitized halpha4beta2 nAChR ion channels. Reboxetine 36-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 23010362-6 2013 Patch-clamp results also indicate that (-)-reboxetine progressively inhibits the halpha4beta2 nAChR with two-fold higher potency at the end of one-second application of agonist, compared with the peak current. Reboxetine 39-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 22796110-3 2013 Here we discuss the role of the cortical cholinergic system in mediating cue detection and attentional control and propose two target mechanisms for cognition enhancers: stimulation of prefrontal alpha4beta2* nicotinic acetylcholine receptors (nAChR) for the enhancement of cue detection and augmentation of tonic acetylcholine levels for the enhancement of attentional control. Acetylcholine 219-232 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 244-249 23468647-4 2013 nAChR agonists phenocopy the developmental effects of clozapine, while nAChR antagonists partially block these effects. Clozapine 54-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 23201341-5 2013 In contrast, when untransfected SH-SY5Y cells were exposed to nicotine, the levels of both alpha3 nAChR mRNA and protein were enhanced; while the levels of BACE1 mRNA and protein were diminished and the corresponding levels of BACE2 enhanced; and the level of Abeta in the culture medium was attenuated. Nicotine 62-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 23966848-2 2013 Recent data have led to a debate about the principal pathway of nicotine action: direct stimulation of the DAergic cells through nAChR activation, or disinhibition mediated through desensitization of nAChRs on GABAergic interneurons. Nicotine 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 23468647-9 2013 alpha-like nAChR signaling is a mechanism through which clozapine may produce its therapeutic and/or toxic effects in humans, a hypothesis that could be tested following identification of the mammalian ortholog of C. elegans acr-7. Clozapine 56-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 23149874-7 2012 Nicotinic acetylcholine receptor (nAChR) blocker hexamethonium, MEK1/2 inhibitor PD98059, p38 MAPK inhibitor SB203580 and NF-kappaB inhibitor PDTC almost completely abolished nicotineinduced CRP expression in mRNA and protein levels in U937 macrophages. Hexamethonium 49-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 22902499-5 2012 KEY FINDINGS: Both nAChR and mAChR antagonists (hexamethonium and methacine, respectively), per se, elevated histamine-releasing activity of the HMC-1 and suppressed the MC responses to most of investigated activators (carbachol, compound 48/80, and to a lesser extent aIgG). Hexamethonium 48-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 22902499-5 2012 KEY FINDINGS: Both nAChR and mAChR antagonists (hexamethonium and methacine, respectively), per se, elevated histamine-releasing activity of the HMC-1 and suppressed the MC responses to most of investigated activators (carbachol, compound 48/80, and to a lesser extent aIgG). methacine 66-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 22902499-5 2012 KEY FINDINGS: Both nAChR and mAChR antagonists (hexamethonium and methacine, respectively), per se, elevated histamine-releasing activity of the HMC-1 and suppressed the MC responses to most of investigated activators (carbachol, compound 48/80, and to a lesser extent aIgG). Carbachol 219-228 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 22902499-5 2012 KEY FINDINGS: Both nAChR and mAChR antagonists (hexamethonium and methacine, respectively), per se, elevated histamine-releasing activity of the HMC-1 and suppressed the MC responses to most of investigated activators (carbachol, compound 48/80, and to a lesser extent aIgG). aigg 269-273 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 23149874-7 2012 Nicotinic acetylcholine receptor (nAChR) blocker hexamethonium, MEK1/2 inhibitor PD98059, p38 MAPK inhibitor SB203580 and NF-kappaB inhibitor PDTC almost completely abolished nicotineinduced CRP expression in mRNA and protein levels in U937 macrophages. Hexamethonium 49-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23149874-7 2012 Nicotinic acetylcholine receptor (nAChR) blocker hexamethonium, MEK1/2 inhibitor PD98059, p38 MAPK inhibitor SB203580 and NF-kappaB inhibitor PDTC almost completely abolished nicotineinduced CRP expression in mRNA and protein levels in U937 macrophages. nicotineinduced 175-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 22544838-7 2012 Progress has been made using knockout mouse models, highlighting the importance of alpha5 nAChR subunits in regulating nicotine intake, particularly those localized to the habenula-interpeduncular nucleus pathway. Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 23149874-7 2012 Nicotinic acetylcholine receptor (nAChR) blocker hexamethonium, MEK1/2 inhibitor PD98059, p38 MAPK inhibitor SB203580 and NF-kappaB inhibitor PDTC almost completely abolished nicotineinduced CRP expression in mRNA and protein levels in U937 macrophages. nicotineinduced 175-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 23149874-9 2012 These demonstrate that nicotine has ability to induce CRP expression in macrophages through nAChR-ERK1/2/p38 MAPK-NF-kappaB signal pathway, which contributes to better understanding of the pro-inflammatory and pro-atherosclerotic effects of nicotine in cigarette smokers. Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 23149874-9 2012 These demonstrate that nicotine has ability to induce CRP expression in macrophages through nAChR-ERK1/2/p38 MAPK-NF-kappaB signal pathway, which contributes to better understanding of the pro-inflammatory and pro-atherosclerotic effects of nicotine in cigarette smokers. Nicotine 241-249 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 22990212-2 2012 The regulation of feeding and metabolism by nicotine is complex, and recent studies have begun to identify nicotinic acetylcholine receptor (nAChR) subtypes and circuits or cell types involved in this regulation. Nicotine 44-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-139 22923641-6 2012 Treatment of primary cultures of BEC with nicotine increased levels of nAChR subunits and that increase was potentiated by lynx1 knockdown. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 22990212-2 2012 The regulation of feeding and metabolism by nicotine is complex, and recent studies have begun to identify nicotinic acetylcholine receptor (nAChR) subtypes and circuits or cell types involved in this regulation. Nicotine 44-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 22990212-4 2012 Then, we will describe the nAChR subtypes expressed in these structures in mammals to identify the possible molecular targets for nicotine. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 23060793-1 2012 BACKGROUND: The procognitive actions of the nicotinic acetylcholine receptor (nAChR) agonist nicotine are believed, in part, to motivate the excessive cigarette smoking in schizophrenia, a disorder associated with deficits in multiple cognitive domains, including low-level auditory sensory processes and higher-order attention-dependent operations. Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-76 22804734-1 2012 Long-term treatment with nicotine or selective alpha7 nicotinic acetylcholine receptor (nAChR) agonists increases the number of alpha7 nAChRs and this up-regulation may be involved in the mechanism underlying the sustained procognitive effect of these compounds. Nicotine 25-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 22804734-3 2012 We show that the type II PAMs, PNU-120596 (10 muM) or TQS (1 and 10 muM), inhibit up-regulation, as measured by protein levels, induced by the alpha7 nAChR agonist A-582941 (10 nM or 10 muM), in SH-EP1 cells stably expressing human alpha7 nAChR, whereas the type I PAMs AVL-3288 or NS1738 do not. N-neopentyl-N-nitrosourea 31-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 22804734-3 2012 We show that the type II PAMs, PNU-120596 (10 muM) or TQS (1 and 10 muM), inhibit up-regulation, as measured by protein levels, induced by the alpha7 nAChR agonist A-582941 (10 nM or 10 muM), in SH-EP1 cells stably expressing human alpha7 nAChR, whereas the type I PAMs AVL-3288 or NS1738 do not. N-neopentyl-N-nitrosourea 31-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 239-244 22804734-3 2012 We show that the type II PAMs, PNU-120596 (10 muM) or TQS (1 and 10 muM), inhibit up-regulation, as measured by protein levels, induced by the alpha7 nAChR agonist A-582941 (10 nM or 10 muM), in SH-EP1 cells stably expressing human alpha7 nAChR, whereas the type I PAMs AVL-3288 or NS1738 do not. N-(6-methoxy-8-quinolyl)-4-toluenesulfonamide 54-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 22804734-3 2012 We show that the type II PAMs, PNU-120596 (10 muM) or TQS (1 and 10 muM), inhibit up-regulation, as measured by protein levels, induced by the alpha7 nAChR agonist A-582941 (10 nM or 10 muM), in SH-EP1 cells stably expressing human alpha7 nAChR, whereas the type I PAMs AVL-3288 or NS1738 do not. N-(6-methoxy-8-quinolyl)-4-toluenesulfonamide 54-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 239-244 22804734-5 2012 We further show in vivo that 3 mg/kg PNU-120596 inhibits up-regulation of the alpha7 nAChR induced by 10 mg/kg A-582941, as measured by [(125)I]-bungarotoxin autoradiography, whereas 1 mg/kg AVL-3288 does not. N-neopentyl-N-nitrosourea 37-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 22804734-8 2012 Furthermore, our data suggest that nicotine and A-582941 induce up-regulation through different mechanisms, and that this confers differential sensitivity to the effects of alpha7 nAChR PAMs. Nicotine 35-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 22804734-8 2012 Furthermore, our data suggest that nicotine and A-582941 induce up-regulation through different mechanisms, and that this confers differential sensitivity to the effects of alpha7 nAChR PAMs. A-582941 48-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 22547331-1 2012 RATIONALE: Emerging evidence suggests that the alpha4beta2 form of the nicotinic acetylcholine receptor (nAChR) modulates the rewarding effects of alcohol. Alcohols 147-154 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-103 22547331-1 2012 RATIONALE: Emerging evidence suggests that the alpha4beta2 form of the nicotinic acetylcholine receptor (nAChR) modulates the rewarding effects of alcohol. Alcohols 147-154 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 22547331-2 2012 The nAChR alpha4beta2 subunit partial agonist varenicline (Chantix ), which is approved by the Food and Drug Administration for smoking cessation, also decreases ethanol consumption in rodents (Steensland et al., Proc Natl Acad Sci U S A 104:12518-12523, 2007) and in human laboratory and open-label studies (Fucito et al., Psychopharmacology (Berl) 215:655-663, 2011; McKee et al., Biol Psychiatry 66:185-190 2009). Varenicline 46-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 22547331-2 2012 The nAChR alpha4beta2 subunit partial agonist varenicline (Chantix ), which is approved by the Food and Drug Administration for smoking cessation, also decreases ethanol consumption in rodents (Steensland et al., Proc Natl Acad Sci U S A 104:12518-12523, 2007) and in human laboratory and open-label studies (Fucito et al., Psychopharmacology (Berl) 215:655-663, 2011; McKee et al., Biol Psychiatry 66:185-190 2009). Varenicline 59-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 22547331-2 2012 The nAChR alpha4beta2 subunit partial agonist varenicline (Chantix ), which is approved by the Food and Drug Administration for smoking cessation, also decreases ethanol consumption in rodents (Steensland et al., Proc Natl Acad Sci U S A 104:12518-12523, 2007) and in human laboratory and open-label studies (Fucito et al., Psychopharmacology (Berl) 215:655-663, 2011; McKee et al., Biol Psychiatry 66:185-190 2009). Ethanol 162-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 22928944-2 2012 In this study, a cocrystal structure of the acetylcholine binding protein (AChBP) from Capitella teleta (Ct) in complex with a cyclopropane-containing selective alpha4beta2-nicotinic acetylcholine receptor (nAChR) partial agonist (compound 5) was acquired. cyclopropane 127-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 207-212 23060793-1 2012 BACKGROUND: The procognitive actions of the nicotinic acetylcholine receptor (nAChR) agonist nicotine are believed, in part, to motivate the excessive cigarette smoking in schizophrenia, a disorder associated with deficits in multiple cognitive domains, including low-level auditory sensory processes and higher-order attention-dependent operations. Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 22952075-2 2012 The authors examined multiple dosages of tropisetron, a partial agonist at the nAChR, for short-term effects on cognition and P50 deficits in schizophrenia. Tropisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 22613724-6 2012 Azemiopsin efficiently competed with alpha-bungarotoxin for binding to Torpedo nicotinic acetylcholine receptor (nAChR) (IC(50) 0.18 +- 0.03 mum) and with lower efficiency to human alpha7 nAChR (IC(50) 22 +- 2 mum). azemiopsin 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-111 22791813-7 2012 Using the PDAC cell lines BxPC-3 and Panc-1 and immortalized pancreatic duct epithelial cell line HPDE6-C7, our current experiments reveal a significant sensitization of the nAChR-driven autocrine catecholamine regulatory loop in cells pre-exposed to nicotine for 7 days. Catecholamines 197-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 22791813-7 2012 Using the PDAC cell lines BxPC-3 and Panc-1 and immortalized pancreatic duct epithelial cell line HPDE6-C7, our current experiments reveal a significant sensitization of the nAChR-driven autocrine catecholamine regulatory loop in cells pre-exposed to nicotine for 7 days. Nicotine 251-259 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 22791813-8 2012 The resulting increase in catecholamine production was associated with significant inductions in the phosphorylation of signaling proteins ERK, CREB, Src and AKT, upregulated protein expression of nAChR subunits alpha3, alpha4, alpha5 and alpha7 and increased responsiveness to nicotine in 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl tetrazolium bromide and cell migration assays. Catecholamines 26-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 22851633-1 2012 UNLABELLED: The PET radioligand 2-fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ((18)F-nifene) is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonist developed to provide accelerated in vivo equilibrium compared with existing alpha4beta2* radioligands. 2-fluoro-3-[2-((s)-3-pyrrolinyl)methoxy]pyridine 32-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-147 22851633-1 2012 UNLABELLED: The PET radioligand 2-fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ((18)F-nifene) is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonist developed to provide accelerated in vivo equilibrium compared with existing alpha4beta2* radioligands. 2-fluoro-3-[2-((s)-3-pyrrolinyl)methoxy]pyridine 32-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 22851633-1 2012 UNLABELLED: The PET radioligand 2-fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ((18)F-nifene) is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonist developed to provide accelerated in vivo equilibrium compared with existing alpha4beta2* radioligands. nifene 88-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-147 22851633-1 2012 UNLABELLED: The PET radioligand 2-fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ((18)F-nifene) is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) agonist developed to provide accelerated in vivo equilibrium compared with existing alpha4beta2* radioligands. nifene 88-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 22851633-9 2012 RESULTS: The rapid uptake and binding of (18)F-nifene in nAChR-rich regions of the brain was appropriately modeled using the 1TCM. f-nifene 45-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 22673050-2 2012 In the present study, a series of PTZ derivatives 1-11 were investigated on the inhibition of the cloned alpha7 subunit of the human nicotinic acetylcholine receptor (alpha7-nAChR) expressed in Xenopus oocytes by using the two-electrode voltage-clamp technique. phenothiazine 34-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 22613724-6 2012 Azemiopsin efficiently competed with alpha-bungarotoxin for binding to Torpedo nicotinic acetylcholine receptor (nAChR) (IC(50) 0.18 +- 0.03 mum) and with lower efficiency to human alpha7 nAChR (IC(50) 22 +- 2 mum). azemiopsin 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 22613724-6 2012 Azemiopsin efficiently competed with alpha-bungarotoxin for binding to Torpedo nicotinic acetylcholine receptor (nAChR) (IC(50) 0.18 +- 0.03 mum) and with lower efficiency to human alpha7 nAChR (IC(50) 22 +- 2 mum). azemiopsin 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 22613724-7 2012 It dose-dependently blocked acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR and was more potent against the adult form (alpha1beta1epsilondelta) than the fetal form (alpha1beta1gammadelta), EC(50) being 0.44 +- 0.1 mum and 1.56 +- 0.37 mum, respectively. Acetylcholine 28-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 22613724-9 2012 Ala scanning showed that amino acid residues at positions 3-6, 8-11, and 13-14 are essential for binding to Torpedo nAChR. Alanine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-121 22876217-7 2012 We will characterize both ethanol and nicotine"s effects on nAChR-mediated synaptic transmission and plasticity in several key brain areas that are important for addiction. Ethanol 26-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 22580045-7 2012 The ganglionic blocker mecamylamine was most potent for blocking alpha3beta4 receptors, least potent for alpha7, and roughly equipotent for the muscle receptors and the beta2-containing nAChR. Mecamylamine 23-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 22876217-7 2012 We will characterize both ethanol and nicotine"s effects on nAChR-mediated synaptic transmission and plasticity in several key brain areas that are important for addiction. Nicotine 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 22580045-9 2012 Three prototypical alpha7-selective agonists, choline, tropane, and 4OH-GTS-21, were tested, and these agents were observed to activate both fish alpha7 and alpha4beta2 nAChR. Choline 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 22580045-9 2012 Three prototypical alpha7-selective agonists, choline, tropane, and 4OH-GTS-21, were tested, and these agents were observed to activate both fish alpha7 and alpha4beta2 nAChR. Tropanes 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 22580045-9 2012 Three prototypical alpha7-selective agonists, choline, tropane, and 4OH-GTS-21, were tested, and these agents were observed to activate both fish alpha7 and alpha4beta2 nAChR. Estetrol 68-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 22627701-1 2012 The 3-methylmaleimide congeners of the natural product methyllycaconitine (MLA) and an analogue covalently attach to functional cysteine mutants of the alpha7 nicotinic acetylcholine receptor (nAChR). 3-methylmaleimide 4-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22665477-6 2012 alpha5 subunit incorporation into alpha3beta4* nAChR also alters the relative efficacies of competitive agonists and changes the potency of the non-competitive antagonist mecamylamine. Mecamylamine 171-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 22574675-4 2012 Evidence suggests that the effects of nAChR partial agonists and antagonists have promise for the management of alcohol dependence and other alcohol use disorders. Alcohols 112-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 22574675-8 2012 Future research indicating the ability of nAChR based compounds to reduce alcohol consumption or modulate alcohol drinking behavior in preclinical and clinical studies, are also discussed. Alcohols 74-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 22742586-0 2012 Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidine analogues of 2"-fluoro-3"-(4-nitrophenyl)deschloroepibatidine. 2"-fluoro-3"-(substituted phenyl)deschloroepibatidine 98-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 22742586-0 2012 Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidine analogues of 2"-fluoro-3"-(4-nitrophenyl)deschloroepibatidine. 2-fluoro-3-(4-nitrophenyl)deschloroepibatidine 165-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 22742586-1 2012 Herein, we report the synthesis and nicotinic acetylcholine receptor (nAChR) in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 5b-g, analogues of 3"-(4-nitrophenyl) compound 5a. 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 128-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-68 22742586-1 2012 Herein, we report the synthesis and nicotinic acetylcholine receptor (nAChR) in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 5b-g, analogues of 3"-(4-nitrophenyl) compound 5a. 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 128-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 22742586-1 2012 Herein, we report the synthesis and nicotinic acetylcholine receptor (nAChR) in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 5b-g, analogues of 3"-(4-nitrophenyl) compound 5a. 3"-(4-nitrophenyl) compound 202-229 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-68 22742586-1 2012 Herein, we report the synthesis and nicotinic acetylcholine receptor (nAChR) in vitro and in vivo pharmacological properties of 2"-fluoro-3"-(substituted phenyl)deschloroepibatidines 5b-g, analogues of 3"-(4-nitrophenyl) compound 5a. 3"-(4-nitrophenyl) compound 202-229 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 22716019-2 2012 Previous studies have established that unnatural amino acid mutagenesis can probe three key binding interactions at the nAChR: a cation-pi interaction, and two hydrogen-bonding interactions to the protein backbone of the receptor. Hydrogen 160-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 22627701-1 2012 The 3-methylmaleimide congeners of the natural product methyllycaconitine (MLA) and an analogue covalently attach to functional cysteine mutants of the alpha7 nicotinic acetylcholine receptor (nAChR). methyllycaconitine 55-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22627701-1 2012 The 3-methylmaleimide congeners of the natural product methyllycaconitine (MLA) and an analogue covalently attach to functional cysteine mutants of the alpha7 nicotinic acetylcholine receptor (nAChR). Cysteine 128-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 22593584-0 2012 A highly conserved cytoplasmic cysteine residue in the alpha4 nicotinic acetylcholine receptor is palmitoylated and regulates protein expression. Cysteine 31-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-94 22593584-5 2012 When this cysteine is mutated to a serine, producing a depalmitoylated alpha4 nAChR, total protein expression decreases, but surface expression increases compared with wild-type alpha4 levels, as determined by Western blotting and enzyme-linked immunoassays, respectively. Cysteine 10-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 22593584-1 2012 Nicotinic acetylcholine receptor (nAChR) cell surface expression levels are modulated during nicotine dependence and multiple disorders of the nervous system, but the mechanisms underlying nAChR trafficking remain unclear. Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 22593584-5 2012 When this cysteine is mutated to a serine, producing a depalmitoylated alpha4 nAChR, total protein expression decreases, but surface expression increases compared with wild-type alpha4 levels, as determined by Western blotting and enzyme-linked immunoassays, respectively. Serine 35-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 22593584-9 2012 Thus, our results identify a novel palmitoylation site on cysteine 273 in the M1-M2 loop of the alpha4 nAChR and determine that cysteines in both intracellular loops are regulatory factors in total and cell surface protein expression of the alpha4beta2 nAChR. Cysteine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 22593584-1 2012 Nicotinic acetylcholine receptor (nAChR) cell surface expression levels are modulated during nicotine dependence and multiple disorders of the nervous system, but the mechanisms underlying nAChR trafficking remain unclear. Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 22593584-9 2012 Thus, our results identify a novel palmitoylation site on cysteine 273 in the M1-M2 loop of the alpha4 nAChR and determine that cysteines in both intracellular loops are regulatory factors in total and cell surface protein expression of the alpha4beta2 nAChR. Cysteine 128-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 253-258 22506649-3 2012 Bis-quaternary amines proved to have a strong affinity for all nAChR epitopes and negatively charged phospholipids, even in the presence of the physiological neurotransmitter acetylcholine. bis-quaternary amines 0-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 22556416-7 2012 Interestingly, the PNU-120596 agonist co-application data revealed that for wild-type alpha7 nAChR, the 3-furan desensitized state was relatively stabilized compared with that of 2-furan, a reversal of the relationship observed with respect to the barrier for entry into the desensitized state. N-neopentyl-N-nitrosourea 19-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 22556416-7 2012 Interestingly, the PNU-120596 agonist co-application data revealed that for wild-type alpha7 nAChR, the 3-furan desensitized state was relatively stabilized compared with that of 2-furan, a reversal of the relationship observed with respect to the barrier for entry into the desensitized state. 3-furan 104-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 22556416-8 2012 These data highlight the importance of hydrogen bonding on the receptor-ligand state, and suggest that it may be possible to fine-tune features of agonists that mediate state selection in the nAChR. Hydrogen 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 22631603-1 2012 Neonicotinoid insecticides target nicotinic acetylcholine receptors (nAChR) in the nervous system of insects but are largely ineffective against ticks. Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-67 22631603-1 2012 Neonicotinoid insecticides target nicotinic acetylcholine receptors (nAChR) in the nervous system of insects but are largely ineffective against ticks. Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 22631603-5 2012 To test this, we sequenced nAChR genes from five tick species and found that instead of the conserved arginine found in insects, a glutamine was present in all the tick sequences. Glutamine 131-140 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 22421703-7 2012 We conclude that LMA 10203 could be used as an interesting compound to identify specific insect nAChR subtypes. LMA 10203 17-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 22286500-3 2012 Using whole-cell patch-clamp electrophysiology adapted for dissociated cockroach dorsal unpaired median (DUM) neurons, we demonstrated that intracellular factors involved in the regulation of nAChR function modulated neonicotinoid sensitivity. Neonicotinoids 217-230 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 22300022-3 2012 The alpha7-nAChR subunit forms homo-oligodimeric nAChR with unique distinctive properties, such as high permeability to calcium and modulation by the extracellular calcium concentrations, the possibility of binding two-five molecules of agonist, function modulation via phosphorylation and/or via calcium-dependent serine/threonine kinases and modulating transmitter release and activation of GABAergic interneurons. Calcium 120-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 22300022-3 2012 The alpha7-nAChR subunit forms homo-oligodimeric nAChR with unique distinctive properties, such as high permeability to calcium and modulation by the extracellular calcium concentrations, the possibility of binding two-five molecules of agonist, function modulation via phosphorylation and/or via calcium-dependent serine/threonine kinases and modulating transmitter release and activation of GABAergic interneurons. Calcium 120-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 22300022-3 2012 The alpha7-nAChR subunit forms homo-oligodimeric nAChR with unique distinctive properties, such as high permeability to calcium and modulation by the extracellular calcium concentrations, the possibility of binding two-five molecules of agonist, function modulation via phosphorylation and/or via calcium-dependent serine/threonine kinases and modulating transmitter release and activation of GABAergic interneurons. Calcium 164-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 22300022-3 2012 The alpha7-nAChR subunit forms homo-oligodimeric nAChR with unique distinctive properties, such as high permeability to calcium and modulation by the extracellular calcium concentrations, the possibility of binding two-five molecules of agonist, function modulation via phosphorylation and/or via calcium-dependent serine/threonine kinases and modulating transmitter release and activation of GABAergic interneurons. Calcium 164-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 22300028-2 2012 Several studies suggest that alpha7 nicotinic receptor (nAChR) activation represents a useful therapeutic strategy for the cognitive impairments associated with early Alzheimer"s disease as the alpha7 subtype of nicotinic acetylcholine receptors are expressed by basal forebrain cholinergic projection neurons as well as by their targets in the hippocampus. Acetylcholine 222-235 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 22300030-4 2012 Evidences of nAChR-mediated protection against neurotoxicity induced by rotenone, 6- hydroxydopamine (6-OHDA), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are briefly reviewed. Rotenone 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 22300030-4 2012 Evidences of nAChR-mediated protection against neurotoxicity induced by rotenone, 6- hydroxydopamine (6-OHDA), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are briefly reviewed. Oxidopamine 82-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 22300030-4 2012 Evidences of nAChR-mediated protection against neurotoxicity induced by rotenone, 6- hydroxydopamine (6-OHDA), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are briefly reviewed. Oxidopamine 102-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 22300030-4 2012 Evidences of nAChR-mediated protection against neurotoxicity induced by rotenone, 6- hydroxydopamine (6-OHDA), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are briefly reviewed. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 115-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 22300030-4 2012 Evidences of nAChR-mediated protection against neurotoxicity induced by rotenone, 6- hydroxydopamine (6-OHDA), and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are briefly reviewed. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 161-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 22300030-5 2012 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was blocked not only by alpha4beta2 but also by alpha7 nAChR antagonists. Rotenone 3-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 22300030-5 2012 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was blocked not only by alpha4beta2 but also by alpha7 nAChR antagonists. Oxidopamine 17-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 22349182-7 2012 The nicotine-induced Cx43 downregulation functionally impaired intercellular dye transfer, which could be prevented by mecamylamine, kappa-bungarotoxin, lobeline, and dihydro-beta-erythroidine but not alpha-bungarotoxin, indicating that the nAChR subtypes alpha4beta2 and alpha3beta2 but not alpha7 are involved in signal cascade. Nicotine 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 22349182-7 2012 The nicotine-induced Cx43 downregulation functionally impaired intercellular dye transfer, which could be prevented by mecamylamine, kappa-bungarotoxin, lobeline, and dihydro-beta-erythroidine but not alpha-bungarotoxin, indicating that the nAChR subtypes alpha4beta2 and alpha3beta2 but not alpha7 are involved in signal cascade. Dihydro-beta-Erythroidine 167-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 22349182-8 2012 RT-PCR analysis revealed that nicotine exposure resulted in the upregulation of alpha3 and beta4 and the downregulation of alpha4-nAChR, while alpha7- and beta2-nAChR-mRNA expressions remained unaltered. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 22349182-8 2012 RT-PCR analysis revealed that nicotine exposure resulted in the upregulation of alpha3 and beta4 and the downregulation of alpha4-nAChR, while alpha7- and beta2-nAChR-mRNA expressions remained unaltered. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 22395733-1 2012 The primary objective of this project was to determine the alpha4beta2(*) nicotinic acetylcholine receptor (nAChR) occupancy in human brain of a single low dose of varenicline (0.5 mg), and to explore the relationship between receptor occupancy by varenicline and tobacco withdrawal symptoms ((*)denoting other putative nAChR subunits). Varenicline 164-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-106 22395733-1 2012 The primary objective of this project was to determine the alpha4beta2(*) nicotinic acetylcholine receptor (nAChR) occupancy in human brain of a single low dose of varenicline (0.5 mg), and to explore the relationship between receptor occupancy by varenicline and tobacco withdrawal symptoms ((*)denoting other putative nAChR subunits). Varenicline 164-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 22344459-8 2012 These results suggest that KYNA levels generated from 20 muM kynurenine inhibit tonically active alpha7 nAChR-dependent GABAergic transmission to the pyramidal neurons. Kynurenine 61-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 22394239-8 2012 Instead of the in situ protein-templated azide-alkyne cycloaddition reaction occurring at a localized, sequestered enzyme active center as previously shown, we demonstrate that the in situ reaction can take place at the subunit interfaces of an oligomeric protein and can thus be used as a tool for identifying novel candidate nAChR ligands. Azides 41-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 327-332 22595161-3 2012 BACKGROUND: [(18)F]-2-Fluoro-A85380 was developed for in vivo positron emission tomography (PET) imaging of nAChR subunits in the human brain. -2-fluoro-a85380 19-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 22595161-11 2012 CONCLUSIONS: [(18)F]-2-Fluoro-A85380 can provide specific information on the nAChR distribution in human arteries. 2-fluoro-a85380 21-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 22394239-8 2012 Instead of the in situ protein-templated azide-alkyne cycloaddition reaction occurring at a localized, sequestered enzyme active center as previously shown, we demonstrate that the in situ reaction can take place at the subunit interfaces of an oligomeric protein and can thus be used as a tool for identifying novel candidate nAChR ligands. Alkynes 47-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 327-332 22155207-8 2012 These results indicate that fluoxetine via axo-axonal interaction mechanism exhibits bimodal effects on nAChR-mediated neurogenic nitrergic dilation of basilar arteries. Fluoxetine 28-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 20641434-8 2004 5-(3"-fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine (nifrolidine) is a putative and selective nAChR antagonist with nanomolar affinity. 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 0-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 20641434-8 2004 5-(3"-fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine (nifrolidine) is a putative and selective nAChR antagonist with nanomolar affinity. 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 59-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 20641434-11 2004 5-(3"-[(18)F]-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine ([(18)F]nifrolidine) is being developed as a PET agent with faster kinetics than 2-[(18)F]FA and 6-[(18)F]FA for the non-invasive study of nAChR in the brain. 5-(3"-[(18)f]-fluoropropyl)-3-(2-(s)-pyrrolidinylmethoxy)pyridine 0-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 20641434-11 2004 5-(3"-[(18)F]-Fluoropropyl)-3-(2-(S)-pyrrolidinylmethoxy)pyridine ([(18)F]nifrolidine) is being developed as a PET agent with faster kinetics than 2-[(18)F]FA and 6-[(18)F]FA for the non-invasive study of nAChR in the brain. 5-(3'-fluoropropyl)-3-(2-pyrrolidinylmethoxy)pyridine 74-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 22474108-11 2012 In women, beta(2)*-nAChR availability in the cortex and cerebellum was negatively and significantly correlated with progesterone level on the SPECT imaging day. Progesterone 116-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 22410083-0 2012 Consequences of linker length alteration of the alpha7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. 5-morpholin-4-ylpentanoic acid (4-pyridin-3-ylphenyl)amide 105-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 22410083-1 2012 A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the alpha7 nicotinic acetylcholine receptor (nAChR) subtype. 5-morpholin-4-ylpentanoic acid (4-pyridin-3-ylphenyl)amide 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 228-233 22095388-12 2012 Therefore, we concluded that alpha1, alpha5, alpha7, and beta2 nAChR subunits are highly expressed in human bronchial epithelial cells (HBE16) after nicotinic incubation and that the alpha7 subunit is involved in the nicotine-induced inhibitory effect on the production of inflammatory factors. Nicotine 217-225 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 22382680-0 2012 Nicotinic acetylcholine receptor alpha7 and beta4 subunits contribute nicotine-induced apoptosis in periodontal ligament stem cells. Nicotine 70-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 22382680-3 2012 Thus, the purpose of this study was to determine the cytotoxic effect of nicotine by means of nicotinic acetylcholine receptor (nAChR) activation in PDLSCs. Nicotine 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-126 22382680-3 2012 Thus, the purpose of this study was to determine the cytotoxic effect of nicotine by means of nicotinic acetylcholine receptor (nAChR) activation in PDLSCs. Nicotine 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 22382680-5 2012 The gene expressions of alpha7 and beta4 nAChR were increased by nicotine administration. Nicotine 65-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 22382680-10 2012 However, the apoptotic effect of nicotine was inhibited by the pretreatment of alpha-bungarotoxin, a selective alpha7 nAChR antagonist or mecamylamine, a non-selective nAChR antagonist. Nicotine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 22382680-10 2012 However, the apoptotic effect of nicotine was inhibited by the pretreatment of alpha-bungarotoxin, a selective alpha7 nAChR antagonist or mecamylamine, a non-selective nAChR antagonist. Nicotine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 22382680-10 2012 However, the apoptotic effect of nicotine was inhibited by the pretreatment of alpha-bungarotoxin, a selective alpha7 nAChR antagonist or mecamylamine, a non-selective nAChR antagonist. Mecamylamine 138-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 22382680-11 2012 Finally, increases in the subG1 phase and DNA fragmentation by nicotine was attenuated by each nAChR antagonist. Nicotine 63-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 22394379-3 2012 Based on inhibition of [(125)I]SADU-3-72 binding, SADU-3-72 binds with high affinity (IC(50) = 0.8 muM) to the Torpedo nAChR in the resting (closed channel) state and in the agonist-induced desensitized state, and bupropion binds to that site with 3-fold higher affinity in the desensitized (IC(50) = 1.2 muM) than in the resting state. Bupropion 214-223 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 22394379-8 2012 These results establish the presence of two distinct bupropion binding sites within the Torpedo nAChR transmembrane domain: a high affinity site at the middle (M2-9) of the ion channel and a second site near the extracellular end of alphaM1 within a previously described halothane (general anesthetic) binding pocket. Bupropion 53-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 22394379-8 2012 These results establish the presence of two distinct bupropion binding sites within the Torpedo nAChR transmembrane domain: a high affinity site at the middle (M2-9) of the ion channel and a second site near the extracellular end of alphaM1 within a previously described halothane (general anesthetic) binding pocket. Halothane 271-280 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 22170867-5 2012 We observe that binding of (nAChR) agonists to AChBP elicits clockwise rotation of the inner beta-sheet with respect to the outer beta-sheet, causing tilting of the cys-loop away from the five-fold axis, in a manner quite similar to that speculated for alpha-subunits of the heteromeric nAChR structure (Unwin, J Mol Biol 2005;346:967), making this motion potentially important in transmission of the gating signal to the transmembrane domain of a LGIC. achbp 47-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 22170867-5 2012 We observe that binding of (nAChR) agonists to AChBP elicits clockwise rotation of the inner beta-sheet with respect to the outer beta-sheet, causing tilting of the cys-loop away from the five-fold axis, in a manner quite similar to that speculated for alpha-subunits of the heteromeric nAChR structure (Unwin, J Mol Biol 2005;346:967), making this motion potentially important in transmission of the gating signal to the transmembrane domain of a LGIC. achbp 47-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 287-292 22170867-5 2012 We observe that binding of (nAChR) agonists to AChBP elicits clockwise rotation of the inner beta-sheet with respect to the outer beta-sheet, causing tilting of the cys-loop away from the five-fold axis, in a manner quite similar to that speculated for alpha-subunits of the heteromeric nAChR structure (Unwin, J Mol Biol 2005;346:967), making this motion potentially important in transmission of the gating signal to the transmembrane domain of a LGIC. Cysteine 165-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 22170867-5 2012 We observe that binding of (nAChR) agonists to AChBP elicits clockwise rotation of the inner beta-sheet with respect to the outer beta-sheet, causing tilting of the cys-loop away from the five-fold axis, in a manner quite similar to that speculated for alpha-subunits of the heteromeric nAChR structure (Unwin, J Mol Biol 2005;346:967), making this motion potentially important in transmission of the gating signal to the transmembrane domain of a LGIC. Cysteine 165-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 287-292 22165966-2 2012 Nicotinic acetylcholine receptor (nAChR)-mediated intracellular signaling in response to nicotine has recently been implicated in the growth regulation of NSCLC. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 22378897-5 2012 Despite depolarizing MCs directly, the net effect of nAChR activation is to suppress olfactory nerve-evoked responses in these cells via activity-dependent feedback GABAergic mechanisms. mcs 21-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 22348963-8 2012 Application of AC253, an amylin receptor antagonist, blocked the excitatory effects of not only hAmylin but also nicotine; dihydro-beta-erythroidine (DHbetaE), a nAChR antagonist, also blocked the effects of nicotine and hAmylin. ac253 15-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 22348963-8 2012 Application of AC253, an amylin receptor antagonist, blocked the excitatory effects of not only hAmylin but also nicotine; dihydro-beta-erythroidine (DHbetaE), a nAChR antagonist, also blocked the effects of nicotine and hAmylin. Dihydro-beta-Erythroidine 123-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 22165966-2 2012 Nicotinic acetylcholine receptor (nAChR)-mediated intracellular signaling in response to nicotine has recently been implicated in the growth regulation of NSCLC. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 22165966-7 2012 Our data indicate that nicotine stimulated the growth of NSCLC xenografts via modulation of nAChR upregulation and activation of cAMP signaling. Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 22165966-9 2012 Activation of critical proteins in the oncogenic pathway, including CREB, ERK, Akt, and Src, and upregulation of alpha-4 and alpha-7 subunits of nAChR provided mechanistic insight for the observed stimulatory effect of nicotine. Nicotine 219-227 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 22048466-6 2012 For varenicline, continuous abstinence (weeks 9-12) was associated with multiple nAChR subunit genes (including CHRNB2, CHRNA5, and CHRNA4) (OR=1.76; 95% CI: 1.23-2.52) (p<0.005); for bupropion, abstinence was associated with CYP2B6 (OR=1.78; 95% CI: 1.27-2.50) (p<0.001). Varenicline 4-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 22048466-6 2012 For varenicline, continuous abstinence (weeks 9-12) was associated with multiple nAChR subunit genes (including CHRNB2, CHRNA5, and CHRNA4) (OR=1.76; 95% CI: 1.23-2.52) (p<0.005); for bupropion, abstinence was associated with CYP2B6 (OR=1.78; 95% CI: 1.27-2.50) (p<0.001). Bupropion 187-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 22001448-8 2012 In a second step co-incubation was performed using the antioxidant N-acetylcysteine (NAC) and the nAChR antagonist mecamylamine. Mecamylamine 115-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 22148173-0 2012 Identification of novel alpha4beta2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity. isoxazole ether 98-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-68 22148173-0 2012 Identification of novel alpha4beta2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity. isoxazole ether 98-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 22148173-2 2012 The nicotinic acetylcholine receptor (nAChR) antagonist, mecamylamine, has been shown to be an effective add-on in patients that do not respond to selective serotonin reuptake inhibitors. Mecamylamine 57-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 22148173-2 2012 The nicotinic acetylcholine receptor (nAChR) antagonist, mecamylamine, has been shown to be an effective add-on in patients that do not respond to selective serotonin reuptake inhibitors. Mecamylamine 57-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 22148173-4 2012 In this study, a new series of nAChR ligands based on an isoxazole-ether scaffold have been designed and synthesized for binding and functional assays. Isoxazoles 57-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 22148173-4 2012 In this study, a new series of nAChR ligands based on an isoxazole-ether scaffold have been designed and synthesized for binding and functional assays. Ether 67-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 22222032-4 2012 Interestingly, the epiboxidine-related dimethylammonium iodide (+-)-17, which retained a good affinity for the alpha4beta2 nAChR (K(i)=13.30nM), tightly bound also to the alpha7 subtype (K(i)=1.60nM), thus displaying a reversal of the affinity trend among the reference and new nicotinic ligands under investigation. nicotinic 278-287 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 22222032-3 2012 The set of 3-pyridinyl derivatives (+-)-10, (+-)-11 and (+-)-12 exhibited an affinity for the alpha4beta2 nAChR subtype in the subnanomolar range (K(i) values of 0.20, 0.40 and 0.50nM, respectively) and behaved as alpha4beta2 versus alpha7 subtype selective ligands. 3-pyridinyl 11-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 22222032-4 2012 Interestingly, the epiboxidine-related dimethylammonium iodide (+-)-17, which retained a good affinity for the alpha4beta2 nAChR (K(i)=13.30nM), tightly bound also to the alpha7 subtype (K(i)=1.60nM), thus displaying a reversal of the affinity trend among the reference and new nicotinic ligands under investigation. epiboxidine 19-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 22222032-4 2012 Interestingly, the epiboxidine-related dimethylammonium iodide (+-)-17, which retained a good affinity for the alpha4beta2 nAChR (K(i)=13.30nM), tightly bound also to the alpha7 subtype (K(i)=1.60nM), thus displaying a reversal of the affinity trend among the reference and new nicotinic ligands under investigation. dimethylammonium iodide (+-)-17 39-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 22108052-2 2012 Among the many chemicals in CS is nicotine - which affects cells through nicotinic acetylcholine receptors (nAChR). Cesium 28-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 22108052-2 2012 Among the many chemicals in CS is nicotine - which affects cells through nicotinic acetylcholine receptors (nAChR). Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 22119468-5 2012 Compound (+-)-[(125)I]-3 represents the first successful example of a DAT and nAChR photoaffinity ligand based on the bupropion scaffold. Bupropion 118-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 22119468-6 2012 Such ligands are expected to assist in mapping bupropion-binding pockets within plasma membrane monoamine transporters and ligand-gated nAChR ion channels. Bupropion 47-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 22320303-4 2012 We additionally present data about the decrease of the propagation velocity of rSD waves after nicotine application and show analogical effects obtained with epibatidine, a specific nicotinic acetylcholine receptor (nAChR) agonist. epibatidine 158-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-214 22425227-6 2012 Expression of PPAR gamma and PPAR gamma-target genes was significantly inhibited by pretreatment with d-tubocurarine, antagonist of non-selective nicotinic acetylcholine receptors (nAChR). Tubocurarine 102-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-179 22425227-6 2012 Expression of PPAR gamma and PPAR gamma-target genes was significantly inhibited by pretreatment with d-tubocurarine, antagonist of non-selective nicotinic acetylcholine receptors (nAChR). Tubocurarine 102-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 22320303-4 2012 We additionally present data about the decrease of the propagation velocity of rSD waves after nicotine application and show analogical effects obtained with epibatidine, a specific nicotinic acetylcholine receptor (nAChR) agonist. epibatidine 158-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 216-221 21994270-6 2012 The response facilitation was completely or strongly blocked by atropine (At), a muscarinic ACh receptor (mAChR) antagonist, in almost all neurons (96% of cells), whereas any residual effect after At administration was fully removed by mecamylamine, a nicotinic AChR (nAChR) antagonist, suggesting a predominant role for mAChRs in this mechanism. Atropine 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-273 21917987-4 2012 The alpha6*-preferring alpha-Ctx MII mutant analogs, alpha-Ctx MII[H9A,L15A] and alpha-Ctx MII[S4A,E11A,L15A], blocked nAChR currents with an IC(50) of 217.8 and 33 nM, respectively. methylphenyl carbinol 4-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 21764527-3 2012 Genome wide association studies revealed a relationship between development of nicotine dependence and a single-nucleotide polymorphism (SNP, rs16969968) of the nicotine acetylcholine receptor (nAChR) alpha-5 subunit gene (CHRNA5). Nicotine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-192 21764527-3 2012 Genome wide association studies revealed a relationship between development of nicotine dependence and a single-nucleotide polymorphism (SNP, rs16969968) of the nicotine acetylcholine receptor (nAChR) alpha-5 subunit gene (CHRNA5). Nicotine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 22201862-5 2012 More data is needed to determine whether repetitive activation of nAChR with intermittent or acute exposure to nicotine, acute activation of nAChR, or long-lasting inactivation of nAChR secondary to chronic nicotine exposure will have a therapeutic effect and/or explain the beneficial effects of those types of drugs. Nicotine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 22013232-7 2012 Similar results were produced using RJR-2403, showing that DNE influences primarily the alpha4beta2 nAChR subtype. dne 59-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 22013232-9 2012 These data provide new evidence that chronic DNE modulates XII MN nAChR function, and suggests an explanation for the association between DNE and the incidence of central and obstructive apneas. dne 45-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 21994270-6 2012 The response facilitation was completely or strongly blocked by atropine (At), a muscarinic ACh receptor (mAChR) antagonist, in almost all neurons (96% of cells), whereas any residual effect after At administration was fully removed by mecamylamine, a nicotinic AChR (nAChR) antagonist, suggesting a predominant role for mAChRs in this mechanism. Atropine 74-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-273 22013232-5 2012 nAChR-mediated inward currents were evoked by brief pressure pulses of nicotine or the alpha4beta2 nAChR agonist RJR-2403. Nicotine 71-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 21969449-6 2012 These effects of ROS on nAChR function are due to the highly conserved Cys residues in the receptors: replacing the cysteine residues in alpha3 allow ganglionic transmission and sympathetic reflexes to function normally in diabetes. Reactive Oxygen Species 17-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 21969449-6 2012 These effects of ROS on nAChR function are due to the highly conserved Cys residues in the receptors: replacing the cysteine residues in alpha3 allow ganglionic transmission and sympathetic reflexes to function normally in diabetes. Cysteine 71-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 21969449-6 2012 These effects of ROS on nAChR function are due to the highly conserved Cys residues in the receptors: replacing the cysteine residues in alpha3 allow ganglionic transmission and sympathetic reflexes to function normally in diabetes. Cysteine 116-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 26451072-3 2012 Gamma-aminobutyric acid B receptor 2 (GABBR2), dopa decarboxylase (DDC), and cholinergic receptor nicotinic alpha 4 (CHRNA4) are three examples of genes that have previously shown strong associations with nicotine dependence. Nicotine 205-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-115 22447304-4 2012 Here, we introduce recent advances in this field and describe the role of the following nAChR-related brain mechanisms in modulating impulsive behavior: dopamine release in the ventral striatum; alpha4beta2 nAChRs in the infralimbic cortex, which is a ventral part of the medial prefrontal cortex (mPFC); and dopamine release in the mPFC. Dopamine 153-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 22447304-4 2012 Here, we introduce recent advances in this field and describe the role of the following nAChR-related brain mechanisms in modulating impulsive behavior: dopamine release in the ventral striatum; alpha4beta2 nAChRs in the infralimbic cortex, which is a ventral part of the medial prefrontal cortex (mPFC); and dopamine release in the mPFC. Dopamine 309-317 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 22441542-2 2012 Whether these effects can be contributed to the immunomodulatory effects of nicotine via nicotinic acetylcholine receptor (nAChR) activation is unclear. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 22441542-7 2012 RESULTS: Repeated nicotine exposure upregulated CHRNA7 expression on THP-I monocytes and led to an enhanced potential of alpha7 nAChR agonist GSK1345038A to reduce TNF levels. Nicotine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 22441542-7 2012 RESULTS: Repeated nicotine exposure upregulated CHRNA7 expression on THP-I monocytes and led to an enhanced potential of alpha7 nAChR agonist GSK1345038A to reduce TNF levels. gsk1345038a 142-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 26451072-3 2012 Gamma-aminobutyric acid B receptor 2 (GABBR2), dopa decarboxylase (DDC), and cholinergic receptor nicotinic alpha 4 (CHRNA4) are three examples of genes that have previously shown strong associations with nicotine dependence. Nicotine 205-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-123 22761932-4 2012 In addition, the acquisition of contextual fear conditioning in the presence of nicotine is associated with a beta2-subunit containing nAChR-dependent increase in jnk1 (mapk8) transcription in the hippocampus. Nicotine 80-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 22761932-6 2012 The acquisition of contextual fear conditioning in the presence of nicotine resulted in an increase in phosphorylated CREB (pCREB) binding to the jnk1 promoter in the hippocampus in a beta2-subunit containing nAChR dependent manner, but had no effect on CREB binding; neither fear conditioning alone nor nicotine administration alone altered transcription factor binding to the jnk1 promoter. Nicotine 67-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 21309712-2 2011 ACh/agonist evoked currents at the alpha7 nAChR are transient, and, typically, calcium flux responses are difficult to detect using conventional fluorometric assay techniques. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 22393406-8 2012 Significant excitatory Ca(2+) influxes were evoked by ACE, IMI, and nicotine at concentrations greater than 1 microM in small neurons in cerebellar cultures that expressed the mRNA of the alpha3, alpha4, and alpha7 nAChR subunits. Nicotine 68-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 215-220 22393406-11 2012 Furthermore, the effects of the neonicotinoids were significantly inhibited by the nAChR antagonists mecamylamine, alpha-bungarotoxin, and dihydro-beta-erythroidine. Neonicotinoids 32-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 22393406-11 2012 Furthermore, the effects of the neonicotinoids were significantly inhibited by the nAChR antagonists mecamylamine, alpha-bungarotoxin, and dihydro-beta-erythroidine. Mecamylamine 101-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 22393406-11 2012 Furthermore, the effects of the neonicotinoids were significantly inhibited by the nAChR antagonists mecamylamine, alpha-bungarotoxin, and dihydro-beta-erythroidine. Dihydro-beta-Erythroidine 139-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 21309712-4 2011 In this study, we demonstrate that inclusion of type II PAMs such as PNU-120596, but not type I, can enable detection of endogenous alpha7 nAChR-mediated calcium responses in human neuroblastoma (IMR-32) cells. N-neopentyl-N-nitrosourea 69-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 21309712-4 2011 In this study, we demonstrate that inclusion of type II PAMs such as PNU-120596, but not type I, can enable detection of endogenous alpha7 nAChR-mediated calcium responses in human neuroblastoma (IMR-32) cells. Calcium 154-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 21309712-5 2011 Using this approach, we characterized the pharmacological profile of nicotine, epibatidine, choline, and other nAChR agonists such as PNU-282987, SSR-180711, GTS-21, OH-GTS21, tropisetron, NS6784, and A-582941. N-neopentyl-N-nitrosourea 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 22654728-7 2011 In the present review, we summarize recent electrophysiological and pharmacological studies on the extrasynaptic and synaptic differences between insect and mammalian nAChR subtypes and we discuss on the pharmacological impact of several drugs such as neonicotinoid insecticides targeting these receptors. Neonicotinoids 252-265 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 21884762-5 2011 Nicotine and selective alpha7 nicotinic acetylcholine receptor (nAChR) agonists reduce WM impairments in patients with SP and reverse WM deficits in animals treated with NMDAR antagonists. nmdar 170-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 21889951-2 2011 Improvements in stimulus selection with the nAChR agonist nicotine have been reported but its effects on visual spatial selective attention are unclear. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 21889951-6 2011 Nicotine modulation of the ERP marker of spatial attentional selection corroborates in general the attentional effects of nAChR agonists and extends these properties to include altered selective mechanisms during visual spatial processing. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 22112852-1 2011 BACKGROUND: Along with high affinity binding of epibatidine (Kd1 10 pM) to alpha4beta2 nicotinic acetylcholine receptor (nAChR), low affinity binding of epibatidine (Kd2 1-10 nM) to an independent binding site has been reported. epibatidine 48-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 22112852-3 2011 The binding behavior of epibatidine and alpha4beta2 AChR raises a question about interpreting binding data from two independent sites with ligand depletion and nonspecific binding, both of which can affect equilibrium binding of [3H]epibatidine and alpha4beta2 nAChR. epibatidine 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 261-266 22112852-3 2011 The binding behavior of epibatidine and alpha4beta2 AChR raises a question about interpreting binding data from two independent sites with ligand depletion and nonspecific binding, both of which can affect equilibrium binding of [3H]epibatidine and alpha4beta2 nAChR. Epibatidine 229-244 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 261-266 21940627-4 2011 Nicotine markedly increased alpha4beta2 nAChR binding site density and beta2 subunit protein. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 21940627-5 2011 Carbachol, a known nAChR and muscarinic receptor agonist, up-regulated both alpha4beta2 nAChR binding sites and subunit protein 2-fold more than did nicotine. Carbachol 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21940627-5 2011 Carbachol, a known nAChR and muscarinic receptor agonist, up-regulated both alpha4beta2 nAChR binding sites and subunit protein 2-fold more than did nicotine. Carbachol 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 21940627-5 2011 Carbachol, a known nAChR and muscarinic receptor agonist, up-regulated both alpha4beta2 nAChR binding sites and subunit protein 2-fold more than did nicotine. Nicotine 149-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21962147-1 2011 A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the alpha4beta2 neuronal nicotinic acetylcholine receptor (nAChR). diazabicyclo[3.3.0]octane substituted pyridines 12-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 21962147-1 2011 A series of diazabicyclo[3.3.0]octane substituted pyridines and pyrazines was synthesized and characterized at the alpha4beta2 neuronal nicotinic acetylcholine receptor (nAChR). Pyrazines 64-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 21962147-2 2011 The compounds were designed to mimic the profile of ABT-089, high affinity binding ligand for the alpha4beta2 nAChR, with limited agonist activity. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 52-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. Asparagine 50-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. Asparagine 50-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 21873428-9 2011 These studies yield insight into assembly of functional alpha6alpha5*-nAChR and provide tools for development of alpha6*-nAChR-selective ligands that could be important in the treatment of nicotine dependence, and perhaps other neurological diseases. Nicotine 189-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. Methionine 62-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. Methionine 62-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. halpha6hbeta4 142-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21832048-7 2011 More specifically, nAChR halpha6 subunit residues Asn-143 and Met-145 are important for dominant-negative effects of nAChR hbeta3 subunits on halpha6hbeta4-nAChR function. halpha6hbeta4 142-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 21832048-8 2011 Asn-143 and additional residues in the N-terminal domain of nAChR halpha6 subunits are involved in the gain-of-function effects of nAChR hbeta3(V9"S) subunits on alpha6beta2*-nAChR function. Asparagine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 21799193-12 2011 CONCLUSION: The study highlights the fact that intake of nicotine, through agonism to nAChR, might predispose epileptic patients to lower seizure threshold and induce a state of refractoriness to the protective effects of the antiepileptic drugs, resulting in possible breakthrough seizure attacks. Nicotine 57-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 21911609-6 2011 Zoniporide, a more selective inhibitor of NHE1, reversibly inhibited alpha3beta4-, alpha7- and alpha4-containing (*) nAChRs in Xenopus oocytes and in brain slices, as well as in PS120 cells deficient in NHE1 and virally transduced with nAChRs, suggesting a generalized effect of zoniporide in most neuronal nAChR subtypes. zoniporide 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 21763685-3 2011 ABT-594, for the first time, provided clinical validation to the nAChR agonist pharmacology as a novel mechanism for treatment of pain. 5-(2-azetidinylmethoxy)-2-chloropyridine 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 21745762-3 2011 We report a patient with antibody-confirmed AAG and elevated levels of ACh binding antibodies that did not meet clinical or electrodiagnostic criteria for MG. We presume that his skeletal muscle nAChR seropositivity was a false positive, perhaps due to the cross reactivity of the patient"s ganglionic nAChR antibodies with skeletal nAChR subtypes. aag 44-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 21684266-1 2011 Although a relative newcomer to the nicotinic acetylcholine receptor (nAChR) family, substantial evidence suggests that alpha6 containing nAChRs play a key role in CNS function. alpha6 120-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-68 21575610-3 2011 In this review, we discuss models for the activation and desensitization of nAChR, and the discovery of multiple types of ligands that influence those processes in both heteromeric nAChR, such as the high-affinity nicotine receptors of the brain, and homomeric alpha7-type receptors. Nicotine 214-222 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 21763685-7 2011 NS9283 (also known as A-969933), the first oxadiazole analog, was found to selectively enhance the potency of a range of nAChR agonists at alpha4beta2, but not alpha3beta4, nAChRs. 3-(3-(pyridine-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 21684266-1 2011 Although a relative newcomer to the nicotinic acetylcholine receptor (nAChR) family, substantial evidence suggests that alpha6 containing nAChRs play a key role in CNS function. alpha6 120-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 21684266-6 2011 Converging evidence suggest that the major alpha6 containing nAChRs subtypes in the nigrostriatal and mesolimbic dopamine system are the alpha6beta2beta3 and alpha6alpha4beta2beta3 nAChR populations. Dopamine 113-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 23256274-5 2011 The activation of the nAChR causes a twisting motion of the receptor, which opens a gate allowing for the passage of sodium, potassium, and calcium cations through the cell membrane. Sodium 117-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 21684266-7 2011 They appear to have a dominant role in regulating dopamine release, with consequent effects on nAChR-modulated dopaminergic functions such as reinforcement and motor behavior. Dopamine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 21718690-3 2011 Schizophrenic patients have low levels of alpha7*nAChR, as measured by binding of the ligand [(125)I]-alpha-bungarotoxin (I-BTX). iberiotoxin 122-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-54 23256274-5 2011 The activation of the nAChR causes a twisting motion of the receptor, which opens a gate allowing for the passage of sodium, potassium, and calcium cations through the cell membrane. Potassium 125-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 23256274-5 2011 The activation of the nAChR causes a twisting motion of the receptor, which opens a gate allowing for the passage of sodium, potassium, and calcium cations through the cell membrane. Calcium 140-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 21633116-8 2011 Nicotine-exposed offspring presented nAChR upregulation during exposure in all brain regions, reduced HC-3 binding during and 11 days postexposure, and increased HC-3 binding on PN90. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 21703337-2 2011 A direct pharmacologic intervention at the nicotinic acetylcholine receptor (nAChR) was proposed as an alternative therapeutic approach and promising in vitro and in vivo results were obtained with the bispyridinium compound SAD-128. bispyridinium 202-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-75 21703337-2 2011 A direct pharmacologic intervention at the nicotinic acetylcholine receptor (nAChR) was proposed as an alternative therapeutic approach and promising in vitro and in vivo results were obtained with the bispyridinium compound SAD-128. bispyridinium 202-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 21703337-4 2011 We investigated the interaction of six of these SAD-128 analogues with the orthosteric binding site of the human alpha7 nAChR and Torpedo californica nAChR with a high-throughput assay using radioactive ligands. SAD-128 48-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 21703337-4 2011 We investigated the interaction of six of these SAD-128 analogues with the orthosteric binding site of the human alpha7 nAChR and Torpedo californica nAChR with a high-throughput assay using radioactive ligands. SAD-128 48-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21742012-1 2011 Given the cognitive-promoting properties of the nicotinic acetylcholinergic receptor (nAChR) agonist, nicotine, the increased prevalence of smoke-inhaled nicotine in schizophrenia has been interpreted as an attempt to self-correct cognitive deficits, which have been particularly pronounced in the attentional domain. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-84 21742012-1 2011 Given the cognitive-promoting properties of the nicotinic acetylcholinergic receptor (nAChR) agonist, nicotine, the increased prevalence of smoke-inhaled nicotine in schizophrenia has been interpreted as an attempt to self-correct cognitive deficits, which have been particularly pronounced in the attentional domain. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 21742012-1 2011 Given the cognitive-promoting properties of the nicotinic acetylcholinergic receptor (nAChR) agonist, nicotine, the increased prevalence of smoke-inhaled nicotine in schizophrenia has been interpreted as an attempt to self-correct cognitive deficits, which have been particularly pronounced in the attentional domain. Nicotine 154-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-84 21742012-1 2011 Given the cognitive-promoting properties of the nicotinic acetylcholinergic receptor (nAChR) agonist, nicotine, the increased prevalence of smoke-inhaled nicotine in schizophrenia has been interpreted as an attempt to self-correct cognitive deficits, which have been particularly pronounced in the attentional domain. Nicotine 154-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 21742012-2 2011 As glutamatergic abnormalities have been implicated in these attentional deficiencies, this study attempted to shed light on the separate and interactive roles of the N-methyl-d-aspartate receptor (NMDAR) and nAChR systems in the modulation of attention by investigating, in healthy volunteers, the separate and combined effects of nicotine and the NMDAR antagonist ketamine on neural and behavioural responses in a sustained attention task. Nicotine 332-340 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 21742012-2 2011 As glutamatergic abnormalities have been implicated in these attentional deficiencies, this study attempted to shed light on the separate and interactive roles of the N-methyl-d-aspartate receptor (NMDAR) and nAChR systems in the modulation of attention by investigating, in healthy volunteers, the separate and combined effects of nicotine and the NMDAR antagonist ketamine on neural and behavioural responses in a sustained attention task. Ketamine 366-374 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 21683344-1 2011 BACKGROUND: Several studies report association of alpha-4 nicotinic acetylcholine receptors (encoded by CHRNA4) with nicotine dependence (ND). Nicotine 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-110 21536968-6 2011 Main Outcome Measure Changes induced by SHS in 2-FA specific binding volume of distribution as a measure of alpha(4)beta(2)* nAChR occupancy. 4-fluoroamphetamine 48-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 21536968-10 2011 CONCLUSIONS: Nicotine from SHS exposure results in substantial brain alpha(4)beta(2)* nAChR occupancy in smokers and nonsmokers. Nicotine 13-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 20953833-1 2011 The primary aim of this study was to elucidate the role of the estrogen receptor (ER), a transcription factor involved in the nicotine- and 17beta-estradiol (E2)-mediated up-regulation of alpha9-nAChR gene expression. Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 20953833-1 2011 The primary aim of this study was to elucidate the role of the estrogen receptor (ER), a transcription factor involved in the nicotine- and 17beta-estradiol (E2)-mediated up-regulation of alpha9-nAChR gene expression. Estradiol 140-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 20953833-6 2011 In vitro promoter-binding assays demonstrated that the ER is a major transcription factor that mediates nicotine- and E2-induced up-regulation of alpha9-nAChR gene expression in MCF-7 cells. Nicotine 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 20953833-7 2011 In conclusion, our data indicate that the ER plays a central role in mediating alpha9-nAChR gene up-regulation in response to either nicotine or E2 stimulation. Nicotine 133-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 21586512-4 2011 In both cell types, silencing CHRNA5 or inhibiting receptors containing nAChR alpha5 with alpha-conotoxin MII exerted a nicotine-like effect, with increased motility and invasiveness in vitro and increasing calcium influx. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21445957-1 2011 CHRNA4, the gene that encodes the nicotinic acetylcholine receptor alpha(4) subunit, is a potential candidate gene for nicotine dependence (ND). Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-6 21498873-3 2011 As the physiological effects of nicotine are mediated by nicotinic acetylcholine receptors (nAChRs), we aimed at examining whether single nucleotide polymorphisms (SNPs) residing in nAChR subunit (CHRN) genes, other than CHRNA3/CHRNA5/CHRNB4 gene cluster previously showing association in our sample, are associated with smoking quantity or serum cotinine levels. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21498873-10 2011 CONCLUSIONS: These results provide further evidence that the gamma-delta nAChR subunit gene region is associated with cotinine levels but not with the number of CPD, illustrating the usefulness of biomarkers in genetic analyses. Cotinine 118-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 21795541-2 2011 One of the major subtypes expressed in brain, the alpha4beta2-nAChR, endogenously modulates neuronal excitability and thereby, modifies certain normal as well as nicotine-induced behaviors. Nicotine 162-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 21795541-10 2011 This is the first work to develop a dopaminergic specific deletion of a nAChR subunit and examine resulting changes in nicotine-related behaviors. Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 20554619-0 2011 The alpha7-nicotinic acetylcholine receptor and MMP-2/-9 pathway mediate the proangiogenic effect of nicotine in human retinal endothelial cells. Nicotine 101-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-43 20554619-8 2011 RESULTS: Nicotine-induced angiogenesis required nAChR function and was associated with the upregulation of MMP-2 and -9 in HRMECs. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20554619-10 2011 Treatment of HRMECs with alpha7-nAChR antagonists ablated nicotine-induced angiogenesis. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 20554619-12 2011 CONCLUSIONS: The alpha7-nAChR is vital for the proangiogenic activity of nicotine. Nicotine 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 21498509-2 2011 One such drug, [(3)H]TDBzl-etomidate (4-[3-(trifluoromethyl)-3H-diazirin-3-yl]benzyl-[(3)H]1-(1-phenylethyl)-1H-imidazole-5-carboxylate), acts as a positive allosteric potentiator of Torpedo nACh receptor (nAChR) and binds to a novel site in the transmembrane domain at the gamma-alpha subunit interface. [(3)h]tdbzl-etomidate 15-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-204 21498509-2 2011 One such drug, [(3)H]TDBzl-etomidate (4-[3-(trifluoromethyl)-3H-diazirin-3-yl]benzyl-[(3)H]1-(1-phenylethyl)-1H-imidazole-5-carboxylate), acts as a positive allosteric potentiator of Torpedo nACh receptor (nAChR) and binds to a novel site in the transmembrane domain at the gamma-alpha subunit interface. [(3)h]tdbzl-etomidate 15-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 21498509-2 2011 One such drug, [(3)H]TDBzl-etomidate (4-[3-(trifluoromethyl)-3H-diazirin-3-yl]benzyl-[(3)H]1-(1-phenylethyl)-1H-imidazole-5-carboxylate), acts as a positive allosteric potentiator of Torpedo nACh receptor (nAChR) and binds to a novel site in the transmembrane domain at the gamma-alpha subunit interface. 4-[3-(trifluoromethyl)-3h-diazirin-3-yl]benzyl-[(3)h]1-(1-phenylethyl)-1h-imidazole-5-carboxylate 38-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-204 21498509-2 2011 One such drug, [(3)H]TDBzl-etomidate (4-[3-(trifluoromethyl)-3H-diazirin-3-yl]benzyl-[(3)H]1-(1-phenylethyl)-1H-imidazole-5-carboxylate), acts as a positive allosteric potentiator of Torpedo nACh receptor (nAChR) and binds to a novel site in the transmembrane domain at the gamma-alpha subunit interface. 4-[3-(trifluoromethyl)-3h-diazirin-3-yl]benzyl-[(3)h]1-(1-phenylethyl)-1h-imidazole-5-carboxylate 38-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 21498509-4 2011 TFD-etomidate inhibited acetylcholine-induced currents with an IC(50) = 4 muM, whereas it inhibited the binding of [(3)H]phencyclidine to the Torpedo nAChR ion channel in the resting and desensitized states with IC(50) values of 2.5 and 0.7 mm, respectively. CHEMBL2392771 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21498509-4 2011 TFD-etomidate inhibited acetylcholine-induced currents with an IC(50) = 4 muM, whereas it inhibited the binding of [(3)H]phencyclidine to the Torpedo nAChR ion channel in the resting and desensitized states with IC(50) values of 2.5 and 0.7 mm, respectively. Etomidate 4-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21498509-4 2011 TFD-etomidate inhibited acetylcholine-induced currents with an IC(50) = 4 muM, whereas it inhibited the binding of [(3)H]phencyclidine to the Torpedo nAChR ion channel in the resting and desensitized states with IC(50) values of 2.5 and 0.7 mm, respectively. [(3)h]phencyclidine 115-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21498509-8 2011 These results also suggest that the gamma-alpha subunit interface is a binding site for Torpedo nAChR negative allosteric modulators (TFD-etomidate) and for positive modulators (TDBzl-etomidate). CHEMBL2392771 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 21498509-8 2011 These results also suggest that the gamma-alpha subunit interface is a binding site for Torpedo nAChR negative allosteric modulators (TFD-etomidate) and for positive modulators (TDBzl-etomidate). Etomidate 138-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 21498509-8 2011 These results also suggest that the gamma-alpha subunit interface is a binding site for Torpedo nAChR negative allosteric modulators (TFD-etomidate) and for positive modulators (TDBzl-etomidate). 4-(3-(trifluoromethyl)-3H-diazirin-3-yl)benzyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate 178-193 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 21444681-3 2011 In vitro and in vivo animal studies have shown that homopentameric nAChR inhibitors, such as methyllycaconitine and alpha-Bgtx, can attenuate nicotine-induced proliferative, angiogenic, and metastatic effects in lung, colon, and bladder cancer cells. methyllycaconitine 93-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 21444681-3 2011 In vitro and in vivo animal studies have shown that homopentameric nAChR inhibitors, such as methyllycaconitine and alpha-Bgtx, can attenuate nicotine-induced proliferative, angiogenic, and metastatic effects in lung, colon, and bladder cancer cells. alpha-bgtx 116-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 21444681-3 2011 In vitro and in vivo animal studies have shown that homopentameric nAChR inhibitors, such as methyllycaconitine and alpha-Bgtx, can attenuate nicotine-induced proliferative, angiogenic, and metastatic effects in lung, colon, and bladder cancer cells. Nicotine 142-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 21444681-6 2011 For cancer therapy, natural compounds such as garcinol and EGCG have been found to block nicotine- and estrogen-induced breast cancer cell proliferation through inhibition of the alpha9-nAChR signaling pathway. garcinol 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 21444681-6 2011 For cancer therapy, natural compounds such as garcinol and EGCG have been found to block nicotine- and estrogen-induced breast cancer cell proliferation through inhibition of the alpha9-nAChR signaling pathway. epigallocatechin gallate 59-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 21444681-6 2011 For cancer therapy, natural compounds such as garcinol and EGCG have been found to block nicotine- and estrogen-induced breast cancer cell proliferation through inhibition of the alpha9-nAChR signaling pathway. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 21330654-13 2011 NT, which did not result in either cell death or proliferation, induced beta1 nAchR, upregulated VEGF, and downregulated PEDF expression through nAChR in ARPE-19 cells. Nicotine 0-2 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 21341671-1 2011 Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-85 21368748-5 2011 Varenicline (VAR), a high-affinity partial agonist at alpha(4)beta(2) and a lower affinity full agonist at alpha(7) neuronal nAChR, injected in doses of 1-5 mg/kg/s.c. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 21368748-7 2011 This upregulation of GAD(67) was abolished by the nAChR antagonist mecamylamine. Mecamylamine 67-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 21486776-2 2011 In this work we studied, using the patch clamp technique, the functional modulation of recombinant human alpha3beta4 nAChR by the A2A adenosine receptor, co-expressed in HEK cells. Adenosine 134-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. UNII-042A8N37WH 154-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-78 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. UNII-042A8N37WH 154-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Glutamic Acid 162-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-78 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Glutamic Acid 162-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Rotenone 173-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-78 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Rotenone 173-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 187-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-78 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 187-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 206-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-78 23251750-3 2011 In this review article we present evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by beta amyloid (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 206-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 23251750-6 2011 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was also observed, and the effect was blocked not only by alpha7 but also by alpha4beta2 nAChR antagonists. Rotenone 3-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 23251750-6 2011 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was also observed, and the effect was blocked not only by alpha7 but also by alpha4beta2 nAChR antagonists. Rotenone 3-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 23251750-6 2011 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was also observed, and the effect was blocked not only by alpha7 but also by alpha4beta2 nAChR antagonists. Oxidopamine 17-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 23251750-6 2011 In rotenone- and 6-OHDA-induced PD models, nAChR-mediated neuroprotection was also observed, and the effect was blocked not only by alpha7 but also by alpha4beta2 nAChR antagonists. Oxidopamine 17-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 23251750-7 2011 We also document that nAChR stimulation blocks glutamate neurotoxicity in spinal cord motor neurons. Glutamic Acid 47-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 21397497-1 2011 A series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective alpha9alpha10 nicotinic acetylcholine receptor (nAChR) antagonists. azaaromatic 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 21397497-1 2011 A series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective alpha9alpha10 nicotinic acetylcholine receptor (nAChR) antagonists. quaternary ammonium 24-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 21341671-1 2011 Neonicotinoid agonists selectively act on the insect nicotinic acetylcholine receptor (nAChR). Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 21436053-3 2011 Previous studies have identified a series of nAChR-positive allosteric modulators (PAMs) that lack agonist activity but are able to potentiate responses to orthosteric agonists, such as acetylcholine. Acetylcholine 186-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 21436053-1 2011 Conventional nicotinic acetylcholine receptor (nAChR) agonists, such as acetylcholine, act at an extracellular "orthosteric" binding site located at the interface between two adjacent subunits. Acetylcholine 23-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 21436053-4 2011 It has been shown, for example, that TQS acts as a conventional alpha7 nAChR PAM. N-(6-methoxy-8-quinolyl)-4-toluenesulfonamide 37-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 21436053-6 2011 Whereas the alpha7 nAChR antagonist metyllycaconitine acts competitively with conventional nicotinic agonists, metyllycaconitine is a noncompetitive antagonist of 4BP-TQS. metyllycaconitine 36-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 21168537-8 2011 Furthermore, using nicotinic acetylcholine receptor antagonists blocked the majority of the nicotine effects, indicating that these changes are dependent on nAChR activation. Nicotine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 21241679-7 2011 Moreover, several GABA and ACh-related genes were predicted to be alternatively spliced in TS compared to HC including GABA receptors GABRA4 and GABRG1, the nicotinic ACh receptor CHRNA4 and cholinergic differentiation factor (CDF). gamma-Aminobutyric Acid 18-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-186 21241679-7 2011 Moreover, several GABA and ACh-related genes were predicted to be alternatively spliced in TS compared to HC including GABA receptors GABRA4 and GABRG1, the nicotinic ACh receptor CHRNA4 and cholinergic differentiation factor (CDF). Acetylcholine 27-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-186 21059985-9 2011 Reduction in nAChR antibody titer resulted in a decrease in orthostatic hypotension, an increased concentration of upright plasma norepinephrine, improvement in some sweat function, and improvement in symptoms. Norepinephrine 130-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 21319801-0 2011 Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine. 2-(substituted phenyl)-3,5,5-trimethylmorpholine 13-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-143 21319801-1 2011 Toward development of smoking cessation aids superior to bupropion (2), we describe synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues 5a-5h and their effects on inhibition of dopamine, norepinephrine, and serotonin uptake, nicotinic acetylcholine receptor (nAChR) function, acute actions of nicotine, and nicotine-conditioned place preference (CPP). 2-(substituted phenyl)-3,5,5-trimethylmorpholine 97-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 245-277 21319801-1 2011 Toward development of smoking cessation aids superior to bupropion (2), we describe synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues 5a-5h and their effects on inhibition of dopamine, norepinephrine, and serotonin uptake, nicotinic acetylcholine receptor (nAChR) function, acute actions of nicotine, and nicotine-conditioned place preference (CPP). 2-(substituted phenyl)-3,5,5-trimethylmorpholine 97-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 279-284 21319801-2 2011 Several analogues encompassing aryl substitutions, N-alkylation, and alkyl extensions of the morpholine ring 3-methyl group provided analogues more potent in vitro than (S,S)-hydroxybupropion (4a) as inhibitors of dopamine or norepinephrine uptake and antagonists of nAChR function. morpholine 93-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 267-272 21252236-4 2011 At 5-30 muM, ws-LYNX1 competed with (125)I-alpha-bungarotoxin for binding to the acetylcholine-binding proteins (AChBPs) and to Torpedo nAChR. Tungsten 13-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 21252236-7 2011 A common feature for ws-LYNX1 and LYNX1 is a decrease of nAChR sensitivity to high concentrations of acetylcholine. Acetylcholine 101-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 21252231-2 2011 The predominant nAChR subtype in the mammalian brain with a high affinity for nicotine is composed of alpha4 and beta2 subunits. Nicotine 78-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 21252231-3 2011 This nAChR subtype is responsible for addiction to nicotine and is thought to be implicated in Alzheimer and Parkinson diseases and therefore presents an important target for drug design. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 21370452-0 2011 Tea polyphenol (-)-epigallocatechin-3-gallate inhibits nicotine- and estrogen-induced alpha9-nicotinic acetylcholine receptor upregulation in human breast cancer cells. Polyphenols 4-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-125 21370452-0 2011 Tea polyphenol (-)-epigallocatechin-3-gallate inhibits nicotine- and estrogen-induced alpha9-nicotinic acetylcholine receptor upregulation in human breast cancer cells. epigallocatechin gallate 15-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-125 21370452-0 2011 Tea polyphenol (-)-epigallocatechin-3-gallate inhibits nicotine- and estrogen-induced alpha9-nicotinic acetylcholine receptor upregulation in human breast cancer cells. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-125 21370452-3 2011 Luciferase promoter activity experiment was performed to test the alpha9-nAChR promoter activity affected by Nic, E2 or EGCG. Estradiol 114-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 21370452-3 2011 Luciferase promoter activity experiment was performed to test the alpha9-nAChR promoter activity affected by Nic, E2 or EGCG. epigallocatechin gallate 120-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 21370452-4 2011 The results indicate that treatment with EGCG (1 muM) profoundly decreases Nic- and E2-induced MCF-7 proliferation by down regulating alpha9-nAChR expression. epigallocatechin gallate 41-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 21370452-5 2011 The alpha9-nAChR promoter activity is significantly induced by 24-h treatment with Nic (10 muM) or E2 (10 nM) (>1.8 and ~2.3-fold, respectively) in MCF-7 cells. Nicotine 83-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 21370452-6 2011 Pretreatment with EGCG eliminated the Nic- and E2-induced alpha9-nAChR promoter-dependent luciferase activity. epigallocatechin gallate 18-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 21370452-7 2011 We further demonstrate that combined treatment with EGCG profoundly inhibits [3H]-Nic/ alpha9-nAChR binding activity in breast cancer cells. epigallocatechin gallate 52-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 21370452-7 2011 We further demonstrate that combined treatment with EGCG profoundly inhibits [3H]-Nic/ alpha9-nAChR binding activity in breast cancer cells. Tritium 78-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 21370452-8 2011 CONCLUSIONS: We found that the EGCG could be used as an agent for blocking smoking (Nic)- or hormone (E2)-induced breast cancer cell proliferation by inhibiting of alpha9-nAChR signaling pathway. epigallocatechin gallate 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 171-176 21290632-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. Cysteine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. (2-(trimethylammonium)ethyl)methanethiosulfonate 116-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. MTSET 166-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. Acetylcholine 47-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. methyl methanethiosulfonate 243-271 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. methyl methanethiosulfonate 273-277 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21115477-1 2011 Covalent modification of alpha7 W55C nicotinic acetylcholine receptors (nAChR) with the cysteine-modifying reagent [2-(trimethylammonium)ethyl] methanethiosulfonate (MTSET(+)) produces receptors that are unresponsive to acetylcholine, whereas methyl methanethiolsulfonate (MMTS) produces enhanced acetylcholine-gated currents. Acetylcholine 220-233 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Strychnine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-176 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Strychnine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Tubocurarine 15-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-176 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Tubocurarine 15-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Tubocurarine 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-176 21468359-2 2011 Strychnine and d-tubocurarine (d-TC) are neurotoxins that have been highly instrumental in decades of research on glycine receptors (GlyR) and nicotinic acetylcholine receptors (nAChR), respectively. Tubocurarine 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. Strychnine 45-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. Tubocurarine 61-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. achbp 66-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. Alanine 95-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. Strychnine 272-282 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-7 2011 Based on the ligand interactions observed in strychnine- and d-TC-AChBP complexes we performed alanine-scanning mutagenesis in the binding pocket of the human alpha1 GlyR and alpha7 nAChR and showed the functional relevance of these residues in conferring high potency of strychnine and d-TC, respectively. Tubocurarine 287-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 21468359-8 2011 Our results demonstrate that a limited number of ligand interactions in the binding pocket together with an energetic stabilization of the extracellular domain are key to the poor selective recognition of strychnine and d-TC by CLRs as diverse as the GlyR, nAChR, and 5-HT(3)R. Strychnine 205-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 257-262 21468359-8 2011 Our results demonstrate that a limited number of ligand interactions in the binding pocket together with an energetic stabilization of the extracellular domain are key to the poor selective recognition of strychnine and d-TC by CLRs as diverse as the GlyR, nAChR, and 5-HT(3)R. Tubocurarine 220-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 257-262 21048701-3 2011 Recent human genetic association studies have implicated the gene cluster CHRNA3-CHRNA5-CHRNB4 encoding the alpha3, alpha5, and beta4 subunits of the nAChR in susceptibility to develop nicotine and alcohol dependence; however, their role in ethanol-mediated behaviors is unknown due to the lack of suitable and selective research tools. Nicotine 185-193 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21048701-3 2011 Recent human genetic association studies have implicated the gene cluster CHRNA3-CHRNA5-CHRNB4 encoding the alpha3, alpha5, and beta4 subunits of the nAChR in susceptibility to develop nicotine and alcohol dependence; however, their role in ethanol-mediated behaviors is unknown due to the lack of suitable and selective research tools. Alcohols 198-205 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21048701-3 2011 Recent human genetic association studies have implicated the gene cluster CHRNA3-CHRNA5-CHRNB4 encoding the alpha3, alpha5, and beta4 subunits of the nAChR in susceptibility to develop nicotine and alcohol dependence; however, their role in ethanol-mediated behaviors is unknown due to the lack of suitable and selective research tools. Ethanol 241-248 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 150-155 21290632-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21290632-12 2004 4-[(11)C]Methylphenyl-1,4-diazabicyclo[3.2.2]nonane-4-carboxylate ([(11)C]CHIBA-1001) has been developed as a PET agent for the non-invasive study of alpha7 nAChR in the brain (13). 4-[(11)c]methylphenyl-1,4-diazabicyclo[3.2.2]nonane-4-carboxylate 0-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 21290632-13 2004 In this chapter, another alpha7 nAChR agonist, 4-[5-(4-[(18)F]fluoro-phenyl)-[1,3,4]oxadiazol-2-yl]-1,4-diaza-bicyclo[3.2.2]nonane ([(18)F]NS10743) (14), is being evaluated for use as a PET imaging agent. 4-[5-(4-[(18)f]fluoro-phenyl)-[1,3,4]oxadiazol-2-yl]-1,4-diaza-bicyclo[3.2.2]nonane 47-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 20229177-7 2011 Furthermore, we found that Nic-induced human breast cancer (MDA-MB-231) cell proliferation was inhibited by 1 muM of garcinol (Gar), isolated from the edible fruit Garcinia indica, through down-regulation of alpha9-nAChR and cyclin D3 expression. Nicotine 27-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 215-220 21290621-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21290621-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21290621-12 2004 4-[(11)C]Methylphenyl-1,4-diazabicyclo(3.2.2)nonane-4-carboxylate ([(11)C]CHIBA-1001) has been developed as a PET agent for the noninvasive study of alpha7 nAChR in the brain (14). 4-[(11)c]methylphenyl-1,4-diazabicyclo(3.2.2)nonane-4-carboxylate 0-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 21290621-13 2004 In this chapter, another alpha7 nAChR agonist, 2-(5-[(11)C]methyl-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl)-xanthene-9-one ([(11)C]A-844606) (15), is being evaluated as a useful PET imaging agent. 2-(5-[(11)c]methyl-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl)-xanthene-9-one 47-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 21290619-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21290619-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 21290619-12 2004 4-[(11)C]Methylphenyl-1,4-diazabicyclo(3.2.2)nonane-4-carboxylate ([(11)C]CHIBA-1001) has been developed as a PET agent for the noninvasive study of alpha7 nAChR in the brain (14). 4-[(11)c]methylphenyl-1,4-diazabicyclo(3.2.2)nonane-4-carboxylate 0-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 21290619-13 2004 In this chapter, another alpha7 nAChR agonist, 2-[(11)C]methyl-5-[6-phenylpyridazine-3-yl]octahydropyrrolo[3,4-c]pyrrole ([(11)C]A-582941) (15), is being evaluated as a useful PET imaging agent. 2-[(11)c]methyl-5-[6-phenylpyridazine-3-yl]octahydropyrrolo[3,4-c]pyrrole 47-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 20229177-7 2011 Furthermore, we found that Nic-induced human breast cancer (MDA-MB-231) cell proliferation was inhibited by 1 muM of garcinol (Gar), isolated from the edible fruit Garcinia indica, through down-regulation of alpha9-nAChR and cyclin D3 expression. garcinol 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 215-220 22085699-6 2011 METHODS: Using human benign MCF10A and malignant MDA-MB-231 breast cells and specific inhibitors of possible downstream kinases, we identified nAChR effectors that were activated by treatment with nicotine. Nicotine 197-205 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 22085699-9 2011 After the ligation of nAChR with nicotine, EGFR was shown to be activated and then internalized in both MCF10A and MDA-MB-231 breast cancer cells. Nicotine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 20229177-8 2011 These results suggest that alpha9-nAChR-mediated cyclin D3 overexpression is important for nicotine-induced transformation of normal human breast epithelial cells. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 22085699-11 2011 We further demonstrated that through Src, the ligation of nicotine with nAChR stimulated the EGFR/ERK1/2 pathway for the activation of E2F1 and further cell progression. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 21691078-0 2011 Nicotine reduces TNF-alpha expression through a alpha7 nAChR/MyD88/NF-kB pathway in HBE16 airway epithelial cells. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 22085699-13 2011 CONCLUSIONS: Our study reveals the existence of a potential, regulatory network governed by the interaction of nicotine and nAChR that integrates the conventional, mitogenic Src and EGFR signals for breast cancer development. Nicotine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 21691078-11 2011 CONCLUSION: Nicotine reduces TNF-alpha expression in HBE16 airway epithelial cells, mainly through an alpha7 nAChR/MyD88/NF-kappaB pathway. Nicotine 12-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 21097981-2 2011 METHODS: We evaluated heteromeric nAChR regulation via [3H]epibatidine binding following cessation of chronic nicotine or varenicline treatment. Epibatidine 55-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 21110812-6 2011 A number of studies suggest that brain nAChR are critical targets for the development of pharmacotherapy for nicotine and other drug addictions. Nicotine 109-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 21110812-7 2011 In this review, we will discuss the nAChR subtypes, their function in response to endogenous brain transmitters, and how their functions are regulated in the presence of nicotine. Nicotine 170-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 21093112-4 2011 Modeling the inhibitor-nAChR complexes by molecular docking studies explained the structure-activity relationships observed in vitro, and revealed an intriguing molecular binding mode at the active site of nAChR, which raised the possibility that these analogues may arbitrate their insecticidal activity through a mechanism other than imidacloprid. imidacloprid 336-348 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 21093112-4 2011 Modeling the inhibitor-nAChR complexes by molecular docking studies explained the structure-activity relationships observed in vitro, and revealed an intriguing molecular binding mode at the active site of nAChR, which raised the possibility that these analogues may arbitrate their insecticidal activity through a mechanism other than imidacloprid. imidacloprid 336-348 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Glutamic Acid 157-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Glutamic Acid 157-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Rotenone 168-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Rotenone 168-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 182-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 182-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 201-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 21403387-2 2011 This review article presents evidence of nicotinic acetylcholine receptor (nAChR)-mediated protection against neurotoxicity induced by amyloid-beta (Abeta), glutamate, rotenone, and 6-hydroxydopamine (6-OHDA) and the signal transduction involved in this mechanism. Oxidopamine 201-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 21187334-3 2011 This study visualizes and quantifies the subcellular mechanisms involved in nicotine-induced nAChR up-regulation by using transfected fluorescent protein (FP)-tagged alpha4 nAChR subunits and an FP-tagged Sec24D endoplasmic reticulum (ER) exit site marker. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 21187334-3 2011 This study visualizes and quantifies the subcellular mechanisms involved in nicotine-induced nAChR up-regulation by using transfected fluorescent protein (FP)-tagged alpha4 nAChR subunits and an FP-tagged Sec24D endoplasmic reticulum (ER) exit site marker. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 21187334-8 2011 The alpha4beta2(enhanced-ER-export) nAChR resembles nicotine-exposed nAChRs with regard to stoichiometry, intracellular mobility, ERES enhancement, and PM localization. Nicotine 52-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 21187334-10 2011 The experimental data are simulated with a model incorporating two mechanisms: (1) nicotine acts as a stabilizing pharmacological chaperone for nascent alpha4beta2 nAChRs in the ER, eventually increasing PM receptors despite a bottleneck(s) in ER export; and (2) removal of the bottleneck (e.g., by expression of the beta2(enhanced-ER-export) subunit) is sufficient to increase PM nAChR numbers, even without nicotine. Nicotine 83-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 21097981-2 2011 METHODS: We evaluated heteromeric nAChR regulation via [3H]epibatidine binding following cessation of chronic nicotine or varenicline treatment. Nicotine 110-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 21097981-2 2011 METHODS: We evaluated heteromeric nAChR regulation via [3H]epibatidine binding following cessation of chronic nicotine or varenicline treatment. Varenicline 122-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 22125646-8 2011 These results suggested that alpha9 nAChR plays important roles in regulation of bronchial cell growth by endogenous acetylcholine and exogenous nicotine, and susceptibility to NNK-induced carcinogenic transformation. Acetylcholine 117-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 22125646-8 2011 These results suggested that alpha9 nAChR plays important roles in regulation of bronchial cell growth by endogenous acetylcholine and exogenous nicotine, and susceptibility to NNK-induced carcinogenic transformation. Nicotine 145-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 21199776-4 2011 The current review summarizes the important preclinical and clinical data, demonstrating the ability of nAChR ligands to modulate nicotine and alcohol-induced biobehavioral and neurochemical changes in laboratory animals and humans. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 22073194-1 2011 The NCS protein Visinin-like Protein 1 (VILIP-1) transduces calcium signals in the brain and serves as an effector of the non-retinal receptor guanylyl cyclases (GCs) GC-A and GC-B, and nicotinic acetyl choline receptors (nAchR). Calcium 60-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-220 22073194-1 2011 The NCS protein Visinin-like Protein 1 (VILIP-1) transduces calcium signals in the brain and serves as an effector of the non-retinal receptor guanylyl cyclases (GCs) GC-A and GC-B, and nicotinic acetyl choline receptors (nAchR). Calcium 60-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 222-227 21199776-4 2011 The current review summarizes the important preclinical and clinical data, demonstrating the ability of nAChR ligands to modulate nicotine and alcohol-induced biobehavioral and neurochemical changes in laboratory animals and humans. Alcohols 143-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 20875851-2 2010 Here we have investigated whether the alpha7 nicotinic acetylcholine receptor (nAChR) agonist PNU282987 can prevent cell death once the cells have already undergone an oxidative stress. PNU-282987 94-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 21058296-4 2011 Critical protein-sugar interactions implicate residues Ser187 and Trp184 of nAChR and Thr6, Ser9, and Thr15 of alpha-Btx, as well as Thr6 and Pro7 of alpha-Cbtx. Sugars 17-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 20946306-0 2010 The nicotinic acetylcholine receptor partial agonist varenicline increases the ataxic and sedative-hypnotic effects of acute ethanol administration in C57BL/6J mice. Varenicline 53-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 20946306-0 2010 The nicotinic acetylcholine receptor partial agonist varenicline increases the ataxic and sedative-hypnotic effects of acute ethanol administration in C57BL/6J mice. Ethanol 125-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Varenicline 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Varenicline 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Ethanol 110-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Ethanol 110-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20696214-1 2010 Genome-wide association studies have underscored the importance of the clustered neuronal nicotinic acetylcholine receptor (nAChR) subunit genes with respect to nicotine dependence as well as lung cancer susceptibility. Nicotine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-122 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. alkylene 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-99 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. alkylene 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. bis-imi 22-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-99 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. bis-imi 22-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. chloropyridine 120-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-99 20973548-2 2010 The alkylene-tethered bis-IMI binds in a unique mode to the insect nicotinic acetylcholine receptor (nAChR) wherein the chloropyridine moieties are embraced by two distinct and distant domains. chloropyridine 120-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 20973548-6 2010 The nAChR structural model, simulating the binding site interactions of the furan-2,5-dimethylene-tethered bis-IMI, reveals that the furan ring is nestled in a hydrophobic pocket, consisting of three aromatic amino acids, and is stabilized via hydrogen bonding. furan-2,5-dimethylene 76-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 20973548-6 2010 The nAChR structural model, simulating the binding site interactions of the furan-2,5-dimethylene-tethered bis-IMI, reveals that the furan ring is nestled in a hydrophobic pocket, consisting of three aromatic amino acids, and is stabilized via hydrogen bonding. bis-imi 107-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 20973548-6 2010 The nAChR structural model, simulating the binding site interactions of the furan-2,5-dimethylene-tethered bis-IMI, reveals that the furan ring is nestled in a hydrophobic pocket, consisting of three aromatic amino acids, and is stabilized via hydrogen bonding. furan 76-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 20973548-6 2010 The nAChR structural model, simulating the binding site interactions of the furan-2,5-dimethylene-tethered bis-IMI, reveals that the furan ring is nestled in a hydrophobic pocket, consisting of three aromatic amino acids, and is stabilized via hydrogen bonding. Amino Acids, Aromatic 200-220 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 20973548-6 2010 The nAChR structural model, simulating the binding site interactions of the furan-2,5-dimethylene-tethered bis-IMI, reveals that the furan ring is nestled in a hydrophobic pocket, consisting of three aromatic amino acids, and is stabilized via hydrogen bonding. Hydrogen 244-252 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 21267696-10 2010 Both nAChR inhibitors also abolished the upregulation of hBD-2 by nicotine. Nicotine 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 20696214-1 2010 Genome-wide association studies have underscored the importance of the clustered neuronal nicotinic acetylcholine receptor (nAChR) subunit genes with respect to nicotine dependence as well as lung cancer susceptibility. Nicotine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 20696214-2 2010 CHRNB4, which encodes the nAChR beta4 subunit, plays a major role in the molecular mechanisms that govern nicotine withdrawal. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 20849857-6 2010 Specifically, we used (125)I-labeled epibatidine binding to assay brain nicotinic receptor containing 4alpha and 2beta subunits (alpha4beta2-nAChR), since this nicotinic receptor subtype has been shown previously to be sensitive to other estrogens. epibatidine 37-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 20725741-0 2010 Nicotinic acetylcholine receptor genes on chromosome 15q25.1 are associated with nicotine and opioid dependence severity. Nicotine 81-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 20725741-1 2010 A locus on chromosome 15q25.1 previously implicated in nicotine, alcohol, and cocaine dependence, smoking, and lung cancer encodes subunits of the nicotinic acetylcholine receptor (nAChR) expressed in the mesolimbic system and thought to mediate substance dependence. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-179 20725741-1 2010 A locus on chromosome 15q25.1 previously implicated in nicotine, alcohol, and cocaine dependence, smoking, and lung cancer encodes subunits of the nicotinic acetylcholine receptor (nAChR) expressed in the mesolimbic system and thought to mediate substance dependence. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno(1,2-b)pyrrole 200-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 20725741-1 2010 A locus on chromosome 15q25.1 previously implicated in nicotine, alcohol, and cocaine dependence, smoking, and lung cancer encodes subunits of the nicotinic acetylcholine receptor (nAChR) expressed in the mesolimbic system and thought to mediate substance dependence. Alcohols 65-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-179 20725741-1 2010 A locus on chromosome 15q25.1 previously implicated in nicotine, alcohol, and cocaine dependence, smoking, and lung cancer encodes subunits of the nicotinic acetylcholine receptor (nAChR) expressed in the mesolimbic system and thought to mediate substance dependence. Alcohols 65-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno(1,2-b)pyrrole 116-198 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno(1,2-b)pyrrole 116-198 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno(1,2-b)pyrrole 200-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 20736995-1 2010 Common single-nucleotide polymorphisms (SNPs) at nicotinic acetylcholine receptor (nAChR) subunit genes have previously been associated with measures of nicotine dependence. Nicotine 153-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-81 20736995-1 2010 Common single-nucleotide polymorphisms (SNPs) at nicotinic acetylcholine receptor (nAChR) subunit genes have previously been associated with measures of nicotine dependence. Nicotine 153-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. pcp 257-260 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 20822184-0 2010 Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as alpha4beta2-nicotinic acetylcholine receptor-selective partial agonists. Nitrogen 56-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-205 20633568-1 2010 In this study, we compared the in vitro and in vivo neuronal nicotinic acetylcholine receptor (nAChR) properties of 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno[1,2,-b]pyrrole (HDMP, 4) to that of negative allosteric modulator (NAM), PCP. pcp 257-260 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 20633568-6 2010 All together, our in vitro and in vivo data suggest that HDMP is a novel NAM of neuronal nAChRs with potent inhibitory activity at alpha7 nAChR subtype at concentrations <= 1muM that are not effective for alpha4beta2 and alpha3beta4 nAChRs. 1,2,3,3a,4,8b-hexahydro-2-benzyl-6-N,N-dimethylamino-1-methylindeno(1,2-b)pyrrole 57-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 20708605-8 2010 The secreted Abeta was decreased and alphaAPPs was significantly increased by non-selective nAChR agonist nicotine (10 muM) and specific alpha7 nAChR agonist GTS-21 (1 muM), and APP expression was not affected. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20708605-9 2010 Furthermore, specific alpha7 nAChR antagonist methyllycaconitine (MLA) reversed the alterations induced by activation of alpha7 nAChR. methyllycaconitine 46-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 20708605-9 2010 Furthermore, specific alpha7 nAChR antagonist methyllycaconitine (MLA) reversed the alterations induced by activation of alpha7 nAChR. methyllycaconitine 46-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 20822184-0 2010 Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as alpha4beta2-nicotinic acetylcholine receptor-selective partial agonists. amop-h-oh 78-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-205 20708605-9 2010 Furthermore, specific alpha7 nAChR antagonist methyllycaconitine (MLA) reversed the alterations induced by activation of alpha7 nAChR. methyllycaconitine 66-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 20708605-9 2010 Furthermore, specific alpha7 nAChR antagonist methyllycaconitine (MLA) reversed the alterations induced by activation of alpha7 nAChR. methyllycaconitine 66-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 20822184-0 2010 Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as alpha4beta2-nicotinic acetylcholine receptor-selective partial agonists. sazetidine-A 89-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-205 20822184-0 2010 Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as alpha4beta2-nicotinic acetylcholine receptor-selective partial agonists. SCHEMBL2843467 103-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-205 20822184-2 2010 Herein we report the synthesis and pharmacological evaluation of members of a new series of 3-alkoxy-5-aminopyridine derivatives that display good selectivity for the alpha4beta2-nAChR subtype based on ligand binding and functional evaluations. 3-alkoxy-5-aminopyridine 92-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 20822184-5 2010 Structure-activity relationship (SAR) analyses suggest that the introduction of additional substituents to the amino group present on the pyridine ring of the N-demethylated analogue of compound 17 can provide potent alpha4beta2-nAChR-selective ligands for possible use in treatment of neurological and psychiatric disorders including depression. pyridine 138-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 229-234 20828128-2 2010 To guide future fragment-screening using surface plasmon resonance (SPR) biosensor technology as a label-free, direct binding, biophysical screening assay, a focused fragment library was generated based on deconstruction of a set of alpha7 nAChR selective quinuclidine containing ligands with nanomolar affinities. Quinuclidines 256-268 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 240-245 20727979-5 2010 We found that the effects of nicotine on trace and contextual fear conditioning vary by brain region and nAChR subtype. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 20930482-3 2010 In addition, we unexpectedly found that the galantamine-induced improvements in PPI deficits were prevented by the muscarinic ACh receptor (mAChR) antagonists scopolamine and telenzepine (preferential for M(1) subtype), but not by the nAChR antagonists. Galantamine 44-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 20930482-3 2010 In addition, we unexpectedly found that the galantamine-induced improvements in PPI deficits were prevented by the muscarinic ACh receptor (mAChR) antagonists scopolamine and telenzepine (preferential for M(1) subtype), but not by the nAChR antagonists. telenzepine 175-186 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 20704351-3 2010 Relative to etomidate, TFD-etomidate was a more potent inhibitor of the excitatory receptors, nAChR (nicotinic acetylcholine receptor) ((alpha1)(2)beta1delta1gamma1) and 5-HT(3A)R (serotonin type 3A receptor), causing significant inhibition at anesthetic concentrations. CHEMBL2392771 23-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 20661501-0 2010 The role of structured water in mediating general anesthetic action on alpha4beta2 nAChR. Water 23-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 20661501-5 2010 At the majority of binding sites in alpha4beta2 nAChR, halothane replaced the slow-exchanging water molecules and caused a regional water population decrease. Halothane 55-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20661501-5 2010 At the majority of binding sites in alpha4beta2 nAChR, halothane replaced the slow-exchanging water molecules and caused a regional water population decrease. Water 94-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20661501-5 2010 At the majority of binding sites in alpha4beta2 nAChR, halothane replaced the slow-exchanging water molecules and caused a regional water population decrease. Water 132-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 20733118-12 2010 CONCLUSION: The alpha9-nAChR is important for nicotine-induced transformation of normal human breast epithelial cells. Nicotine 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 20704351-3 2010 Relative to etomidate, TFD-etomidate was a more potent inhibitor of the excitatory receptors, nAChR (nicotinic acetylcholine receptor) ((alpha1)(2)beta1delta1gamma1) and 5-HT(3A)R (serotonin type 3A receptor), causing significant inhibition at anesthetic concentrations. Etomidate 27-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 20704351-5 2010 [(3)H]TFD-etomidate photolabeled the alpha-subunit of the nAChR in a manner allosterically regulated by agonists and noncompetitive inhibitors. Etomidate 10-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 20598018-2 2010 This frequency-dependent inhibition is because of nicotine desensitizing heteromeric beta2 subunit-containing nicotinic acetylcholine receptor (nAChR) subtypes. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 19803686-0 2010 The association between dopamine DRD2 polymorphisms and working memory capacity is modulated by a functional polymorphism on the nicotinic receptor gene CHRNA4. Dopamine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-159 20598018-3 2010 Surprisingly, a high dose of nicotine (2 muM; capable of interacting with additional nAChR subtypes) produced an inhibition of dopamine evoked by high frequency stimulation, an effect that was not seen with the low dose of nicotine or the beta2 antagonist, dihydro-beta-erythroidine hydrobromide. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 20598018-4 2010 This inhibition was replicated by application of alpha7 nAChR antagonists methyllcaconitine citrate or alpha-bungarotoxin in conjunction with the low dose of nicotine or dihydro-beta-erythroidine hydrobromide. methyllcaconitine citrate 74-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 20598018-3 2010 Surprisingly, a high dose of nicotine (2 muM; capable of interacting with additional nAChR subtypes) produced an inhibition of dopamine evoked by high frequency stimulation, an effect that was not seen with the low dose of nicotine or the beta2 antagonist, dihydro-beta-erythroidine hydrobromide. Dopamine 127-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 20598018-4 2010 This inhibition was replicated by application of alpha7 nAChR antagonists methyllcaconitine citrate or alpha-bungarotoxin in conjunction with the low dose of nicotine or dihydro-beta-erythroidine hydrobromide. Nicotine 158-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 20598018-3 2010 Surprisingly, a high dose of nicotine (2 muM; capable of interacting with additional nAChR subtypes) produced an inhibition of dopamine evoked by high frequency stimulation, an effect that was not seen with the low dose of nicotine or the beta2 antagonist, dihydro-beta-erythroidine hydrobromide. Nicotine 223-231 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 20598018-3 2010 Surprisingly, a high dose of nicotine (2 muM; capable of interacting with additional nAChR subtypes) produced an inhibition of dopamine evoked by high frequency stimulation, an effect that was not seen with the low dose of nicotine or the beta2 antagonist, dihydro-beta-erythroidine hydrobromide. Dihydro-beta-erythroidine hydrobromide 257-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 20598018-4 2010 This inhibition was replicated by application of alpha7 nAChR antagonists methyllcaconitine citrate or alpha-bungarotoxin in conjunction with the low dose of nicotine or dihydro-beta-erythroidine hydrobromide. Dihydro-beta-erythroidine hydrobromide 170-208 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 20551292-4 2010 During calcium accumulation assays, these NAMs inhibited nAChR activation with IC(50) values ranging from 2.4 microM to more than 100 microM. Calcium 7-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 20504915-2 2010 In this study, we describe the in vitro profile of a novel selective alpha7 nAChR agonist, 5-(6-[(3R)-1-azabicyclo[2,2,2]oct-3-yloxy]pyridazin-3-yl)-1H-indole (ABT-107). 5-(6-(1-azabicyclo(2,2,2)oct-3-yloxy)pyridazin-3-yl)-1H-indole 91-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 20340174-1 2010 Ethanol associated behaviors have been linked to the beta(2)-subunit containing nicotinic acetylcholine receptors (beta(2)*-nAChR); however, there is conflicting evidence on ethanol-induced changes in nAChR expression during and after chronic ethanol consumption. Ethanol 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-129 20504915-2 2010 In this study, we describe the in vitro profile of a novel selective alpha7 nAChR agonist, 5-(6-[(3R)-1-azabicyclo[2,2,2]oct-3-yloxy]pyridazin-3-yl)-1H-indole (ABT-107). 5-(6-(1-azabicyclo(2,2,2)oct-3-yloxy)pyridazin-3-yl)-1H-indole 160-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 20504915-5 2010 ABT-107 potently evoked human and rat alpha7 nAChR current responses in oocytes (EC(50), 50-90 nM total charge, approximately 80% normalized to acetylcholine) that were enhanced by the positive allosteric modulator (PAM) 4-[5-(4-chloro-phenyl)-2-methyl-3-propionyl-pyrrol-1-yl]-benzenesulfonamide (A-867744). 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 20504915-8 2010 In the presence of an alpha7 PAM [A-867744 or N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride (PNU-120596)], the addition of ABT-107 elicited MLA-sensitive alpha7 nAChR-mediated Ca(2+) signals in IMR-32 cells and rat cortical cultures and enhanced extracellular signal-regulated kinase phosphorylation in differentiated PC-12 cells. n-[(3r)-1-azabicyclo[2.2.2]oct-3-yl 46-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 20504915-10 2010 In summary, ABT-107 is a selective high affinity alpha7 nAChR agonist suitable for characterizing the roles of this subtype in pharmacological studies. 5-(6-(1-azabicyclo(2,2,2)oct-3-yloxy)pyridazin-3-yl)-1H-indole 12-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 20614106-5 2010 Preclinical studies have suggested antidepressant-like effects of drugs targeting nAChRs, with the most consistent results observed with alpha4beta2 nAChR modulators such as varenicline and nonspecific nAChR antagonists such as mecamylamine. Mecamylamine 228-240 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 20340174-6 2010 Prolonged withdrawal from chronic ethanol consumption is associated with a decrease in beta(2)*-nAChR availability. Ethanol 34-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 20340174-1 2010 Ethanol associated behaviors have been linked to the beta(2)-subunit containing nicotinic acetylcholine receptors (beta(2)*-nAChR); however, there is conflicting evidence on ethanol-induced changes in nAChR expression during and after chronic ethanol consumption. Ethanol 174-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 201-206 20340174-5 2010 The percent decrease in beta(2)*-nAChR availability from baseline to 5-13 wks withdrawal in the parietal cortex was negatively correlated with total grams of ethanol consumed in lifetime and in the midbrain was negatively correlated with average daily ethanol consumption (g/kg). Ethanol 158-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. Alcohols 61-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. Alcohols 61-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 20340174-5 2010 The percent decrease in beta(2)*-nAChR availability from baseline to 5-13 wks withdrawal in the parietal cortex was negatively correlated with total grams of ethanol consumed in lifetime and in the midbrain was negatively correlated with average daily ethanol consumption (g/kg). Ethanol 252-259 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. Alcohols 124-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 20616056-5 2010 Here we use unnatural amino acid mutagenesis coupled with agonist analogs to examine whether such a hydrogen bond is functionally significant in the alpha4beta2 neuronal nAChR, the receptor most associated with nicotine addiction. Hydrogen 100-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. Alcohols 124-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. beta(2) 16-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 20340174-7 2010 The decrease in beta(2)*-nAChR availability is influenced by alcohol consumption, suggesting the chronicity and severity of alcohol consumption may underlie persistent changes in beta(2)*-nAChR availability. beta(2) 16-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 20660787-0 2010 Multiple binding sites for the general anesthetic isoflurane identified in the nicotinic acetylcholine receptor transmembrane domain. Isoflurane 50-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-111 20660787-1 2010 An extensive search for isoflurane binding sites in the nicotinic acetylcholine receptor (nAChR) and the proton gated ion channel from Gloebacter violaceus (GLIC) has been carried out based on molecular dynamics (MD) simulations in fully hydrated lipid membrane environments. Isoflurane 24-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-88 20660787-1 2010 An extensive search for isoflurane binding sites in the nicotinic acetylcholine receptor (nAChR) and the proton gated ion channel from Gloebacter violaceus (GLIC) has been carried out based on molecular dynamics (MD) simulations in fully hydrated lipid membrane environments. Isoflurane 24-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 20660787-3 2010 Specifically, isoflurane binds persistently to three classes of sites in the nAChR transmembrane domain: (i) An isoflurane dimer occludes the pore, contacting residues identified by previous mutagenesis studies; analogous behavior is observed in GLIC. Isoflurane 14-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 20660787-3 2010 Specifically, isoflurane binds persistently to three classes of sites in the nAChR transmembrane domain: (i) An isoflurane dimer occludes the pore, contacting residues identified by previous mutagenesis studies; analogous behavior is observed in GLIC. Isoflurane 112-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 20660787-5 2010 (iii) Isoflurane binds to the subunit centers of both nAChR alpha chains and one of the GLIC chains, in a site that has had little experimental targeting. Isoflurane 6-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 20660383-10 2010 At approximately 6 h after the start of the infusion, three 30-min SPECT scans and a 15-min transmission-emission scan were acquired to obtain baseline beta(2)*-nAChR availability. beta(2)* 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 20426799-11 2010 CONCLUSIONS & INFERENCES: The C-terminal tail of P2X2 receptors mediates cross-inhibition between alpha3beta4 nAChR-P2X2 receptors. Adenosine Monophosphate 13-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 20616056-5 2010 Here we use unnatural amino acid mutagenesis coupled with agonist analogs to examine whether such a hydrogen bond is functionally significant in the alpha4beta2 neuronal nAChR, the receptor most associated with nicotine addiction. Nicotine 211-219 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 20400469-2 2010 Although few animal studies have assessed the role of the alpha5 nAChR in nicotine-mediated behaviors, recent evidence suggests an association between polymorphisms in the alpha5 nAChR gene and nicotine dependence phenotypes in humans. Nicotine 194-202 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 20400469-2 2010 Although few animal studies have assessed the role of the alpha5 nAChR in nicotine-mediated behaviors, recent evidence suggests an association between polymorphisms in the alpha5 nAChR gene and nicotine dependence phenotypes in humans. Nicotine 74-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 20515764-8 2010 Microscopy analysis of lymphocytes structure showed a direct relationship between their size, their a-7 nAChR expression, and calcium release upon nicotine stimulation. Nicotine 147-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 20400469-2 2010 Although few animal studies have assessed the role of the alpha5 nAChR in nicotine-mediated behaviors, recent evidence suggests an association between polymorphisms in the alpha5 nAChR gene and nicotine dependence phenotypes in humans. Nicotine 74-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 20509659-5 2010 The results suggest that compounds acting via some combination of DA, NE, or 5HT inhibition and/or antagonism of alpha4beta2-nAChR can potentially be new pharmacotherapeutics for treatment of nicotine dependence. Nicotine 192-200 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 20515764-9 2010 Then, this relationship suggested that lymphocytes need a prime activation to express the a-7 nAChR, and therefore to release calcium in response to nicotine. Calcium 126-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 20515764-9 2010 Then, this relationship suggested that lymphocytes need a prime activation to express the a-7 nAChR, and therefore to release calcium in response to nicotine. Nicotine 149-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 20393456-4 2010 The PPI-enhancing effects of nicotine in rodents are strain dependent, suggesting a genetic contribution to PPI within the nicotinic acetylcholine receptor (nAChR) system. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 20105082-3 2010 Dihydrobetaerythroidine (antagonist of heteromeric nAChR), and hexamethonium (antagonist of peripheral nAChR), fully antagonized the effect of MDMA. Dihydro-beta-Erythroidine 0-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 20105082-3 2010 Dihydrobetaerythroidine (antagonist of heteromeric nAChR), and hexamethonium (antagonist of peripheral nAChR), fully antagonized the effect of MDMA. Hexamethonium 63-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 20105082-3 2010 Dihydrobetaerythroidine (antagonist of heteromeric nAChR), and hexamethonium (antagonist of peripheral nAChR), fully antagonized the effect of MDMA. N-Methyl-3,4-methylenedioxyamphetamine 143-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 20105082-3 2010 Dihydrobetaerythroidine (antagonist of heteromeric nAChR), and hexamethonium (antagonist of peripheral nAChR), fully antagonized the effect of MDMA. N-Methyl-3,4-methylenedioxyamphetamine 143-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 20114055-2 2010 Among known subtypes of receptors, alpha 4 beta 2* and alpha 6 beta 2*-nAChR have the highest affinity for nicotine (where * indicates possibility of other subunits). Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 20114055-5 2010 alpha 4 beta 2*-nAChR also modulate GABA release in these areas. gamma-Aminobutyric Acid 36-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 20393456-4 2010 The PPI-enhancing effects of nicotine in rodents are strain dependent, suggesting a genetic contribution to PPI within the nicotinic acetylcholine receptor (nAChR) system. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 20100906-9 2010 The properties of cytisine-related compounds are similar for mouse, rat, and human nAChR, except that varenicline produced greater residual inhibition of mouse alpha4beta2 receptors than with human receptors. cytisine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 20223446-0 2010 Nicotine restores endothelial dysfunction caused by excess sFlt1 and sEng in an in vitro model of preeclamptic vascular endothelium: a possible therapeutic role of nicotinic acetylcholine receptor (nAChR) agonists for preeclampsia. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-196 20223446-0 2010 Nicotine restores endothelial dysfunction caused by excess sFlt1 and sEng in an in vitro model of preeclamptic vascular endothelium: a possible therapeutic role of nicotinic acetylcholine receptor (nAChR) agonists for preeclampsia. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-203 20304984-2 2010 Changes in nicotinic acetylcholine receptor (nAChR) subunit composition may alter electrophysiologic, pharmacologic, and metabolic characteristics of the receptor inducing hyperkalemia on exposure to succinylcholine. Succinylcholine 200-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-43 20304984-2 2010 Changes in nicotinic acetylcholine receptor (nAChR) subunit composition may alter electrophysiologic, pharmacologic, and metabolic characteristics of the receptor inducing hyperkalemia on exposure to succinylcholine. Succinylcholine 200-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 20400893-2 2010 Although numerous studies have shown that high-affinity beta2-containing nAChRs are necessary for the nicotine-induced enhancement of contextual fear conditioning, it is unknown whether other high-affinity nAChR agonists are capable of enhancing this learning. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 20309583-6 2010 In vivo, an experimental periodontitis rat model was established, and the effects of nicotine/alpha-Btx administration on expression of alpha 7 nAChR and development of periodontitis were evaluated. Nicotine 85-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 20309583-8 2010 The expressions of alpha 7 nAChR and IL-1 beta were significantly increased by nicotine administration, whereas alpha-Btx treatment partially suppressed these effects. Nicotine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 20153815-0 2010 Telithromycin blocks neuromuscular transmission and inhibits nAChR currents in vitro. telithromycin 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 20331614-7 2010 CONCLUSIONS AND IMPLICATIONS: The data provide a plausible explanation for the higher abstinence rate in smoking cessation trials following treatment with varenicline than with the two other alpha4beta2 nAChR partial agonists. Varenicline 155-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 20147893-6 2010 Electrochemical recordings of prefrontal cholinergic transients evoked by S 38232 and nicotine indicated that the alpha4beta2(*) nAChR agonist evoked cholinergic transients that were characterized by a faster rise time and more rapid decay than those evoked by nicotine. Nicotine 86-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 19479336-0 2010 Computational analysis of the binding ability of heterocyclic and conformationally constrained epibatidine analogs in the neuronal nicotinic acetylcholine receptor. epibatidine 95-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 19479336-2 2010 In this study, we describe a computational approach aimed at estimating the binding ability of epibatidine analogs to interact with the neuronal nicotinic acetylcholine receptor (nAChR) and get insights into the bioactive conformation. epibatidine 95-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-177 19479336-2 2010 In this study, we describe a computational approach aimed at estimating the binding ability of epibatidine analogs to interact with the neuronal nicotinic acetylcholine receptor (nAChR) and get insights into the bioactive conformation. epibatidine 95-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 20147893-6 2010 Electrochemical recordings of prefrontal cholinergic transients evoked by S 38232 and nicotine indicated that the alpha4beta2(*) nAChR agonist evoked cholinergic transients that were characterized by a faster rise time and more rapid decay than those evoked by nicotine. Nicotine 261-269 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 20106947-0 2010 Long-term nicotine exposure-induced chemoresistance is mediated by activation of Stat3 and downregulation of ERK1/2 via nAChR and beta-adrenoceptors in human bladder cancer cells. Nicotine 10-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 20116429-4 2010 These alkaloids and their enantiomers were more effective in depolarizing TE-671 cells which express the human fetal-muscle type nicotinic acetylcholine receptor (nAChR) relative to SH-SY5Y cells which predominately express autonomic nAChRs. Alkaloids 6-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 20371741-1 2010 INTRODUCTION: Nicotine and tobacco smoking administration have demonstrated antinociceptive effects that are mediated by the nicotinic acetylcholine receptor containing the beta2* subunit (beta(2)*-nAChR). Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-203 20167427-4 2010 Nonselective nAChR agonists ABT-594 and varenicline were effective analgesics. 5-(2-azetidinylmethoxy)-2-chloropyridine 28-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 19303028-9 2010 SIGNIFICANCE: The continuous efforts of radiomedicinal chemists led to the development of several interesting PET radioligands for imaging of nAChR including [(18)F]AZAN, a potentially superior alternative to 2-[(18)F]FA. Azaguanine 165-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 20373480-1 2010 Varenicline, alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, is a new class of medications for treating nicotine dependence. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 20373480-1 2010 Varenicline, alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, is a new class of medications for treating nicotine dependence. Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 20373480-2 2010 As an alpha4beta2 nAChR partial agonist, varenicline serves to reduce nicotine withdrawal symptoms, while high-affinity binding of the agonist mitigates the reinforcing effects of smoking. Varenicline 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 20167427-4 2010 Nonselective nAChR agonists ABT-594 and varenicline were effective analgesics. Varenicline 40-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 20303856-6 2010 Although dianionic PA does not play a role in nAChR function, we found that both the stabilization of monoanionic PA and the concentration of other cations at the bilayer surface can account for changes in bilayer physical properties that are observed upon incorporation of the nAChR into 3:2 PC/PA membranes. Phosphatidylcholines 293-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 278-283 20004742-7 2010 Upregulation of IL-10 production by auto/paracrine ACh was mediated predominantly through alpha7 nAChR. Acetylcholine 51-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 70-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-57 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 70-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 70-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 70-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 89-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-57 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 89-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 89-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 140-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-57 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 140-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 140-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20303856-1 2010 Interactions between the nicotinic acetylcholine receptor (nAChR) and phosphatidic acid (PA) are bidirectional in that membranes containing PA are effective at stabilizing an agonist-responsive nAChR, whereas incorporation of the nAChR into the same membranes leads to a substantial increase in lipid lateral packing density. Phosphatidic Acids 140-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 20007924-1 2010 RATIONALE: Genome-wide association studies have identified genetic variants in the nicotinic acetylcholine receptor (nAChR) on chromosome 15q24/25 as a risk for nicotine dependence, lung cancer, and chronic obstructive pulmonary disease (COPD). Nicotine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-115 20007924-1 2010 RATIONALE: Genome-wide association studies have identified genetic variants in the nicotinic acetylcholine receptor (nAChR) on chromosome 15q24/25 as a risk for nicotine dependence, lung cancer, and chronic obstructive pulmonary disease (COPD). Nicotine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 19959340-0 2010 The nicotinic acetylcholine receptor partial agonist varenicline and the treatment of drug dependence: a review. Varenicline 53-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Nicotine 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Nicotine 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Alcohols 93-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Alcohols 93-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Cocaine 129-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 19959340-3 2010 The nicotinic acetylcholine receptor (nAChR) plays an important role in nicotine dependence, alcohol consumption and cue-induced cocaine craving. Cocaine 129-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 19959340-5 2010 Varenicline, an alpha4beta2 nAChR partial agonist and an alpha7 nAChR full agonist registered for the treatment of nicotine dependence, significantly reduces nicotine craving and prevents relapse. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 19959340-5 2010 Varenicline, an alpha4beta2 nAChR partial agonist and an alpha7 nAChR full agonist registered for the treatment of nicotine dependence, significantly reduces nicotine craving and prevents relapse. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 19896527-10 2010 These findings provide evidence that early postnatal exposure to nicotine significantly affects nAChR subunit expressions in the developing brainstem. Nicotine 65-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 20146581-3 2010 Experimental evidence indicates that the alpha(7)-nicotinic acetylcholine receptor (alpha(7)nAChR) stimulates PDAC via stress neurotransmitter-mediated activation of beta-adrenergic signaling while the alpha(4)beta(2)nAChR inhibits PDAC via GABA-mediated inhibition of adenylyl cyclase activation. pdac 110-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20146581-3 2010 Experimental evidence indicates that the alpha(7)-nicotinic acetylcholine receptor (alpha(7)nAChR) stimulates PDAC via stress neurotransmitter-mediated activation of beta-adrenergic signaling while the alpha(4)beta(2)nAChR inhibits PDAC via GABA-mediated inhibition of adenylyl cyclase activation. pdac 110-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 217-222 20146581-3 2010 Experimental evidence indicates that the alpha(7)-nicotinic acetylcholine receptor (alpha(7)nAChR) stimulates PDAC via stress neurotransmitter-mediated activation of beta-adrenergic signaling while the alpha(4)beta(2)nAChR inhibits PDAC via GABA-mediated inhibition of adenylyl cyclase activation. pdac 232-236 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20146581-3 2010 Experimental evidence indicates that the alpha(7)-nicotinic acetylcholine receptor (alpha(7)nAChR) stimulates PDAC via stress neurotransmitter-mediated activation of beta-adrenergic signaling while the alpha(4)beta(2)nAChR inhibits PDAC via GABA-mediated inhibition of adenylyl cyclase activation. gamma-Aminobutyric Acid 241-245 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 19896527-2 2010 We tested the hypothesis that nicotine increases expression of the nicotinic acetylcholine receptor (nAChR) subunits alpha7 and beta2 in a piglet model. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-99 19896527-2 2010 We tested the hypothesis that nicotine increases expression of the nicotinic acetylcholine receptor (nAChR) subunits alpha7 and beta2 in a piglet model. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 19921817-5 2010 On the other hand, combined treatment with luteolin (Lut, 0.5 microM) and quercetin (Que, 0.5 microM) profoundly decreased MDA-MB-231 proliferation by down-regulating alpha9-nAChR expression. Quercetin 74-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 20049590-4 2010 Based on predictions arising from the mechanism of receptor inhibition by MK-801 and cocaine, we developed two classes of RNA aptamers: class I members, which inhibit the nAChR, and class II members, which alleviate inhibition of the receptor by MK-801 and cocaine. Dizocilpine Maleate 74-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 171-176 20049590-7 2010 We demonstrate that a truncated class I aptamer containing a sequence of seven nucleotides inhibits the nAChR and that a truncated class II aptamer containing a sequence of only four nucleotides can alleviate MK-801 inhibition. Dizocilpine Maleate 209-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 20124469-2 2010 Nicotine addiction begins with the binding of nicotine to its cognate receptor, the nicotinic acetylcholine receptor (nAChR). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-116 20124469-2 2010 Nicotine addiction begins with the binding of nicotine to its cognate receptor, the nicotinic acetylcholine receptor (nAChR). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 20124469-2 2010 Nicotine addiction begins with the binding of nicotine to its cognate receptor, the nicotinic acetylcholine receptor (nAChR). Nicotine 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-116 20124469-2 2010 Nicotine addiction begins with the binding of nicotine to its cognate receptor, the nicotinic acetylcholine receptor (nAChR). Nicotine 46-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 20124469-3 2010 Genome-wide association studies have implicated the nAChR gene cluster, CHRNA5/A3/B4, in nicotine addiction and lung cancer susceptibility. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19901032-3 2010 They are characterized by a conserved two-disulfide bond framework, which gives rise to two intervening loops of extensively mutated amino acids that determine their selectivity for different nAChR subtypes. Disulfides 42-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 19901032-5 2010 A positional scan synthetic combinatorial library was constructed based on the three residues of the n-loop of alpha-conotoxin ImI to give a total of 10,648 possible combinations that were screened for functional activity in an alpha(7) nAChR Fluo-4/Ca2+ assay, allowing amino acids that confer antagonistic activity for this receptor to be identified. Fluo 4 243-249 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 237-242 20014754-0 2010 Higher susceptibility to halothane modulation in open- than in closed-channel alpha4beta2 nAChR revealed by molecular dynamics simulations. Halothane 25-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 20014754-12 2010 The study concludes that sensitivity and global dynamics responsiveness of alpha4beta2 nAChR to halothane are conformation dependent. Halothane 96-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 19923442-1 2010 The use of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea], a positive allosteric modulator of alpha7 nicotinic acetylcholine receptor (nAChR), may be beneficial for enhancing cholinergic therapies. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 11-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 19923442-1 2010 The use of PNU-120596 [1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)-urea], a positive allosteric modulator of alpha7 nicotinic acetylcholine receptor (nAChR), may be beneficial for enhancing cholinergic therapies. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 23-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 19923442-3 2010 In the presence of PNU-120596, subthreshold (i.e., inactive) physiological concentrations of choline ( approximately 10 microM) elicited repetitive step-like whole-cell responses reminiscent of single ion channel openings that were reversibly blocked by 20 nM methyllycaconitine, a selective alpha7 nAChR antagonist. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 19-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 299-304 19923442-3 2010 In the presence of PNU-120596, subthreshold (i.e., inactive) physiological concentrations of choline ( approximately 10 microM) elicited repetitive step-like whole-cell responses reminiscent of single ion channel openings that were reversibly blocked by 20 nM methyllycaconitine, a selective alpha7 nAChR antagonist. Choline 93-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 299-304 19923442-6 2010 In the presence of PNU-120596 in current clamp, transient step-like depolarizations ( approximately 5 mV) enhanced neuronal excitability and triggered voltage-gated conductances; a single opening of an alpha7-containing nAChR channel appeared to transiently depolarize the entire neuron and facilitate spontaneous firing. 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea 19-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 220-225 19961216-1 2010 The nicotinic acetylcholine receptor (nAChR) is a member of the important Cys loop ligand-gated ion channel superfamily that modulates neuronal excitability. Cysteine 74-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 19961216-1 2010 The nicotinic acetylcholine receptor (nAChR) is a member of the important Cys loop ligand-gated ion channel superfamily that modulates neuronal excitability. Cysteine 74-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 19961216-3 2010 We monitored structural changes occurring during fast and slow desensitization in the transmembrane domain of the Torpedo nAChR using time-resolved photolabeling with the hydrophobic probe 3-(trifluoromethyl)-3-(m-iodophenyl)diazirine (TID). 3-(trifluoromethyl)-3-(3-iodophenyl)diazirine 189-234 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 19921817-5 2010 On the other hand, combined treatment with luteolin (Lut, 0.5 microM) and quercetin (Que, 0.5 microM) profoundly decreased MDA-MB-231 proliferation by down-regulating alpha9-nAChR expression. Quercetin 85-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 19921817-8 2010 Such results show that Lut- or Que-induced antitransforming activities were not limited to specific inhibition of the alpha9-nAChR receptor. Quercetin 31-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 20109141-8 2010 The non-selective nAChR agonist nicotine has been shown to improve CDS in several human clinical studies, and recent trials have been undertaken to evaluate the efficacy of more alpha4beta2 selective compounds. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 20150622-7 2010 The mAChR3 antagonist, 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP), or the nAChR antagonist, mecamylamine hydrochloride (Meca), inhibited SBC3 cell proliferation in the presence or the absence of exogenous Ach. Mecamylamine 106-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 20109141-8 2010 The non-selective nAChR agonist nicotine has been shown to improve CDS in several human clinical studies, and recent trials have been undertaken to evaluate the efficacy of more alpha4beta2 selective compounds. cds 67-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 19693492-1 2009 RATIONALE: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is approved for smoking cessation. Varenicline 11-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-66 19583978-8 2009 In addition, clothianidin-induced currents were completely blocked by methyllicaconitine suggesting that (1) clothianidin acted as a specific agonist of nAChR subtypes and (2) a small proportion of receptors blocked by MLA was insensitive to alpha-bungarotoxin. clothianidin 13-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19583978-8 2009 In addition, clothianidin-induced currents were completely blocked by methyllicaconitine suggesting that (1) clothianidin acted as a specific agonist of nAChR subtypes and (2) a small proportion of receptors blocked by MLA was insensitive to alpha-bungarotoxin. methyllicaconitine 70-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19583978-8 2009 In addition, clothianidin-induced currents were completely blocked by methyllicaconitine suggesting that (1) clothianidin acted as a specific agonist of nAChR subtypes and (2) a small proportion of receptors blocked by MLA was insensitive to alpha-bungarotoxin. clothianidin 109-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19861413-1 2009 The strychnine-sensitive glycine receptor (GlyR) is a ligand-gated chloride channel and a member of the superfamily of cysteine loop (Cys-loop) neurotransmitter receptors, which also comprises the nicotinic acetylcholine receptor (nAChR). Cysteine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-229 19861413-1 2009 The strychnine-sensitive glycine receptor (GlyR) is a ligand-gated chloride channel and a member of the superfamily of cysteine loop (Cys-loop) neurotransmitter receptors, which also comprises the nicotinic acetylcholine receptor (nAChR). Cysteine 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-229 19861413-1 2009 The strychnine-sensitive glycine receptor (GlyR) is a ligand-gated chloride channel and a member of the superfamily of cysteine loop (Cys-loop) neurotransmitter receptors, which also comprises the nicotinic acetylcholine receptor (nAChR). Cysteine 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 231-236 19698703-0 2009 Association of nAChR gene haplotypes with heavy alcohol use and body mass. Alcohols 48-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 171-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-37 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 171-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 339-345 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 294-301 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-37 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 294-301 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 339-345 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 294-301 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-37 19698703-8 2009 Moreover, one haplotype of the CHRNA4 (GGTG) was associated with increased body weight as compared to non-carriers of this haplotype, especially in the heavy consumers of alcohol (p=0.004).The present findings are the first to disclose a haplotype association between the CHRNA6 gene and heavy alcohol use as well as an association of the CHRNA4 gene with increased body mass in heavy consumers of alcohol. Alcohols 294-301 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 339-345 19846875-3 2009 In this study, we determined the immunological effects of alpha7 nAChR activation by nicotine. Nicotine 85-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 19644040-1 2009 The alpha6 nicotinic acetylcholine receptor (nAChR) subunit is involved in nicotine-stimulated dopamine release in the striatum. Nicotine 75-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 19644040-1 2009 The alpha6 nicotinic acetylcholine receptor (nAChR) subunit is involved in nicotine-stimulated dopamine release in the striatum. Dopamine 95-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 19644040-2 2009 It is expressed in brain regions and coexpressed with nAChR subtypes implicated in nicotine dependence behaviors; hence, this subunit may play a role in nicotine dependence. Nicotine 83-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 19644040-2 2009 It is expressed in brain regions and coexpressed with nAChR subtypes implicated in nicotine dependence behaviors; hence, this subunit may play a role in nicotine dependence. Nicotine 153-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 19644040-9 2009 These results suggest a role for the alpha6 nAChR subunit in nicotine reward and affective nicotine withdrawal but not acute nicotine-induced or physical withdrawal behaviors. Nicotine 61-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 19644040-9 2009 These results suggest a role for the alpha6 nAChR subunit in nicotine reward and affective nicotine withdrawal but not acute nicotine-induced or physical withdrawal behaviors. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 19644040-9 2009 These results suggest a role for the alpha6 nAChR subunit in nicotine reward and affective nicotine withdrawal but not acute nicotine-induced or physical withdrawal behaviors. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 19693492-1 2009 RATIONALE: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is approved for smoking cessation. Varenicline 11-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 19754159-0 2009 [(3)H]chlorpromazine photolabeling of the torpedo nicotinic acetylcholine receptor identifies two state-dependent binding sites in the ion channel. [(3)h]chlorpromazine 0-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-82 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-63 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 249-254 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-63 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 19754159-1 2009 Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. Chlorpromazine 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 249-254 19754159-2 2009 For nAChR equilibrated with agonist, we confirm previous reports that [(3)H]CPZ occupies a site near the cytoplasmic end of the M2 ion channel domain, photolabeling positions M2-2, M2-6, and/or M2-9 in each subunit. [(3)h]cpz 70-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 19754159-7 2009 These results provide novel information about the modes of drug binding within the nAChR ion channel and indicate that within the nAChR transmembrane domain, the binding of cationic aromatic amine antagonists can be restricted to the ion channel domain, in contrast to the uncharged, allosteric potentiators and inhibitors that also bind within the delta subunit helix bundle and at subunit interfaces. aromatic amine 182-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 19754159-7 2009 These results provide novel information about the modes of drug binding within the nAChR ion channel and indicate that within the nAChR transmembrane domain, the binding of cationic aromatic amine antagonists can be restricted to the ion channel domain, in contrast to the uncharged, allosteric potentiators and inhibitors that also bind within the delta subunit helix bundle and at subunit interfaces. aromatic amine 182-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 19540212-1 2009 A major hurdle in defining the molecular biology of nicotine addiction has been characterizing the different nicotinic acetylcholine receptor (nAChR) subtypes in the brain and how nicotine alters their function. Nicotine 52-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-141 19628475-3 2009 Since neuronal acetylcholine receptors (nAChRs) are part of the glutamatergic pathway, we searched for sequence variants in CHRNA3, CHRNA4 and CHRNB4 genes, encoding neuronal nicotinic AChR subunits, in 245 SALS patients and in 450 controls. Acetylcholine 15-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-138 19628475-10 2009 We suggest that these gain-of-function variants might contribute to disease liability in a subset of SALS because Ca(2+) signals mediate nAChR"s neuromodulatory effects, including regulation of glutamate release and control of cell survival. Glutamic Acid 194-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 19501054-0 2009 Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Varenicline 66-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 19501054-2 2009 Since alpha4beta2 and other nAChR subtypes play important roles in mediating central processes that control reward, mood, cognition and attention, there is interest in examining the effects of selective nAChR ligands such as varenicline in preclinical animal models that assess these behaviors. Varenicline 225-236 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 19501054-1 2009 The pharmacological properties and pharmacokinetic profile of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target receptor that for a large part explain its efficacy as a smoking cessation aid. Varenicline 135-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 19540212-1 2009 A major hurdle in defining the molecular biology of nicotine addiction has been characterizing the different nicotinic acetylcholine receptor (nAChR) subtypes in the brain and how nicotine alters their function. Nicotine 52-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 19564872-2 2009 Brain nicotinic acetylcholine receptor (nAChR)-encoding genes are among the most prominent candidate genes studied in the context of ND, because of their biological relevance as binding sites for nicotine. Nicotine 196-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-38 19576181-3 2009 We determined the anti-inflammatory potential of GTS-21, an alpha7nAChR-selective partial agonist, on primary human leukocytes and compared it with nicotine, the nAChR agonist widely used for research into the anti-inflammatory effects of alpha7nAChR stimulation. 3-(2,4-dimethoxybenzylidene)anabaseine 49-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 19576182-0 2009 Insight in nAChR subtype selectivity from AChBP crystal structures. achbp 42-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 19623583-5 2009 Using siRNA methodology, we found that the alpha(7) nAChR plays a dominant role in nicotine-induced cell signaling (assessed by intracellular calcium and NO imaging, and studies of protein expression and phosphorylation), as well as nicotine-activated EC functions (proliferation, survival, migration, and tube formation). Nicotine 83-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19623583-5 2009 Using siRNA methodology, we found that the alpha(7) nAChR plays a dominant role in nicotine-induced cell signaling (assessed by intracellular calcium and NO imaging, and studies of protein expression and phosphorylation), as well as nicotine-activated EC functions (proliferation, survival, migration, and tube formation). Calcium 142-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19623583-7 2009 Our studies reveal a critical role for the alpha(7) nAChR in mediating the effects of nicotine on the endothelium. Nicotine 86-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19564872-2 2009 Brain nicotinic acetylcholine receptor (nAChR)-encoding genes are among the most prominent candidate genes studied in the context of ND, because of their biological relevance as binding sites for nicotine. Nicotine 196-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 19620239-1 2009 Nicotinic acetylcholine receptor (nAChR) agonists, such as epibatidine and its molecular derivatives, are potential therapeutic agents for a variety of neurological disorders. epibatidine 59-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 20161506-1 2009 Indolizidine (-)-235B" is a particularly interesting natural product, as it is the currently known, most potent and subtype-selective open-channel blocker of the alpha4beta2 nicotinic acetylcholine receptor (nAChR). Indolizidines 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 20161506-1 2009 Indolizidine (-)-235B" is a particularly interesting natural product, as it is the currently known, most potent and subtype-selective open-channel blocker of the alpha4beta2 nicotinic acetylcholine receptor (nAChR). (-)-235b 13-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 19697903-3 2009 Using our published open-channel structure model of alpha4beta2 nAChR, we identified and evaluated six amphiphilic interaction sites for the volatile anesthetic halothane via flexible ligand docking and subsequent 20-ns molecular dynamics simulations. Halothane 161-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 19620239-1 2009 Nicotinic acetylcholine receptor (nAChR) agonists, such as epibatidine and its molecular derivatives, are potential therapeutic agents for a variety of neurological disorders. epibatidine 59-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 19620239-6 2009 Consideration of the location of the photolabeled amino acids in homology models of the nAChRs based upon the acetylcholine-binding protein structure and the results of ligand docking simulations suggests that epibatidine binds in a single preferred orientation within the alpha-gamma transmitter binding site, whereas it binds in two distinct orientations in the alpha4beta2 nAChR. Acetylcholine 110-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 19620239-6 2009 Consideration of the location of the photolabeled amino acids in homology models of the nAChRs based upon the acetylcholine-binding protein structure and the results of ligand docking simulations suggests that epibatidine binds in a single preferred orientation within the alpha-gamma transmitter binding site, whereas it binds in two distinct orientations in the alpha4beta2 nAChR. epibatidine 210-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 19654299-1 2009 We previously showed that nicotine stimulates non-small cell lung carcinoma (NSCLC) cell proliferation through nicotinic acetylcholine receptor (nAChR)-mediated signals. Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-143 19482438-3 2009 Cotinine levels were higher in carriers of the CC genotype of CHRNA4 rs1044396 (371 ng/ml) than in those with the CT or TT genotypes (275 ng/ml, p=0.049), a difference of 0.53 standard deviation units. Cotinine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-68 19523966-6 2009 However, DMSO (>1%) did inhibit alpha7 nAChR-mediated currents. Dimethyl Sulfoxide 9-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 19654299-1 2009 We previously showed that nicotine stimulates non-small cell lung carcinoma (NSCLC) cell proliferation through nicotinic acetylcholine receptor (nAChR)-mediated signals. Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 19654299-6 2009 Of note, nicotine induced complex formation between alpha7 nAChR and PPARbeta/delta protein and increased PPARbeta/delta gene promoter activity through inhibition of AP-2alpha as shown by reduced AP-2alpha binding using electrophoretic gel mobility shift and chromatin immunoprecipitation assays. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 19654299-3 2009 Here, we explore the potential link between nicotine and PPARbeta/delta and report that nicotine increases the expression of PPARbeta/delta protein; this effect was blocked by an alpha7 nAChR antagonist (alpha-bungarotoxin), by alpha7 nAChR short interfering RNA, and by inhibitors of phosphatidylinositol 3-kinase (PI3K; wortmannin and LY294002) and mammalian target of rapamycin (mTOR; rapamycin). Nicotine 44-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 19654299-8 2009 Collectively, our results show that nicotine increases PPARbeta/delta gene expression through alpha7 nAChR-mediated activation of PI3K/mTOR signals that inhibit AP-2alpha protein expression and DNA binding activity to the PPARbeta/delta gene promoter. Nicotine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 19654299-3 2009 Here, we explore the potential link between nicotine and PPARbeta/delta and report that nicotine increases the expression of PPARbeta/delta protein; this effect was blocked by an alpha7 nAChR antagonist (alpha-bungarotoxin), by alpha7 nAChR short interfering RNA, and by inhibitors of phosphatidylinositol 3-kinase (PI3K; wortmannin and LY294002) and mammalian target of rapamycin (mTOR; rapamycin). Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-191 19654299-3 2009 Here, we explore the potential link between nicotine and PPARbeta/delta and report that nicotine increases the expression of PPARbeta/delta protein; this effect was blocked by an alpha7 nAChR antagonist (alpha-bungarotoxin), by alpha7 nAChR short interfering RNA, and by inhibitors of phosphatidylinositol 3-kinase (PI3K; wortmannin and LY294002) and mammalian target of rapamycin (mTOR; rapamycin). Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 19290018-6 2009 The consistent effect estimates across three independent cohorts elaborate on recently published functional studies of rs2236196 from the CHRNA4 3"-untranslated region and seem to converge with accumulating evidence to firmly implicate the variant G allele of this polymorphism in the intensification of nicotine dependence. Nicotine 304-312 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-144 19569163-5 2009 More prolonged exposure to AMOP-H-OH and its analogues produces inhibition of subsequent responses to acute challenges with full nicotinic agonists, again selectively for alpha4beta2-nAChRs over other nAChR subtypes. amop-h-oh 27-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 19569163-10 2009 The net action of prolonged exposure to AMOP-H-OH or its analogues, as for nicotine, seems to be a selective decrease in alpha4beta2-nAChR function. amop-h-oh 40-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 19569163-10 2009 The net action of prolonged exposure to AMOP-H-OH or its analogues, as for nicotine, seems to be a selective decrease in alpha4beta2-nAChR function. Nicotine 75-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 19652217-4 2009 METHODS: A novel nAChR radioligand, 5-(6-fluorohexyn-1-yl)-3-[2(S)-2-azetidinylmethoxy]pyridine (ZW-104), was characterized in vitro using competition binding assays (nAChR subtypes heterologously expressed in HEK 293 cells and in native alpha4beta2 nAChRs from rat brain). (18)F-ZW-104 36-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 19652217-4 2009 METHODS: A novel nAChR radioligand, 5-(6-fluorohexyn-1-yl)-3-[2(S)-2-azetidinylmethoxy]pyridine (ZW-104), was characterized in vitro using competition binding assays (nAChR subtypes heterologously expressed in HEK 293 cells and in native alpha4beta2 nAChRs from rat brain). (18)F-ZW-104 36-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 19652217-4 2009 METHODS: A novel nAChR radioligand, 5-(6-fluorohexyn-1-yl)-3-[2(S)-2-azetidinylmethoxy]pyridine (ZW-104), was characterized in vitro using competition binding assays (nAChR subtypes heterologously expressed in HEK 293 cells and in native alpha4beta2 nAChRs from rat brain). zw-104 97-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 19652217-4 2009 METHODS: A novel nAChR radioligand, 5-(6-fluorohexyn-1-yl)-3-[2(S)-2-azetidinylmethoxy]pyridine (ZW-104), was characterized in vitro using competition binding assays (nAChR subtypes heterologously expressed in HEK 293 cells and in native alpha4beta2 nAChRs from rat brain). zw-104 97-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 19498421-3 2009 RESULTS: Application of 0.1 micromol/L nicotine or 1 mmol/L acetylcholine (ACh) for 1 s or longer induced two phases, with time constants of approximately 70 and approximately 700 ms, for the onset of alpha4beta2-nAChR desensitization. Nicotine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 19339660-0 2009 Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site. Tryptophan 91-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-142 19321668-10 2009 The prospects of designing neonicotinoids that are safe not only for mammals but also for beneficial insects such as honey bees (Apis mellifera) are discussed in terms of interactions with non-alpha nAChR subunits. Neonicotinoids 27-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 19548687-4 2009 The N-substituted cytisines were docked into the rat and human alpha(4)beta(2) nAChR models based on the extracellular domain of a molluscan acetylcholine binding protein. n-substituted cytisines 4-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 19548687-4 2009 The N-substituted cytisines were docked into the rat and human alpha(4)beta(2) nAChR models based on the extracellular domain of a molluscan acetylcholine binding protein. Acetylcholine 141-154 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 19552432-0 2009 Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. octahydropyrrolo(3,4-c)pyrrole 0-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 19552432-0 2009 Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Diamines 34-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 19481945-0 2009 Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. Carbon-11 45-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-165 19481945-0 2009 Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography. pyridyl ethers 63-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-165 19481945-3 2009 In this study, we report the synthesis, nAChR binding affinity, and pharmacological properties of several novel 3-pyridyl ether compounds. 3-pyridyl ether compounds 112-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 19481945-5 2009 Three of these novel nAChR ligands were radiolabeled with the positron-emitting isotope (11)C and evaluated in animal studies as potential PET radiotracers for imaging of cerebral nAChRs with improved brain kinetics. nachrs 180-186 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 19448647-2 2009 The nAChRs are known to be differentially permeable to calcium ions, with the alpha7 nAChR subtype having one of the highest permeabilities to calcium. Calcium 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 19448647-2 2009 The nAChRs are known to be differentially permeable to calcium ions, with the alpha7 nAChR subtype having one of the highest permeabilities to calcium. Calcium 143-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 19448647-5 2009 Downstream signaling events mediated by nAChR-mediated calcium responses can be grouped into instantaneous effects (such as neurotransmitter release, which can occur in milliseconds after nAChR activation), short-term effects (such as the recovery of nAChR desensitization through cellular signaling cascades), and long-term effects (such as neuroprotection via gene expression). Calcium 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 19448647-5 2009 Downstream signaling events mediated by nAChR-mediated calcium responses can be grouped into instantaneous effects (such as neurotransmitter release, which can occur in milliseconds after nAChR activation), short-term effects (such as the recovery of nAChR desensitization through cellular signaling cascades), and long-term effects (such as neuroprotection via gene expression). Calcium 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 19448647-5 2009 Downstream signaling events mediated by nAChR-mediated calcium responses can be grouped into instantaneous effects (such as neurotransmitter release, which can occur in milliseconds after nAChR activation), short-term effects (such as the recovery of nAChR desensitization through cellular signaling cascades), and long-term effects (such as neuroprotection via gene expression). Calcium 55-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 19498421-3 2009 RESULTS: Application of 0.1 micromol/L nicotine or 1 mmol/L acetylcholine (ACh) for 1 s or longer induced two phases, with time constants of approximately 70 and approximately 700 ms, for the onset of alpha4beta2-nAChR desensitization. Acetylcholine 60-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 19448647-6 2009 In addition, nAChR activity can be regulated by cytoplasmic calcium levels, suggesting a complex reciprocal relationship. Calcium 60-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 19448647-7 2009 Further advances in imaging techniques, animal models, and more potent and subtype-selective ligands for neuronal nAChRs would help in understanding the neuronal nAChR-mediated calcium signaling, and lead to the development of improved therapeutic treatments. Calcium 177-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 19498421-3 2009 RESULTS: Application of 0.1 micromol/L nicotine or 1 mmol/L acetylcholine (ACh) for 1 s or longer induced two phases, with time constants of approximately 70 and approximately 700 ms, for the onset of alpha4beta2-nAChR desensitization. Acetylcholine 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 19342512-7 2009 In HEK-293 cells coexpressing alpha(3)beta(4) nAChR/P2X(2) receptors, coapplication of ATP and ACh caused a current that was 58 +/- 7% of the predicted current (P < 0.05). Adenosine Triphosphate 87-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Hydrogen 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 19486673-1 2009 The ligand-gated ion channel from Erwinia chrysanthemi (ELIC) is a prokaryotic homolog of the eukaryotic nicotinic acetylcholine receptor (nAChR) that responds to the binding of neurotransmitter acetylcholine and mediates fast signal transmission. Acetylcholine 115-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Hydrogen 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Amides 178-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Amides 178-183 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Esters 187-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 19405066-1 2009 Probing the sheet: The network of hydrogen bonds formed in the outer beta sheet of the nicotinic acetylcholine receptor (nAChR; see figure) is fairly robust and tolerates single amide-to-ester mutations throughout. Esters 187-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 19405066-2 2009 However, eliminating two proximal hydrogen bonds completely destroys receptor function; this adds further support to gating models that ascribe important roles to these beta strands of the nAChR extracellular domain.Long-range communication is essential for the function of members of the Cys-loop family of neurotransmitter-gated ion channels. Hydrogen 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 19405066-2 2009 However, eliminating two proximal hydrogen bonds completely destroys receptor function; this adds further support to gating models that ascribe important roles to these beta strands of the nAChR extracellular domain.Long-range communication is essential for the function of members of the Cys-loop family of neurotransmitter-gated ion channels. Cysteine 289-292 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 19405066-4 2009 To probe the role of the peptide backbone, we incorporated a series of alpha-hydroxy acid analogues into the beta-sheet-rich extracellular domain of the muscle subtype of the nicotinic acetylcholine receptor, the prototypical Cys-loop receptor. alpha-hydroxy acid 71-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 175-207 19338581-1 2009 BACKGROUND AND PURPOSE: Benzylidene-anabaseines (BAs) are partial agonists of the alpha7 nicotinic acetylcholine receptor (nAChR) but their mechanism(s) of action are unknown. benzylidene-anabaseines 24-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 19419220-0 2009 Anionic lipid and cholesterol interactions with alpha4beta2 nAChR: insights from MD simulations. Cholesterol 18-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 19419220-1 2009 Anionic lipids and cholesterols (CHOL) are critical to the function of nicotinic acetylcholine receptors (nAChR). Cholesterol 19-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-104 19419220-1 2009 Anionic lipids and cholesterols (CHOL) are critical to the function of nicotinic acetylcholine receptors (nAChR). Cholesterol 19-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 19419220-1 2009 Anionic lipids and cholesterols (CHOL) are critical to the function of nicotinic acetylcholine receptors (nAChR). Cholesterol 33-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-104 19419220-1 2009 Anionic lipids and cholesterols (CHOL) are critical to the function of nicotinic acetylcholine receptors (nAChR). Cholesterol 33-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 19419220-11 2009 A higher number of salt bridges and hydrogen bonds (H bonds) between POPA and the alpha4beta2 nAChR were found in the open system than in the closed system, suggesting a potential role of POPA in the equilibrium between different channel states. Hydrogen 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 19270530-8 2009 On the other hand, nicotine (nAChR agonist) enhanced the autophagic process and also inhibited cell death following Abeta application. Nicotine 19-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 19338581-6 2009 Both BAs enhanced [(3)H]TCP binding when the nAChR was initially in the resting but activatable state, suggesting that both compounds desensitized the Torpedo nAChR. [(3)h]tcp 18-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 19338581-10 2009 The NCA-binding site for BAs overlaps both the phencyclidine- and dizocilpine-binding sites in the desensitized Torpedo nAChR ion channel. Phencyclidine 47-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 19338581-10 2009 The NCA-binding site for BAs overlaps both the phencyclidine- and dizocilpine-binding sites in the desensitized Torpedo nAChR ion channel. Dizocilpine Maleate 66-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 20071853-1 2009 Varenicline, a partial agonist of alpha4beta2 nicotinic acetylcholine receptor (nAChR), is the most recently approved drug for smoking cessation. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 19237585-10 2009 Fluorescence-based investigations of nAChR subunit stoichiometry may provide efficient drug discovery methods for nicotine addiction or for other disorders that result from dysregulated nAChRs. Nicotine 114-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 19236104-8 2009 Agonists such as acetylcholine, nicotine, which are used in a diverse array of biological activities, such as enhancements of cognitive performances, were also docked with the theoretical model of human alpha(7)nAChR. Acetylcholine 17-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 211-216 19236104-8 2009 Agonists such as acetylcholine, nicotine, which are used in a diverse array of biological activities, such as enhancements of cognitive performances, were also docked with the theoretical model of human alpha(7)nAChR. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 211-216 19186108-7 2009 These novel ligands could serve as potential pharmaceuticals in the AChBP/nAChR systems. achbp 68-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 20071853-3 2009 As a nAChR partial agonist, Varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 19337288-2 2009 ACh interacts with members of the nicotinic acetylcholine receptor (nAChR) family, in particular with the alpha7 subunit (alpha7nAChR), which is expressed not only by neurons but also macrophages and other cells involved in the inflammatory response. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 19144785-6 2009 In both ventral and dorsal putamen, alpha3/alpha6beta2(*) nAChRs regulated > or =80% of non-burst- (single pulse) nAChR-modulated dopamine release, and alpha4beta2(*) nAChRs regulated the remainder. Dopamine 133-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 19144785-8 2009 Next, we investigated the consequence of long-term nicotine exposure via the drinking water on nAChR-modulated responsiveness. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 19144785-8 2009 Next, we investigated the consequence of long-term nicotine exposure via the drinking water on nAChR-modulated responsiveness. Water 86-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 19144785-11 2009 They also show that long-term nicotine treatment selectively modifies nAChR-modulated release in distinct striatal subregions. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 19337288-2 2009 ACh interacts with members of the nicotinic acetylcholine receptor (nAChR) family, in particular with the alpha7 subunit (alpha7nAChR), which is expressed not only by neurons but also macrophages and other cells involved in the inflammatory response. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-66 19210780-6 2009 Some critical interactions in the binding site such as the salt bridge formed between K145/D200 in the neurotoxin-nAChR complex is further stabilized during the MD simulation, while it is obviously more labile in the apo form. K145 86-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 19183258-2 2009 The results indicate that with 2-min pretreatment, U18666A inhibited different nAChR subtypes with a rank-order of potency (IC(50) of whole-cell peak current): alpha4beta2 (8.0 +/- 3.0 nM) > alpha3beta2 (1.7 +/- 0.4 microM) > alpha4beta4 (26 +/- 7.2 microM) > alpha7 (> 100 microM), suggesting this compound is more selective to alpha4beta2-nAChRs. 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 19183258-6 2009 U18666A-induced inhibition of nAChR function is concentration-, voltage-, and use-dependent, suggesting an open channel block. 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 19111588-6 2009 In addition to nicotine, the agonists epibatidine and cytisine both significantly increased the release of sAPP in M10 cells expressing the alpha4/beta2 nAChR subtype, and this effect was blocked by co-treatment with mecamylamine but not by the alpha4/beta2 competitive antagonist dihydro-beta-erythroidine. epibatidine 38-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19111588-6 2009 In addition to nicotine, the agonists epibatidine and cytisine both significantly increased the release of sAPP in M10 cells expressing the alpha4/beta2 nAChR subtype, and this effect was blocked by co-treatment with mecamylamine but not by the alpha4/beta2 competitive antagonist dihydro-beta-erythroidine. cytisine 54-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19111588-6 2009 In addition to nicotine, the agonists epibatidine and cytisine both significantly increased the release of sAPP in M10 cells expressing the alpha4/beta2 nAChR subtype, and this effect was blocked by co-treatment with mecamylamine but not by the alpha4/beta2 competitive antagonist dihydro-beta-erythroidine. Mecamylamine 217-229 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 19125616-6 2009 Dicarba-alpha-ImI maintained inhibitory activity of nAChR comparable to that of native alpha-ImI in two in vitro assays. dicarba-alpha-imi 0-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19125616-6 2009 Dicarba-alpha-ImI maintained inhibitory activity of nAChR comparable to that of native alpha-ImI in two in vitro assays. alpha-imi 8-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 19232492-1 2009 Several N-pyridin-3-yl spirobicyclic diamines, designed as conformationally restricted analogs of tebanicline (ABT-594), were synthesized as novel ligands for nicotinic acetylcholine receptors (nAChR). n-pyridin-3-yl spirobicyclic diamines 8-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 19048619-8 2009 Since tobacco smoking is established as a risk factor in cervical carcinogenesis, and since nicotine and its derivatives become concentrated in cervical mucus, nAChR-dependent signaling is apparently an important molecular cofactor of human papillomavirus-dependent cervical carcinogenesis. Nicotine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 19098004-1 2009 alpha-Conotoxins are small disulfide-rich peptides from the venom of the Conus species that target the nicotinic acetylcholine receptor (nAChR). Disulfides 27-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 19098004-1 2009 alpha-Conotoxins are small disulfide-rich peptides from the venom of the Conus species that target the nicotinic acetylcholine receptor (nAChR). Disulfides 27-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 19027295-2 2009 The carbamate functionality and a small hydrophobic substituent in the C-3 position were found to be vital for the binding affinity to the nAChRs, whereas the carbamate nitrogen substituents were important for nAChR subtype selectivity. Carbamates 4-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 19063970-1 2009 The neuronal Ca2+-sensor protein VILIP-1, known to affect clathrin-dependent receptor trafficking, has been shown to interact with the cytoplasmic loop of the alpha4-subunit of the alpha4beta2 nicotinic acetylcholine receptor (nAChR), which is the most abundant nAChR subtype with high-affinity for nicotine in the brain. Nicotine 299-307 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 227-232 19063970-1 2009 The neuronal Ca2+-sensor protein VILIP-1, known to affect clathrin-dependent receptor trafficking, has been shown to interact with the cytoplasmic loop of the alpha4-subunit of the alpha4beta2 nicotinic acetylcholine receptor (nAChR), which is the most abundant nAChR subtype with high-affinity for nicotine in the brain. Nicotine 299-307 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 262-267 19063970-2 2009 The alpha4beta2 nAChR is crucial for nicotine addiction and the beneficial effects of nicotine on cognition. Nicotine 37-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 19063970-2 2009 The alpha4beta2 nAChR is crucial for nicotine addiction and the beneficial effects of nicotine on cognition. Nicotine 86-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 19182447-4 2009 Furthermore, the ameliorating effect of nicotine is antagonized by methyllycaconitine, a selective alpha7 nAChR antagonist. Nicotine 40-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 19182447-4 2009 Furthermore, the ameliorating effect of nicotine is antagonized by methyllycaconitine, a selective alpha7 nAChR antagonist. methyllycaconitine 67-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 18818999-1 2009 Phosphorylation of the nicotinic acetylcholine receptor (nAChR) is believed to play a critical role in its nicotine-induced desensitization and up-regulation. Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-55 18818999-1 2009 Phosphorylation of the nicotinic acetylcholine receptor (nAChR) is believed to play a critical role in its nicotine-induced desensitization and up-regulation. Nicotine 107-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 18818999-5 2009 Epibatidine binding revealed a three and sevenfold increase in surface expression for the alpha4S336A and alpha4S336D mutations, respectively, relative to wild-type, therefore, both mutations enhanced expression of the alpha4beta2 nAChR. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 231-236 19082523-8 2009 Including biochemical indicators of serum nicotine can help differentiate smoking- versus disease-associated changes in nAChR expression. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 19081250-4 2009 Initial analysis of the new compounds at 100 microM concentration reveal that the two pyrrole anabaseines are good partial agonists of the alpha7 nAChR, having 40% of the efficacy of ACh, efficacy comparable to 4OH-GTS-21, and dramatically enhanced efficacy relative to the 2- and 4-pyridinyl compounds. pyrrole anabaseines 86-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 19027295-2 2009 The carbamate functionality and a small hydrophobic substituent in the C-3 position were found to be vital for the binding affinity to the nAChRs, whereas the carbamate nitrogen substituents were important for nAChR subtype selectivity. Nitrogen 169-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 19436947-9 2009 The inhibition of these effects by D: -tubocurarine suggests that nicotine acts via the nicotinic acetylcholine receptor (nAChR). Tubocurarine 35-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-120 19499400-13 2009 In addition, mecamylamine, a non-selective antagonist of nicotinic acetylcholine receptors (nAchR), abrogated the effects of nicotine on EPC. Mecamylamine 13-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-90 19499400-13 2009 In addition, mecamylamine, a non-selective antagonist of nicotinic acetylcholine receptors (nAchR), abrogated the effects of nicotine on EPC. Mecamylamine 13-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 19499400-13 2009 In addition, mecamylamine, a non-selective antagonist of nicotinic acetylcholine receptors (nAchR), abrogated the effects of nicotine on EPC. Nicotine 125-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-90 19499400-13 2009 In addition, mecamylamine, a non-selective antagonist of nicotinic acetylcholine receptors (nAchR), abrogated the effects of nicotine on EPC. Nicotine 125-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 19499400-15 2009 In addition, the effects of nicotine might be specifically mediated by nAchR activation. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 19184647-2 2009 nAChR subtypes that are expressed in dopamine neurons, as well as neurons that interact with dopamine neurons (glutamatergic, GABAergic), serve as the focus of this review. Dopamine 37-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 25530665-4 2009 Epibatidine"s unique structure and potent activity made it an ideal lead structure for the development of nAChR ligands with reduced side effects and better nAChR subtype selectivity. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 25530665-4 2009 Epibatidine"s unique structure and potent activity made it an ideal lead structure for the development of nAChR ligands with reduced side effects and better nAChR subtype selectivity. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 25530665-2 2009 Future studies showed that epibatidine was an nAChR ligand with analgesic potency 200-400 times greater than that of morphine. epibatidine 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 18844224-11 2009 The proinvasive effects of nicotine were mediated via a nAChR, Src and calcium-dependent signaling pathway in breast cancer cells. Nicotine 27-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 19436947-9 2009 The inhibition of these effects by D: -tubocurarine suggests that nicotine acts via the nicotinic acetylcholine receptor (nAChR). Tubocurarine 35-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 19436947-9 2009 The inhibition of these effects by D: -tubocurarine suggests that nicotine acts via the nicotinic acetylcholine receptor (nAChR). Nicotine 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-120 19436947-9 2009 The inhibition of these effects by D: -tubocurarine suggests that nicotine acts via the nicotinic acetylcholine receptor (nAChR). Nicotine 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 18989912-3 2008 The high nAChR activity of carbamoylcholine analogue 5d was found to reside in its R-enantiomer, a characteristic most likely true for all other compounds in the series. Carbachol 27-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 18848895-3 2009 Loss of the SK2 gene also results in loss of electrically driven olivocochlear effects in vivo, and down regulation of ryanodine receptors involved in calcium-induced calcium release, the main inducer of nAChR evoked SK2 activity. Calcium 151-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 18848895-3 2009 Loss of the SK2 gene also results in loss of electrically driven olivocochlear effects in vivo, and down regulation of ryanodine receptors involved in calcium-induced calcium release, the main inducer of nAChR evoked SK2 activity. Calcium 167-174 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 19140954-4 2009 It is originally indicated that the key mediator of the cholinergic anti-inflammatory pathway, acetylcholine (ACh), inhibits cytokine release directly via the alpha7 nicotinic ACh receptor (nAChR) expressed on macrophages. Acetylcholine 95-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 19140954-4 2009 It is originally indicated that the key mediator of the cholinergic anti-inflammatory pathway, acetylcholine (ACh), inhibits cytokine release directly via the alpha7 nicotinic ACh receptor (nAChR) expressed on macrophages. Acetylcholine 110-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 19126755-3 2009 With the advancement of functional and genetic studies in the late 1980s, the existence of nAChRs in the mammalian brain was confirmed and the realization that the numerous nAChR subtypes contribute to the psychoactive properties of nicotine and other drugs of abuse and to the neuropathology of various diseases, including Alzheimer"s, Parkinson"s, and schizophrenia, has since emerged. Nicotine 233-241 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 18835908-0 2008 Behavioral differences between phosphatidic acid and phosphatidylcholine in the presence of the nicotinic acetylcholine receptor. Phosphatidic Acids 31-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-128 18835908-0 2008 Behavioral differences between phosphatidic acid and phosphatidylcholine in the presence of the nicotinic acetylcholine receptor. Phosphatidylcholines 53-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-128 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Phosphatidic Acids 57-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Phosphatidic Acids 57-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Phosphatidic Acids 76-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Phosphatidic Acids 76-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Cholesterol 91-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 18835908-1 2008 It has been found experimentally that negatively charged phosphatidic acid (PA) lipids and cholesterol molecules stabilize the nicotinic acetylcholine receptor (nAChR) in a functional resting state that can participate in an agonist-induced conformational change. Cholesterol 91-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 18835908-5 2008 This suggests that the PA domain may help stabilize the nAChR resting state. Phosphatidic Acids 23-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18723411-2 2008 The results indicate that chiral recognition on the alpha3beta4 nAChR is a process involving initial tethering of dextromethorphan and levomethorphan at hydrophobic pockets within the central lumen followed by hydrogen bonding interactions favoring dextromethorphan. Dextromethorphan 114-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 18519132-1 2008 BACKGROUND: A nonsynonymous coding polymorphism, rs16969968, of the CHRNA5 gene that encodes the alpha-5 subunit of the nicotinic acetylcholine receptor (nAChR) has been found to be associated with nicotine dependence. Nicotine 198-206 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 18534558-0 2008 Gene-gene interactions among CHRNA4, CHRNB2, BDNF, and NTRK2 in nicotine dependence. Nicotine 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-35 19040571-13 2008 Proliferation effects of nicotine could be blocked by inhibition of alpha7-nAChR by the high affinity ligand alpha-cobratoxin. Nicotine 25-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 18841955-1 2008 Potential nicotinic acetylcholine receptor (nAChR) ligands have been synthesized in which a methylisoxazole substituent is attached to the 1-position ( 26) of the 2-azabicyclo[2.1.1]hexane ring system or separated by "spacer" atoms ( 21 and 23). bucide 92-107 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 18841955-1 2008 Potential nicotinic acetylcholine receptor (nAChR) ligands have been synthesized in which a methylisoxazole substituent is attached to the 1-position ( 26) of the 2-azabicyclo[2.1.1]hexane ring system or separated by "spacer" atoms ( 21 and 23). 2-azabicyclo[2 163-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 18841955-1 2008 Potential nicotinic acetylcholine receptor (nAChR) ligands have been synthesized in which a methylisoxazole substituent is attached to the 1-position ( 26) of the 2-azabicyclo[2.1.1]hexane ring system or separated by "spacer" atoms ( 21 and 23). Hexanes 181-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 18571741-9 2008 This review will examine the genetic factors that alter susceptibility to nicotine addiction, with an emphasis on the genes that encode nAChR proteins. Nicotine 74-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 18851914-1 2008 A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. tetrakis-azaaromatic 12-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 18851914-1 2008 A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. quaternary ammonium salts 33-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 18851914-1 2008 A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. Nicotine 210-218 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 18851914-1 2008 A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. amsonic acid 226-228 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 19128201-4 2008 In this review, we will discuss the nAChR subtypes, their function in response to endogenous brain transmitters, and how their functions are regulated in the presence of nicotine. Nicotine 170-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 18991407-1 2008 The Torpedo nicotinic acetylcholine receptor (nAChR) is the only member of the Cys-loop superfamily of ligand-gated ion channels (LGICs) that is available in high abundance in a native membrane preparation. Cysteine 79-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-44 18991407-1 2008 The Torpedo nicotinic acetylcholine receptor (nAChR) is the only member of the Cys-loop superfamily of ligand-gated ion channels (LGICs) that is available in high abundance in a native membrane preparation. Cysteine 79-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 18805435-0 2008 Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induce cyclooxygenase-2 activity in human gastric cancer cells: Involvement of nicotinic acetylcholine receptor (nAChR) and beta-adrenergic receptor signaling pathways. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-171 18805435-0 2008 Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induce cyclooxygenase-2 activity in human gastric cancer cells: Involvement of nicotinic acetylcholine receptor (nAChR) and beta-adrenergic receptor signaling pathways. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 18805435-0 2008 Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induce cyclooxygenase-2 activity in human gastric cancer cells: Involvement of nicotinic acetylcholine receptor (nAChR) and beta-adrenergic receptor signaling pathways. 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone 13-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-171 18805435-0 2008 Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induce cyclooxygenase-2 activity in human gastric cancer cells: Involvement of nicotinic acetylcholine receptor (nAChR) and beta-adrenergic receptor signaling pathways. 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone 13-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 18805435-4 2008 We found that nicotine and NNK significantly enhanced cell proliferation in AGS cells that expressed both alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) and beta-adrenergic receptors. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-145 18805435-4 2008 We found that nicotine and NNK significantly enhanced cell proliferation in AGS cells that expressed both alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) and beta-adrenergic receptors. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 19032090-1 2008 Agonists and antagonists of the nicotinic acetylcholine receptor (nAChR) are used to treat nicotine addiction, neuromuscular disorders, and neurological diseases. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-64 19032090-1 2008 Agonists and antagonists of the nicotinic acetylcholine receptor (nAChR) are used to treat nicotine addiction, neuromuscular disorders, and neurological diseases. Nicotine 91-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 19032090-3 2008 Previous studies have shown that cation-pi interactions at the transmitter binding sites of the nAChR are important for receptor activation by strong agonists such as acetylcholine. Acetylcholine 167-180 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 18723411-2 2008 The results indicate that chiral recognition on the alpha3beta4 nAChR is a process involving initial tethering of dextromethorphan and levomethorphan at hydrophobic pockets within the central lumen followed by hydrogen bonding interactions favoring dextromethorphan. Dextromethorphan 135-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 18723411-2 2008 The results indicate that chiral recognition on the alpha3beta4 nAChR is a process involving initial tethering of dextromethorphan and levomethorphan at hydrophobic pockets within the central lumen followed by hydrogen bonding interactions favoring dextromethorphan. Hydrogen 210-218 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 18723411-2 2008 The results indicate that chiral recognition on the alpha3beta4 nAChR is a process involving initial tethering of dextromethorphan and levomethorphan at hydrophobic pockets within the central lumen followed by hydrogen bonding interactions favoring dextromethorphan. Dextromethorphan 249-265 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 18678621-1 2008 The alpha7 nicotinic acetylcholine receptor (nAChR), a homopentameric, rapidly activating and desensitizing ligand-gated ion channel with relatively high degree of calcium permeability, is expressed in the mammalian central nervous system, including regions associated with cognitive processing. Calcium 164-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 18826295-1 2008 Extensive molecular docking, molecular dynamics simulations, and binding free energy calculations have been performed to understand how alpha7-specific agonists of nicotinic acetylcholine receptor (nAChR), including AR-R17779 (1), GTS-21 (4), and 4-OH-GTS-21 (5), interact with the alpha7 receptor, leading to important new insights into the receptor-agonist binding. 4-oh 247-251 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-196 18826295-1 2008 Extensive molecular docking, molecular dynamics simulations, and binding free energy calculations have been performed to understand how alpha7-specific agonists of nicotinic acetylcholine receptor (nAChR), including AR-R17779 (1), GTS-21 (4), and 4-OH-GTS-21 (5), interact with the alpha7 receptor, leading to important new insights into the receptor-agonist binding. 4-oh 247-251 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 198-203 18922921-7 2008 Importantly, on nicotine treatment, the mobility of MCF10A and MCF7 cells is enhanced, which can be blocked by the addition of nAChR or PKC inhibitor. Nicotine 16-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 18852456-7 2008 Pretreatment with mecamylamine (6 micromol/kg s.c.), an nAChR blocker that penetrates the blood-brain barrier, prevents the nicotine-induced decrease of FC DNMT1 expression. Mecamylamine 18-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18852456-7 2008 Pretreatment with mecamylamine (6 micromol/kg s.c.), an nAChR blocker that penetrates the blood-brain barrier, prevents the nicotine-induced decrease of FC DNMT1 expression. Nicotine 124-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18805006-1 2008 The synthesis and structure-activity relationship of a series of carbamate potentiators of alpha4beta2 nAChR is reported herein. Carbamates 65-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 20040957-10 2008 Nicotine, through stimulating alpha4beta2 nAChR, releases dopamine in the reward pathway. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 20040957-10 2008 Nicotine, through stimulating alpha4beta2 nAChR, releases dopamine in the reward pathway. Dopamine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 20040957-11 2008 Partial agonist of alpha4beta2 nAChR elicits moderate and sustained release of dopamine, which is countered during the cessation attempts; it simultaneously blocks the effects of nicotine by binding with alpha4beta2 receptors during smoking. Dopamine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 20040957-11 2008 Partial agonist of alpha4beta2 nAChR elicits moderate and sustained release of dopamine, which is countered during the cessation attempts; it simultaneously blocks the effects of nicotine by binding with alpha4beta2 receptors during smoking. Nicotine 179-187 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 20040957-12 2008 Recently, varenicline, a partial agonist at alpha4beta2 nAChR, has been approved by the FDA (Food and Drug Administration) for smoking cessation. Varenicline 10-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18762859-2 2008 The majority of high affinity nicotine binding sites in the human brain have been implicated in heteropentameric alpha4 and beta2 subunits of neuronal nicotinic acetylcholine receptors; therefore, these two neuronal nicotinic acetylcholine receptors genes (CHRNA4 and CHRNB2) are considered to be attractive candidate genes for the pathophysiology of schizophrenia. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 257-263 18607650-1 2008 In recent years, it has become clear that the neuronal nicotinic acetylcholine receptor (nAChR) is a valid target in the treatment of a variety of diseases, including Alzheimer"s disease, anxiety, and nicotine addiction. Nicotine 201-209 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 18607650-1 2008 In recent years, it has become clear that the neuronal nicotinic acetylcholine receptor (nAChR) is a valid target in the treatment of a variety of diseases, including Alzheimer"s disease, anxiety, and nicotine addiction. Nicotine 201-209 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 18607650-3 2008 Based on a high-resolution crystal structure of AChBP, homology models of the extracellular domain of the neuronal rat and human nAChR subtypes alpha4beta2 and alpha7 (the subtypes most abundant in brain) were built, and their stability assessed with molecular dynamics (MD). achbp 48-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 18768796-0 2008 Embedded cholesterol in the nicotinic acetylcholine receptor. Cholesterol 9-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-60 18606871-4 2008 Because nonhuman primates are evolutionarily closer to humans and may better model the effects of pesticide exposure in man, we examined the effects of paraquat on striatal nAChR function and expression in monkeys. Paraquat 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 18606871-7 2008 Paraquat treatment decreased alpha4beta2(*) but not alpha3/alpha6beta2(*) nAChR expression. Paraquat 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 18606871-8 2008 The differential effects of paraquat on nAChR expression and receptor-evoked [(3)H]DA release emphasize the importance of evaluating changes in functional measures. Paraquat 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 18754612-8 2008 Docking simulations identified several hydrogen bonds lost upon truncation that provide an explanation for the reduced affinities observed at the alpha7 nAChR and AChBP. Hydrogen 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 18754612-8 2008 Docking simulations identified several hydrogen bonds lost upon truncation that provide an explanation for the reduced affinities observed at the alpha7 nAChR and AChBP. achbp 163-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 18768796-3 2008 Purified nAChR must be reconstituted in a mixture containing cholesterol to function. Cholesterol 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 18768796-5 2008 However, the underlying cause of nAChR sensitivity to cholesterol remains controversial, in part because the vast majority of functional studies were conducted before a medium resolution structure was reported. Cholesterol 54-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 18768796-6 2008 We show that the nAChR contains internal sites capable of containing cholesterol, whose occupation stabilizes the protein structure. Cholesterol 69-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 23506178-7 2008 In addition, the neuronal nAChR partial agonist varenicline recently received regulatory approval for use in smoking cessation. Varenicline 48-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 18618000-2 2008 We tested the hypothesis that associations between nicotinic acetylcholine receptor (nAChR) genetic variants and nicotine dependence assessed in adulthood will be stronger among smokers who began daily nicotine exposure during adolescence. Nicotine 113-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-83 18718366-1 2008 Nicotine is a major component of tobacco smoke, and signals via nicotinic acetylcholine receptors (nAChR). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 18718366-8 2008 These results indicate that nicotine suppresses the cytodifferentiation and mineralization of HDPCs, possibly via nAChR. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 18620875-3 2008 This study aimed to; (1) quantify nAChR distribution in vivo with 2-[18F]fluoro-A-85380 (2-FA) in 15 early AD patients compared to 14 age-matched, healthy controls (HC) and (2) correlate nAChR distribution with cognitive performance in both groups. 2-fluoro-3-(2-azetidinylmethoxy)pyridine 66-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 18620875-3 2008 This study aimed to; (1) quantify nAChR distribution in vivo with 2-[18F]fluoro-A-85380 (2-FA) in 15 early AD patients compared to 14 age-matched, healthy controls (HC) and (2) correlate nAChR distribution with cognitive performance in both groups. 2-fluoro-3-(2-azetidinylmethoxy)pyridine 89-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 18602458-3 2008 ACh dose-dependently evoked an alpha9alpha10 nAChR-mediated ion current with an EC(50) of 137 microM. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 18602458-4 2008 When ACh is applied at a low concentration (10 microM), the nAChR-mediated ion current is inhibited by a low concentration (10 microM) of ethylbenzene and p-xylene, but not by the same concentration of the non-ototoxic solvents. Acetylcholine 5-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 18602458-4 2008 When ACh is applied at a low concentration (10 microM), the nAChR-mediated ion current is inhibited by a low concentration (10 microM) of ethylbenzene and p-xylene, but not by the same concentration of the non-ototoxic solvents. ethylbenzene 138-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 18602458-4 2008 When ACh is applied at a low concentration (10 microM), the nAChR-mediated ion current is inhibited by a low concentration (10 microM) of ethylbenzene and p-xylene, but not by the same concentration of the non-ototoxic solvents. 4-xylene 155-163 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 18602458-7 2008 These results demonstrate that low concentrations of the known ototoxic solvents ethylbenzene and p-xylene inhibit alpha9alpha10 nAChR-mediated ion currents, whereas the structurally related, non-ototoxic solvents m-xylene and o-xylene do not, indicating that the alpha9alpha10 nAChR is a potential target for solvent-induced ototoxicity. ethylbenzene 81-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 18602458-7 2008 These results demonstrate that low concentrations of the known ototoxic solvents ethylbenzene and p-xylene inhibit alpha9alpha10 nAChR-mediated ion currents, whereas the structurally related, non-ototoxic solvents m-xylene and o-xylene do not, indicating that the alpha9alpha10 nAChR is a potential target for solvent-induced ototoxicity. ethylbenzene 81-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 278-283 18602458-7 2008 These results demonstrate that low concentrations of the known ototoxic solvents ethylbenzene and p-xylene inhibit alpha9alpha10 nAChR-mediated ion currents, whereas the structurally related, non-ototoxic solvents m-xylene and o-xylene do not, indicating that the alpha9alpha10 nAChR is a potential target for solvent-induced ototoxicity. 4-xylene 98-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 18602458-7 2008 These results demonstrate that low concentrations of the known ototoxic solvents ethylbenzene and p-xylene inhibit alpha9alpha10 nAChR-mediated ion currents, whereas the structurally related, non-ototoxic solvents m-xylene and o-xylene do not, indicating that the alpha9alpha10 nAChR is a potential target for solvent-induced ototoxicity. 4-xylene 98-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 278-283 18602458-7 2008 These results demonstrate that low concentrations of the known ototoxic solvents ethylbenzene and p-xylene inhibit alpha9alpha10 nAChR-mediated ion currents, whereas the structurally related, non-ototoxic solvents m-xylene and o-xylene do not, indicating that the alpha9alpha10 nAChR is a potential target for solvent-induced ototoxicity. 2-xylene 227-235 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 18524766-2 2008 We report here that TDBzl-etomidate, a photoreactive etomidate analog, acts as a positive allosteric nAChR modulator rather than an inhibitor, and we identify its binding sites by photoaffinity labeling. 4-(3-(trifluoromethyl)-3H-diazirin-3-yl)benzyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate 20-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 18524766-2 2008 We report here that TDBzl-etomidate, a photoreactive etomidate analog, acts as a positive allosteric nAChR modulator rather than an inhibitor, and we identify its binding sites by photoaffinity labeling. Etomidate 26-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 18524766-4 2008 At higher concentrations, it inhibited the binding of the noncompetitive antagonists [(3)H]tetracaine and [(3)H]phencyclidine to Torpedo nAChR-rich membranes (IC(50) values of 0. [(3)h]tetracaine 85-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 18524766-4 2008 At higher concentrations, it inhibited the binding of the noncompetitive antagonists [(3)H]tetracaine and [(3)H]phencyclidine to Torpedo nAChR-rich membranes (IC(50) values of 0. [(3)h]phencyclidine 106-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 18524766-6 2008 nAChR-rich membranes were photolabeled with [(3)H]TDBzl-etomidate, and labeled amino acids were identified by Edman degradation. [(3)h]tdbzl-etomidate 44-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 18524766-8 2008 In addition, there was labeling in gammaM3 (gammaMet-299), a residue that contributes to the same pocket in the nAChR structure as alphaM2-10. gammamet-299 44-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 18524766-9 2008 The pharmacological specificity of labeling of residues, together with their locations in the nAChR structure, indicate that TDBzl-etomidate binds at two distinct sites: one within the lumen of the ion channel (labeling of M2-9 and -13), an inhibitory site, and another at the interface between the alpha and gamma subunits (labeling of alphaM2-10 and gammaMet-299) likely to be a site for positive allosteric modulation. 4-(3-(trifluoromethyl)-3H-diazirin-3-yl)benzyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate 125-140 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 18448488-9 2008 We conclude that through nAChR and beta-adrenoceptors, nicotine activates ERK1/2 and Stat3 signaling pathways, leading to Cyclin D1 expression and cell proliferation. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 19094587-2 2008 METHODS: The siRNA coding oligonucleotide sequences targeting alpha 3 nAChR were designed and synthesized. Oligonucleotides 26-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 19094587-7 2008 RESULTS: Compared with the controls, the expression levels of mRNA and protein in the stable SH-SY5Y clone cells transfected with the recombinant alpha 3 nAChR pSilencer 3.1-H1 neo vector were decreased with inhibitory efficiency of 98% and 66%, respectively, the MTT reduction decreased; the product of lipid peroxidation was increased and the activities of SOD and GSH-px were decreased. monooxyethylene trimethylolpropane tristearate 264-267 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 19094587-7 2008 RESULTS: Compared with the controls, the expression levels of mRNA and protein in the stable SH-SY5Y clone cells transfected with the recombinant alpha 3 nAChR pSilencer 3.1-H1 neo vector were decreased with inhibitory efficiency of 98% and 66%, respectively, the MTT reduction decreased; the product of lipid peroxidation was increased and the activities of SOD and GSH-px were decreased. gsh-px 367-373 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 19094587-9 2008 CONCLUSIONS: The expression inhibition of alpha 3 nAChR as a result of recombinant alpha 3 nAChR siRNA can induce oxidative stress and improve the toxicity of Abeta on SH-SY5Y cells, indicating that alpha 3 nAChR may play a significant neuroprotective role in the pathogenesis of Alzheimer disease. UNII-042A8N37WH 159-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 19094587-9 2008 CONCLUSIONS: The expression inhibition of alpha 3 nAChR as a result of recombinant alpha 3 nAChR siRNA can induce oxidative stress and improve the toxicity of Abeta on SH-SY5Y cells, indicating that alpha 3 nAChR may play a significant neuroprotective role in the pathogenesis of Alzheimer disease. UNII-042A8N37WH 159-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 19094587-9 2008 CONCLUSIONS: The expression inhibition of alpha 3 nAChR as a result of recombinant alpha 3 nAChR siRNA can induce oxidative stress and improve the toxicity of Abeta on SH-SY5Y cells, indicating that alpha 3 nAChR may play a significant neuroprotective role in the pathogenesis of Alzheimer disease. UNII-042A8N37WH 159-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 20641651-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20641651-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20641651-8 2004 A-85380 has also been labeled as 5-[(123)I]iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-[(123)I]iodo-A-85380 (5-[(123)I]IA)), which has been developed as a single-photon emission computed tomography (SPECT) agent for the non-invasive study of nAChR in the brain. iodo 43-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 243-248 20641651-8 2004 A-85380 has also been labeled as 5-[(123)I]iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-[(123)I]iodo-A-85380 (5-[(123)I]IA)), which has been developed as a single-photon emission computed tomography (SPECT) agent for the non-invasive study of nAChR in the brain. 3-[2(s)-2-azetidinylmethoxy]pyridine 48-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 243-248 20641651-10 2004 Norchloro-fluoro-homoepibatidine (NCFHEB), an analog of epibatidine, is a highly potent and selective alpha4beta2 nAChR antagonist with subnanomolar affinity (6). fluoronorchloroepibatidine 0-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 20641651-10 2004 Norchloro-fluoro-homoepibatidine (NCFHEB), an analog of epibatidine, is a highly potent and selective alpha4beta2 nAChR antagonist with subnanomolar affinity (6). fluoronorchloroepibatidine 34-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 20641651-10 2004 Norchloro-fluoro-homoepibatidine (NCFHEB), an analog of epibatidine, is a highly potent and selective alpha4beta2 nAChR antagonist with subnanomolar affinity (6). epibatidine 21-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 18605717-0 2008 Discovery of (-)-7-methyl-2-exo-[3"-(6-[18F]fluoropyridin-2-yl)-5"-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties. (-)-7-methyl-2-exo-[3"-(6-[18f]fluoropyridin-2-yl)-5"-pyridinyl]-7-azabicyclo[2.2.1]heptane 13-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 18618000-2 2008 We tested the hypothesis that associations between nicotinic acetylcholine receptor (nAChR) genetic variants and nicotine dependence assessed in adulthood will be stronger among smokers who began daily nicotine exposure during adolescence. Nicotine 113-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 18618000-2 2008 We tested the hypothesis that associations between nicotinic acetylcholine receptor (nAChR) genetic variants and nicotine dependence assessed in adulthood will be stronger among smokers who began daily nicotine exposure during adolescence. Nicotine 202-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-83 18618000-2 2008 We tested the hypothesis that associations between nicotinic acetylcholine receptor (nAChR) genetic variants and nicotine dependence assessed in adulthood will be stronger among smokers who began daily nicotine exposure during adolescence. Nicotine 202-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 18596163-1 2008 The alpha4beta2 subtype is the most abundant nicotinic acetylcholine receptor (nAChR) in the brain and possesses the high-affinity binding site for nicotine. Nicotine 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 18596163-2 2008 The alpha4 and beta2 nAChR subunits assemble into two alternate stoichiometries, (alpha4)(2)(beta2)(3) and (alpha4)(3)(beta2)(2), which differ in their functional properties and sensitivity to chronic exposure to nicotine. Nicotine 213-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 18649634-6 2008 While, a voltage change evoked by binding of acetylcholine to nAChR leads to down-regulate fetal nAChR expression in extrasynaptic nuclei. Acetylcholine 45-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 18343642-0 2008 Alpha-conotoxin MII-sensitive nicotinic acetylcholine receptors are involved in mediating the ghrelin-induced locomotor stimulation and dopamine overflow in nucleus accumbens. Ghrelin 94-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-63 18343642-0 2008 Alpha-conotoxin MII-sensitive nicotinic acetylcholine receptors are involved in mediating the ghrelin-induced locomotor stimulation and dopamine overflow in nucleus accumbens. Dopamine 136-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-63 18343642-1 2008 Previously, we have reported that the orexigenic peptide ghrelin activates the cholinergic-dopaminergic reward link, involving nicotinic acetylcholine receptors (nAChR). Ghrelin 57-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-160 18343642-1 2008 Previously, we have reported that the orexigenic peptide ghrelin activates the cholinergic-dopaminergic reward link, involving nicotinic acetylcholine receptors (nAChR). Ghrelin 57-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 18343642-3 2008 The present experiments show that the locomotor stimulatory effects of ghrelin, either into laterodorsal tegmental area (LDTg) or ventral tegmental area (VTA), are mediated via ventral tegmental nAChR, but neither the alpha(4)beta(2) (using dihydro-beta-erythroidine) nor the alpha(7) (using methyllycaconitine) subtypes appears to be involved. Ghrelin 71-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 18343642-3 2008 The present experiments show that the locomotor stimulatory effects of ghrelin, either into laterodorsal tegmental area (LDTg) or ventral tegmental area (VTA), are mediated via ventral tegmental nAChR, but neither the alpha(4)beta(2) (using dihydro-beta-erythroidine) nor the alpha(7) (using methyllycaconitine) subtypes appears to be involved. Dihydro-beta-Erythroidine 241-266 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 18343642-3 2008 The present experiments show that the locomotor stimulatory effects of ghrelin, either into laterodorsal tegmental area (LDTg) or ventral tegmental area (VTA), are mediated via ventral tegmental nAChR, but neither the alpha(4)beta(2) (using dihydro-beta-erythroidine) nor the alpha(7) (using methyllycaconitine) subtypes appears to be involved. methyllycaconitine 292-310 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 18369179-7 2008 Perfusion of the nAChR antagonist mecamylamine in the anterior VTA completely blocked the elevation of accumbal dopamine levels observed after ethanol perfusion in nAc, whereas mecamylamine in the posterior VTA had no effect. Mecamylamine 34-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 18369179-7 2008 Perfusion of the nAChR antagonist mecamylamine in the anterior VTA completely blocked the elevation of accumbal dopamine levels observed after ethanol perfusion in nAc, whereas mecamylamine in the posterior VTA had no effect. Dopamine 112-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 18369179-7 2008 Perfusion of the nAChR antagonist mecamylamine in the anterior VTA completely blocked the elevation of accumbal dopamine levels observed after ethanol perfusion in nAc, whereas mecamylamine in the posterior VTA had no effect. Ethanol 143-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 18649634-6 2008 While, a voltage change evoked by binding of acetylcholine to nAChR leads to down-regulate fetal nAChR expression in extrasynaptic nuclei. Acetylcholine 45-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 18325740-2 2008 We investigated the effects of the acetylcholinesterase inhibitor and allosteric nAChR modulator, galantamine, on cognitive performance and clinical symptoms when added to a stable antipsychotic medication regimen in nonsmoking outpatients with schizophrenia in a double-blind, placebo-controlled, parallel-group design. Galantamine 98-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 18559515-6 2008 Partially explaining the cholinergic up-regulation seen in SCC, incubation of the H520 SCC cell line with nicotine increased levels of ACh secretion, increased expression of nAChR, and, as measured by electrophysiologic recording, increased activity of the expressed nAChR. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 18559515-6 2008 Partially explaining the cholinergic up-regulation seen in SCC, incubation of the H520 SCC cell line with nicotine increased levels of ACh secretion, increased expression of nAChR, and, as measured by electrophysiologic recording, increased activity of the expressed nAChR. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 267-272 20641602-6 2004 3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 18208544-4 2008 In contrast, isoforms containing an additional exon (exon 2), which is located within a proline-rich N-terminal region, have a greatly reduced ability to enhance nAChR maturation. Proline 88-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 18282683-5 2008 In addition, inhibition of alpha 7 nAChR at protein level was observed in the cells exposed to high amounts of fluoride or ferrous iron. Fluorides 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 18282683-5 2008 In addition, inhibition of alpha 7 nAChR at protein level was observed in the cells exposed to high amounts of fluoride or ferrous iron. Iron 123-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 20641785-6 2004 3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20641785-6 2004 3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 19492010-3 2008 Recent work from human genetics studies has provided evidence that neuronal nicotinic acetylcholine receptors (nAChR) genes may have a role in mediating early behaviors that are risk factors for alcohol and nicotine dependence, such as age of initiation and early subjective responses to the drugs. Alcohols 195-202 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-109 19492010-3 2008 Recent work from human genetics studies has provided evidence that neuronal nicotinic acetylcholine receptors (nAChR) genes may have a role in mediating early behaviors that are risk factors for alcohol and nicotine dependence, such as age of initiation and early subjective responses to the drugs. Alcohols 195-202 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 19492010-3 2008 Recent work from human genetics studies has provided evidence that neuronal nicotinic acetylcholine receptors (nAChR) genes may have a role in mediating early behaviors that are risk factors for alcohol and nicotine dependence, such as age of initiation and early subjective responses to the drugs. Nicotine 207-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-109 19492010-3 2008 Recent work from human genetics studies has provided evidence that neuronal nicotinic acetylcholine receptors (nAChR) genes may have a role in mediating early behaviors that are risk factors for alcohol and nicotine dependence, such as age of initiation and early subjective responses to the drugs. Nicotine 207-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 18262434-4 2008 In synthesis Ach via nAChR or mAChR appears to be involved in the regulation of vital cell functions: proliferation, differentiation, organization of the cytoskeleton, cell-cell contact, ciliary activity, migration, secretion and absorption of ions, water and mucus. Acetylcholine 13-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 18262434-4 2008 In synthesis Ach via nAChR or mAChR appears to be involved in the regulation of vital cell functions: proliferation, differentiation, organization of the cytoskeleton, cell-cell contact, ciliary activity, migration, secretion and absorption of ions, water and mucus. Water 250-255 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 18363376-0 2008 Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands. 2-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane 105-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-199 18363376-1 2008 In an attempt to generate nicotinic acetylcholine receptor (nAChR) ligands selective for the alpha4beta2 and alpha7 subtype receptors we designed and synthesized constrained versions of anabasine, a naturally occurring nAChR ligand. Anabasine 186-195 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-58 18363376-1 2008 In an attempt to generate nicotinic acetylcholine receptor (nAChR) ligands selective for the alpha4beta2 and alpha7 subtype receptors we designed and synthesized constrained versions of anabasine, a naturally occurring nAChR ligand. Anabasine 186-195 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 18363376-1 2008 In an attempt to generate nicotinic acetylcholine receptor (nAChR) ligands selective for the alpha4beta2 and alpha7 subtype receptors we designed and synthesized constrained versions of anabasine, a naturally occurring nAChR ligand. Anabasine 186-195 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 219-224 18385335-4 2008 The nAChR antagonist mecamylamine attenuated the cholinergic signals evoked by either compound. Mecamylamine 21-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 18385335-5 2008 Cholinergic signals evoked by ABT-089 were more efficaciously attenuated by the relatively beta2*-selective nAChR antagonist dihydro-beta-erythroidine. pozanicline 30-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 18385335-5 2008 Cholinergic signals evoked by ABT-089 were more efficaciously attenuated by the relatively beta2*-selective nAChR antagonist dihydro-beta-erythroidine. Dihydro-beta-Erythroidine 125-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 18342165-3 2008 Varenicline is the first in a new class of agents for smoking cessation, the alpha(4)beta(2) nicotinic acetylcholine receptor (nAChR) partial agonists. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 18342165-5 2008 As a nAChR partial agonist, varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 20641602-6 2004 3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 18298895-9 2008 Hump currents blocked by the alpha4beta2-nAChR antagonist dihydro-beta-erythroidine were reduced when alpha4beta2-nAChR were desensitized, and were more pronounced in the absence of external Ca2+. Dihydro-beta-Erythroidine 58-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 18385094-5 2008 METHODS: The effect of the nonselective nAChR antagonist mecamylamine was tested on human retinal and choroidal endothelial cells in vitro and in a murine model of CNV. Mecamylamine 57-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 18348519-8 2008 In particular, normal-mode analysis revealed that cobratoxin binding to this protein significantly dampened the axially symmetric motion of the AChBP that may be associated with channel gating in the full nAChR. achbp 144-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 18298895-9 2008 Hump currents blocked by the alpha4beta2-nAChR antagonist dihydro-beta-erythroidine were reduced when alpha4beta2-nAChR were desensitized, and were more pronounced in the absence of external Ca2+. Dihydro-beta-Erythroidine 58-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 18037926-11 2008 A greater understanding of nAChR form and function is imperative to guide the design of ligands with subtype-selective efficacy for improved therapeutic interventions in nicotine addiction as well as Parkinson"s disease. Nicotine 170-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 18037926-7 2008 We will also review how nicotine, acting via nAChR desensitization, promotes the sensitivity of dopamine synapses to activity. Nicotine 24-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 17993502-1 2008 The molecular basis of anesthetic interaction with membrane proteins has been explored via determination of anesthetic effects on the structure and dynamics of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit in dodecylphosphocholine (DPC) micelles by (1)H and (15)N solution-state NMR. dodecylphosphocholine 290-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 230-262 17993502-1 2008 The molecular basis of anesthetic interaction with membrane proteins has been explored via determination of anesthetic effects on the structure and dynamics of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit in dodecylphosphocholine (DPC) micelles by (1)H and (15)N solution-state NMR. dodecylphosphocholine 290-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 264-269 17993502-1 2008 The molecular basis of anesthetic interaction with membrane proteins has been explored via determination of anesthetic effects on the structure and dynamics of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit in dodecylphosphocholine (DPC) micelles by (1)H and (15)N solution-state NMR. dodecylphosphocholine 313-316 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 230-262 17993502-1 2008 The molecular basis of anesthetic interaction with membrane proteins has been explored via determination of anesthetic effects on the structure and dynamics of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit in dodecylphosphocholine (DPC) micelles by (1)H and (15)N solution-state NMR. dodecylphosphocholine 313-316 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 264-269 18088060-4 2008 Thus, the authors developed [(18)F]norchloro-fluoro-homoepibatidine ([(18)F]NCFHEB) for nAChR imaging. fluoronorchloroepibatidine 35-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 18228017-7 2008 Because of the extraordinary long acquisition time with 2-[(18)F]F-A-85380, we developed the new alpha4beta2 nAChR-specific radioligands (+)- and (-)-[(18)F]norchloro-fluoro-homoepibatidine (NCFHEB) and evaluated them preclinically. fluoronorchloroepibatidine 157-189 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Tetracaine 56-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Tetracaine 56-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 299-304 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Phosphatidylcholines 194-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Phosphatidic Acids 254-271 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Phosphatidic Acids 342-359 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 18055762-2 2008 Infrared difference spectra show that concentrations of tetracaine consistent with binding to the ion channel (<50 microM) stabilize a resting-like state when the nAChR is reconstituted into phosphatidylcholine membranes containing the anionic lipid, phosphatidic acid, but have no effect on the nAChR reconstituted into membranes lacking phosphatidic acid, either in the presence or absence of cholesterol. Cholesterol 398-409 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 18055762-6 2008 However, subtle membrane-dependent variations in the vibrations of tyrosine and tryptophan residues, and agonist analog binding studies indicate that the structures of the agonist-bound neurotransmitter sites of the nAChR in membranes lacking both phosphatidic acid and cholesterol differ from the structures of the agonist-desensitized neurotransmitter sites in the presence of both lipids. Tyrosine 67-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 216-221 18055762-6 2008 However, subtle membrane-dependent variations in the vibrations of tyrosine and tryptophan residues, and agonist analog binding studies indicate that the structures of the agonist-bound neurotransmitter sites of the nAChR in membranes lacking both phosphatidic acid and cholesterol differ from the structures of the agonist-desensitized neurotransmitter sites in the presence of both lipids. Tryptophan 80-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 216-221 18055762-6 2008 However, subtle membrane-dependent variations in the vibrations of tyrosine and tryptophan residues, and agonist analog binding studies indicate that the structures of the agonist-bound neurotransmitter sites of the nAChR in membranes lacking both phosphatidic acid and cholesterol differ from the structures of the agonist-desensitized neurotransmitter sites in the presence of both lipids. Phosphatidic Acids 248-265 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 216-221 18055762-6 2008 However, subtle membrane-dependent variations in the vibrations of tyrosine and tryptophan residues, and agonist analog binding studies indicate that the structures of the agonist-bound neurotransmitter sites of the nAChR in membranes lacking both phosphatidic acid and cholesterol differ from the structures of the agonist-desensitized neurotransmitter sites in the presence of both lipids. Cholesterol 270-281 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 216-221 18088060-13 2008 Continuous administration of the nAChR agonist A81418 inhibited the specific binding of (-)- and (+)-[(18)F]NCFHEB but not of 2-[(18)F]F-A85380. 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 47-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 18083118-0 2008 Epibatidine binds to four sites on the Torpedo nicotinic acetylcholine receptor. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-79 18248893-10 2008 These results suggested that nicotine could modulate the immune balance to Th1-dominant via nAChR in the intestine, to improve Th2-type enteritis. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 18305393-4 2008 Nicotine inhibited ROS generation in fAbeta(1-42)-stimulated microglial cells, and this inhibition was blocked by mecamylamine, a non-selective nAChR antagonist, and a-bungarotoxin, a selective alpha7 nAChR antagonist. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 18305393-4 2008 Nicotine inhibited ROS generation in fAbeta(1-42)-stimulated microglial cells, and this inhibition was blocked by mecamylamine, a non-selective nAChR antagonist, and a-bungarotoxin, a selective alpha7 nAChR antagonist. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 201-206 18305393-4 2008 Nicotine inhibited ROS generation in fAbeta(1-42)-stimulated microglial cells, and this inhibition was blocked by mecamylamine, a non-selective nAChR antagonist, and a-bungarotoxin, a selective alpha7 nAChR antagonist. Mecamylamine 114-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 18305393-4 2008 Nicotine inhibited ROS generation in fAbeta(1-42)-stimulated microglial cells, and this inhibition was blocked by mecamylamine, a non-selective nAChR antagonist, and a-bungarotoxin, a selective alpha7 nAChR antagonist. Mecamylamine 114-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 201-206 18248893-0 2008 Chronic nicotine stimulation modulates the immune response of mucosal T cells to Th1-dominant pattern via nAChR by upregulation of Th1-specific transcriptional factor. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 18083118-3 2008 Here we demonstrate directly that each Torpedo nAChR carries at least four binding sites for the potent neuronal nAChR agonist, epibatidine, i.e., twice as many sites as for alpha-bungarotoxin. epibatidine 128-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 18083118-3 2008 Here we demonstrate directly that each Torpedo nAChR carries at least four binding sites for the potent neuronal nAChR agonist, epibatidine, i.e., twice as many sites as for alpha-bungarotoxin. epibatidine 128-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 17942622-7 2007 We also found that a mixture of nAChR subtypes underlies the synaptic modulation in SNc, further distinguishing this nucleus from the VTA, where alpha7 nAChRs enhance glutamate inputs and non-alpha7 receptors enhance GABA inputs. Glutamic Acid 167-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 18005395-8 2008 nAChR expression increases when cells are chronically exposed to either selective antagonists or agonists such as nicotine, a protocol mimicking the condition of chronic heavy smokers. Nicotine 114-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 17977823-3 2008 We find that up-regulation of [(3)H]epibatidine binding and function in HEK293 cells stably expressing alpha4beta2-nAChR is significantly enhanced by co-application of the proinflammatory cytokine, tumor necrosis factor alpha. epibatidine 36-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 18296273-0 2008 Ultrastructural visualization of the transmembranous and cytomatrix-related part of nicotinic acetylcholine receptor of frog motor endplate by means of an immunochemical avidity of IgG for d-tubocurarine. Tubocurarine 189-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-116 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 123-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 123-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 123-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 139-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 139-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. Tubocurarine 139-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. quaternary ammonium 148-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. quaternary ammonium 148-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 18296273-1 2008 In the present study, a fine ultrastructural localization of nicotinic acetylcholine receptor (nAChR) was attempted, using d-tubocurarine (d-TC), a quaternary ammonium compound binding to nAChR. quaternary ammonium 148-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 18296273-11 2008 These cytochemical results confirm that d-TC binds to ACh binding sites in the pore of nAChR, and raise the question of DAB staining of cytoskeletal proteins related to the nAChR complex. Tubocurarine 40-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 18296273-11 2008 These cytochemical results confirm that d-TC binds to ACh binding sites in the pore of nAChR, and raise the question of DAB staining of cytoskeletal proteins related to the nAChR complex. Acetylcholine 54-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 17986233-8 2008 These results suggest that [(18)F]NIDA522131 is a promising positron emission tomography radioligand for studying extrathalamic nAChR in humans. nida522131 34-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-133 17959745-8 2008 The use of a alpha7/5-hydroxytryptamine type-3 chimera revealed that the N-terminal domain of alpha7 nAChR was sufficient to faithfully reproduce the pharmacology of [(3)H]A-585539 binding. Serotonin 22-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 18225945-3 2008 To address the mechanical fundamentals of nAChR gating, both conventional molecular dynamics (CMD) and steered rotation molecular dynamics (SRMD) simulations have been conducted on the cryo-electron microscopy (cryo-EM) structure of nAChR embedded in a dipalmitoylphosphatidylcholine (DPPC) bilayer and water molecules. 1,2-Dipalmitoylphosphatidylcholine 253-283 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 18225945-3 2008 To address the mechanical fundamentals of nAChR gating, both conventional molecular dynamics (CMD) and steered rotation molecular dynamics (SRMD) simulations have been conducted on the cryo-electron microscopy (cryo-EM) structure of nAChR embedded in a dipalmitoylphosphatidylcholine (DPPC) bilayer and water molecules. 1,2-Dipalmitoylphosphatidylcholine 285-289 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 18225945-3 2008 To address the mechanical fundamentals of nAChR gating, both conventional molecular dynamics (CMD) and steered rotation molecular dynamics (SRMD) simulations have been conducted on the cryo-electron microscopy (cryo-EM) structure of nAChR embedded in a dipalmitoylphosphatidylcholine (DPPC) bilayer and water molecules. Water 303-308 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 17600315-8 2007 We then focused on the mechanisms responsible for nicotine-induced fibronectin expression in NSCLC cells and found that nicotine stimulated the surface expression of alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), and that alpha-bungarotoxin, an inhibitor of alpha7 nAChR, abolished the nicotine-induced fibronectin response. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 274-279 17600315-8 2007 We then focused on the mechanisms responsible for nicotine-induced fibronectin expression in NSCLC cells and found that nicotine stimulated the surface expression of alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), and that alpha-bungarotoxin, an inhibitor of alpha7 nAChR, abolished the nicotine-induced fibronectin response. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 17600315-8 2007 We then focused on the mechanisms responsible for nicotine-induced fibronectin expression in NSCLC cells and found that nicotine stimulated the surface expression of alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), and that alpha-bungarotoxin, an inhibitor of alpha7 nAChR, abolished the nicotine-induced fibronectin response. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 274-279 17600315-8 2007 We then focused on the mechanisms responsible for nicotine-induced fibronectin expression in NSCLC cells and found that nicotine stimulated the surface expression of alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), and that alpha-bungarotoxin, an inhibitor of alpha7 nAChR, abolished the nicotine-induced fibronectin response. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 214-219 17600315-8 2007 We then focused on the mechanisms responsible for nicotine-induced fibronectin expression in NSCLC cells and found that nicotine stimulated the surface expression of alpha7 nicotinic acetylcholine receptor (alpha7 nAChR), and that alpha-bungarotoxin, an inhibitor of alpha7 nAChR, abolished the nicotine-induced fibronectin response. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 274-279 17600315-10 2007 These observations suggest that nicotine stimulates NSCLC proliferation through induction of fibronectin, and that these events are mediated through nAChR-mediated signals that include ERK and PI3-K/mTOR pathways. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 18155907-4 2008 The agonist effect of the Cy3-3-acylcholine on nicotinic acetylcholine receptor (nAChR) was confirmed electrophysiologically. Cy3-3-acylcholine 26-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 17662384-8 2008 The nAChR-induced elevation of intracellular calcium ([Ca(2+)](i)) response in undifferentiated cells was due to Ca(2+) influx. Calcium 45-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 17662384-9 2008 In differentiated P19 neurons the nAChR-induced [Ca(2+)](i) response was reduced following pretreatment with ryanodine, while the mAChR-induced response was unaffected indicating the contribution of Ca(2+) release from ryanodine-sensitive stores to nAChR- but not mAChR-mediated Ca(2+) responses. Ryanodine 109-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 17662384-9 2008 In differentiated P19 neurons the nAChR-induced [Ca(2+)](i) response was reduced following pretreatment with ryanodine, while the mAChR-induced response was unaffected indicating the contribution of Ca(2+) release from ryanodine-sensitive stores to nAChR- but not mAChR-mediated Ca(2+) responses. Ryanodine 219-228 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 18183531-3 2008 The examination of selective alpha7 and alpha4beta2 nicotinic acetylcholine receptor (nAChR) agonists suggests that both receptor subtypes mediate improvement in attention, learning and working memory. Acetylcholine 62-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 19079602-4 2008 In the last decade, localization of neuronal nicotinic acetylcholine receptor (nAChR), a specific receptor of nicotine, has been widely detected in non-excitable cells. Nicotine 110-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-77 19079602-4 2008 In the last decade, localization of neuronal nicotinic acetylcholine receptor (nAChR), a specific receptor of nicotine, has been widely detected in non-excitable cells. Nicotine 110-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 19079602-5 2008 Therefore, we hypothesized that nicotine affect growth plate chondrocytes directly and specifically through nAChR to delay skeletal growth. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 19079602-10 2008 Methyllycaconitine (MLA), a specific antagonist of alpha7 nAChR, reversed the inhibition of matrix synthesis and functional calcium signal by nicotine in human growth plate chondrocytes in vitro. methyllycaconitine 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 19079602-10 2008 Methyllycaconitine (MLA), a specific antagonist of alpha7 nAChR, reversed the inhibition of matrix synthesis and functional calcium signal by nicotine in human growth plate chondrocytes in vitro. methyllycaconitine 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 19079602-10 2008 Methyllycaconitine (MLA), a specific antagonist of alpha7 nAChR, reversed the inhibition of matrix synthesis and functional calcium signal by nicotine in human growth plate chondrocytes in vitro. Nicotine 142-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 19079602-12 2008 Maternal nicotine exposure resulted in delayed skeletal growth of alpha7 nAChR +/+ fetuses but not in alpha7 nAChR -/- fetuses, implying that skeletal growth retardation by nicotine is specifically mediated via fetal alpha7 nAChR. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 19079602-12 2008 Maternal nicotine exposure resulted in delayed skeletal growth of alpha7 nAChR +/+ fetuses but not in alpha7 nAChR -/- fetuses, implying that skeletal growth retardation by nicotine is specifically mediated via fetal alpha7 nAChR. Nicotine 173-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 19079602-13 2008 CONCLUSIONS/SIGNIFICANCE: These results suggest that nicotine, from cigarette smoking, acts directly on growth plate chondrocytes to decrease matrix synthesis, suppress hypertrophic differentiation via alpha7 nAChR, leading to delayed skeletal growth. Nicotine 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 18157476-4 2007 In the present study, the nicotinic acetylcholine receptor (nAChR) subtypes and relevant neurotransmitter releases involved in LTP-like response induced by nicotine were investigated by extracellularly recording the PS in the pyramidal cell layer in the hippocampal CA1 region in vitro. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-58 18157476-4 2007 In the present study, the nicotinic acetylcholine receptor (nAChR) subtypes and relevant neurotransmitter releases involved in LTP-like response induced by nicotine were investigated by extracellularly recording the PS in the pyramidal cell layer in the hippocampal CA1 region in vitro. Nicotine 156-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 17942622-7 2007 We also found that a mixture of nAChR subtypes underlies the synaptic modulation in SNc, further distinguishing this nucleus from the VTA, where alpha7 nAChRs enhance glutamate inputs and non-alpha7 receptors enhance GABA inputs. gamma-Aminobutyric Acid 217-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 17942622-9 2007 Thus the observed differences in nicotine-induced DA release from VTA and SNc are likely due to differences in nAChR expression on the afferent inputs as well as on the DA neurons themselves. Nicotine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 17936462-5 2007 Exposure to nicotine upregulates nAChRs and nAChR currents and produces LTP of excitatory inputs to midbrain DA neurons. Nicotine 12-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 17973360-2 2007 Docking simulations indicated that ligand-nAChR complexes were formed by hydrophobic interactions with the cleft and hydrogen bond interactions. Hydrogen 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 17936462-9 2007 A model is proposed in which nicotine exposure regimens that produce transient nAChR upregulation and LTP consequently produce long-lasting sensitization of midbrain DA neuron reactivity and nicotine-induced behaviors. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 17936462-9 2007 A model is proposed in which nicotine exposure regimens that produce transient nAChR upregulation and LTP consequently produce long-lasting sensitization of midbrain DA neuron reactivity and nicotine-induced behaviors. Nicotine 191-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 17878927-6 2007 Placenta cells express the alpha7 nicotinic acetylcholine receptor (alpha7nAChR), and using cholinergic antagonists, we demonstrated that the antiinflammatory effect of nicotine and other cholinergic agonists is, in part, mediated through the nAChR pathway. Nicotine 169-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 17929796-0 2007 Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists. 3,6-diazabicyclo[3.2.0]heptanes 57-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-142 17929796-1 2007 A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the alpha4beta2 nAChR subtype. 3,6-Diazabicyclo[3.2.0]heptane 97-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 17929796-1 2007 A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and evaluated for binding affinity and agonist activity at the alpha4beta2 nAChR subtype. 3,6-Diazabicyclo[3.2.0]heptane 97-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 17929796-2 2007 Structure-activity relationship studies of these novel nAChR ligands focused on substitution effects on the pyridine ring, as well as stereo- and regiochemical influences of the 3,6-diazabicyclo[3.2.0]heptane core. pyridine 108-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 17929796-2 2007 Structure-activity relationship studies of these novel nAChR ligands focused on substitution effects on the pyridine ring, as well as stereo- and regiochemical influences of the 3,6-diazabicyclo[3.2.0]heptane core. 3,6-Diazabicyclo[3.2.0]heptane 178-208 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 17929796-5 2007 Most of the 6-N-pyridinyl-substituted 3,6-diazabicyclo[3.2.0]heptanes are selective for the alpha4beta2 nAChR subtype. 6-n-pyridinyl-substituted 3,6-diazabicyclo[3.2.0]heptanes 12-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r 12-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r) 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r) 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r 12-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17929796-8 2007 (1R,5R)-39, (1R,5R)-41, and (1R,5R)-42 were found to be much more potent at the halpha3beta4 nAChR subtype, whereas (1R,5R)-38 and (1R,5R)-40 were very selective at the halpha4beta2 nAChR subtype. (1r,5r 12-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17662959-4 2007 Key events in the evolution of the nAChR field were the development of high throughput electrophysiological screening tools that provided the means to enable lead optimization efforts in medicinal chemistry and the discovery by John Daly at the NIH of the frog alkaloid, epibatidine, that provided the framework for the discovery of ABT-594, an alpha4beta2 agonist that is 200 times more potent than morphine as an analgesic. epibatidine 271-282 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17543588-4 2007 These effects were blocked by specific antagonists of nAChR (mecamylamine), 5-HT(3) (Y-25130), and TRPV1 (capsazepine). Mecamylamine 61-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 17689497-5 2007 When expressed on postsynaptic membranes, nAChR-initiated calcium signals and depolarization activate intracellular signaling mechanisms and gene transcription. Calcium 58-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 17728248-3 2007 Interactions between nAChR subunits and ERp57 occur via transient intermolecular disulfide bonds and do not require subunit N-linked glycosylation. Disulfides 81-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 17707779-2 2007 In the context of ligand gated ion channels such as nicotinic acetylcholine receptors (nAChRs), it implies that endogenous ligand acetylcholine binds at the orthosteric site, and that molecules that bind elsewhere on the nAChR subunit(s) acts via allosteric interactions. Acetylcholine 62-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 17662959-4 2007 Key events in the evolution of the nAChR field were the development of high throughput electrophysiological screening tools that provided the means to enable lead optimization efforts in medicinal chemistry and the discovery by John Daly at the NIH of the frog alkaloid, epibatidine, that provided the framework for the discovery of ABT-594, an alpha4beta2 agonist that is 200 times more potent than morphine as an analgesic. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 333-336 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17662959-4 2007 Key events in the evolution of the nAChR field were the development of high throughput electrophysiological screening tools that provided the means to enable lead optimization efforts in medicinal chemistry and the discovery by John Daly at the NIH of the frog alkaloid, epibatidine, that provided the framework for the discovery of ABT-594, an alpha4beta2 agonist that is 200 times more potent than morphine as an analgesic. Morphine 400-408 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17869436-0 2007 Potentiation of the nicotinic acetylcholine receptor by aluminum in mammalian neurons. Aluminum 56-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-52 17869436-6 2007 Al(3+) appeared to increase the affinity of nicotine to nAChR but not the efficacy. ALUMINUM ION 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 17869436-9 2007 The present results indicated that Al(3+) enhanced the function of nAChR and this potentiation might underlie the neurological alteration induced by Al(3+). ALUMINUM ION 35-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 17869436-9 2007 The present results indicated that Al(3+) enhanced the function of nAChR and this potentiation might underlie the neurological alteration induced by Al(3+). ALUMINUM ION 149-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 17869436-6 2007 Al(3+) appeared to increase the affinity of nicotine to nAChR but not the efficacy. Nicotine 44-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 17913920-0 2007 Hippocampal alpha4beta2 nicotinic acetylcholine receptor involvement in the enhancing effect of acute nicotine on contextual fear conditioning. Nicotine 102-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-56 17628012-0 2007 The endocannabinoid anandamide inhibits the function of alpha4beta2 nicotinic acetylcholine receptors. Endocannabinoids 4-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-101 17628012-0 2007 The endocannabinoid anandamide inhibits the function of alpha4beta2 nicotinic acetylcholine receptors. anandamide 20-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-101 17628012-1 2007 The effects of the endocannabinoid anandamide (arachidonylethanolamide, AEA) on the function of alpha4beta2 nicotinic acetylcholine receptors (nAChR) stably expressed in SH-EP1 cells were investigated using the whole-cell patch-clamp technique. anandamide 35-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 17628012-1 2007 The effects of the endocannabinoid anandamide (arachidonylethanolamide, AEA) on the function of alpha4beta2 nicotinic acetylcholine receptors (nAChR) stably expressed in SH-EP1 cells were investigated using the whole-cell patch-clamp technique. anandamide 47-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-141 17628012-1 2007 The effects of the endocannabinoid anandamide (arachidonylethanolamide, AEA) on the function of alpha4beta2 nicotinic acetylcholine receptors (nAChR) stably expressed in SH-EP1 cells were investigated using the whole-cell patch-clamp technique. anandamide 47-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 17628012-1 2007 The effects of the endocannabinoid anandamide (arachidonylethanolamide, AEA) on the function of alpha4beta2 nicotinic acetylcholine receptors (nAChR) stably expressed in SH-EP1 cells were investigated using the whole-cell patch-clamp technique. anandamide 72-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-141 17628012-1 2007 The effects of the endocannabinoid anandamide (arachidonylethanolamide, AEA) on the function of alpha4beta2 nicotinic acetylcholine receptors (nAChR) stably expressed in SH-EP1 cells were investigated using the whole-cell patch-clamp technique. anandamide 72-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 17628012-7 2007 Moreover, BSA alone increased peak ACh current amplitudes and diminished desensitization rates in naive cells, suggesting a tonic modulation of alpha4beta2 nAChR function by an endogenous AEA-like lipid. anandamide 188-191 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 17628012-8 2007 Further analysis of AEA effects on alpha4beta2 nAChR-mediated currents, using a two-stage desensitization model, indicated that the first forward rate constant leading to desensitization, k(1), increased nearly 30-fold as a linear function of the AEA concentration. anandamide 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 17628012-8 2007 Further analysis of AEA effects on alpha4beta2 nAChR-mediated currents, using a two-stage desensitization model, indicated that the first forward rate constant leading to desensitization, k(1), increased nearly 30-fold as a linear function of the AEA concentration. anandamide 247-250 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 17898222-5 2007 In particular, a 24 h exposure to nicotine decreased proteasome-dependent degradation of the alpha7 nicotinic acetylcholine receptor (nAChR) subunit, as indicated by the accumulation of ubiquitinated alpha7. Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 17898222-8 2007 The nAChR antagonist mecamylamine was only partially able to block the effects of nicotine on the UPS, indicating that nAChR activation does not completely explain nicotine-induced inhibition of proteasomal catalytic activity. Mecamylamine 21-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 17722904-2 2007 Several of the analogues are potent antagonists of the homomeric alpha7 nicotinic acetylcholine receptor (nAChR), displaying nanomolar binding affinities and inhibiting acetylcholine-evoked signaling through the receptor in a competitive manner. Acetylcholine 82-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 17632185-10 2007 The study indicates that galantamine and risperidone may have synergistic effect on the cognitive impairments in schizophrenia patients by synergistically promoting the nAChR activation-dependent increase of dopamine D1 receptor-mediated neurotransmission. Galantamine 25-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 17768273-9 2007 CONCLUSIONS: Results of analyses ranging from basic biological approaches to clinical outcome data provide consistent evidence that 2 single-nucleotide polymorphisms in CHRNA4 are functional at a biological level and are associated with nicotine dependence phenotypes. Nicotine 237-245 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-175 17632185-10 2007 The study indicates that galantamine and risperidone may have synergistic effect on the cognitive impairments in schizophrenia patients by synergistically promoting the nAChR activation-dependent increase of dopamine D1 receptor-mediated neurotransmission. Risperidone 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 17616467-4 2007 These results suggest that while nAChR expression is similarly decreased in the striatum of motor-asymptomatic and motor-symptomatic MPTP-treated monkeys, there are differences in beta2* and beta4* nAChR expression in cortical regions in these two conditions. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 133-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-147 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Cocaine 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-147 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Cocaine 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Cocaine 169-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-147 17530475-2 2007 Nicotine and cocaine are commonly coabused drugs in humans and recent work in animals suggests that activation of nicotinic acetylcholine receptors (nAChR) can increase cocaine self-administration. Cocaine 169-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 17784838-6 2007 Furthermore, the antiapoptotic effect of nicotine was blocked completely by nicotinic acetylcholine receptor (nAChR) antagonist hexamethonium. Nicotine 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-108 17699659-6 2007 We found a positive correlation between the response to novelty and nAChR function in each assay conducted, including nAChR modulation of glutamatergic and GABAergic synaptic inputs to VTA dopamine neurons, as well as somatic nAChR responses of VTA neurons. Dopamine 189-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 17699659-6 2007 We found a positive correlation between the response to novelty and nAChR function in each assay conducted, including nAChR modulation of glutamatergic and GABAergic synaptic inputs to VTA dopamine neurons, as well as somatic nAChR responses of VTA neurons. Dopamine 189-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 17699659-6 2007 We found a positive correlation between the response to novelty and nAChR function in each assay conducted, including nAChR modulation of glutamatergic and GABAergic synaptic inputs to VTA dopamine neurons, as well as somatic nAChR responses of VTA neurons. Dopamine 189-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 118-123 17699659-8 2007 Consistent with this observation, we found enhanced nAChR responses in vitro after a 48 h corticosterone treatment and in vivo after 48 h of repeated stress. Corticosterone 90-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 17699659-10 2007 These findings suggest that differences in nAChR function within the mesoaccumbens dopamine system may contribute to individual differences in drug abuse vulnerability and that these are likely attributable to differences in stress hormone levels. Dopamine 83-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 17383007-3 2007 Chronic nicotine exposure differentially affects the number, subunit composition, stoichiometry and functional state of some nAChR subtypes, leaving others substantially unaffected. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 17383007-4 2007 In this review, we will summarise recent data concerning the nAChR subtypes expressed in the CNS, and how they are regulated by means of chronic nicotine and/or nicotinic drugs. Nicotine 145-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 17654292-7 2007 Short-term and prolonged 3-day exposures of SH-SY5Y cells to either TPM or nicotine at nicotine concentrations ranging from 0.2 microM to 20 microM increased specific binding, suggesting upregulation of nAChR expression. Topiramate 68-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 17654292-7 2007 Short-term and prolonged 3-day exposures of SH-SY5Y cells to either TPM or nicotine at nicotine concentrations ranging from 0.2 microM to 20 microM increased specific binding, suggesting upregulation of nAChR expression. Nicotine 75-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 17854561-1 2007 OBJECTIVE: To investigate the inhibition effects of Tianshen Yizhi Recipe (TSYZR), a compound traditional Chinese herbal medicine, on decreased expression of nicotinic acetylcholine receptor (nAChR) and the neurotoxicity as well as lipid peroxidation induced by beta-amyloid peptide (Abeta) in human SH-SY5Y neuroblastoma cells. Acetylcholine 168-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 17554626-5 2007 The target for nicotine is the neuronal nicotinic acetylcholine receptor (nAChR). Nicotine 15-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-72 17554626-5 2007 The target for nicotine is the neuronal nicotinic acetylcholine receptor (nAChR). Nicotine 15-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 17784838-6 2007 Furthermore, the antiapoptotic effect of nicotine was blocked completely by nicotinic acetylcholine receptor (nAChR) antagonist hexamethonium. Nicotine 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 17784838-6 2007 Furthermore, the antiapoptotic effect of nicotine was blocked completely by nicotinic acetylcholine receptor (nAChR) antagonist hexamethonium. Hexamethonium 128-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-108 17784838-6 2007 Furthermore, the antiapoptotic effect of nicotine was blocked completely by nicotinic acetylcholine receptor (nAChR) antagonist hexamethonium. Hexamethonium 128-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 17585748-2 2007 Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the alpha 4 beta 2 subtype, placing them with epibatidine among the most potent nAChR ligands described to date. n-(3-pyridinyl) 8-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 17614369-2 2007 In the present study, the homopentameric mollusk ACh binding protein (AChBP), used as a surrogate for the extracellular ligand-binding domain of the nAChR, was specifically derivatized by the highly potent agonist azidoepibatidine (AzEPI) prepared as a photoaffinity probe and radioligand. azidoepibatidine 214-230 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 17614369-2 2007 In the present study, the homopentameric mollusk ACh binding protein (AChBP), used as a surrogate for the extracellular ligand-binding domain of the nAChR, was specifically derivatized by the highly potent agonist azidoepibatidine (AzEPI) prepared as a photoaffinity probe and radioligand. azepi 232-237 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 17614369-7 2007 [3H]AzEPI binds to the alpha4beta2 nAChR at a single high-affinity site and photoaffinity-labels only the alpha4 subunit, presumably modifying Tyr225 spatially corresponding to Tyr195 of AChBP. Tritium 1-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17614369-7 2007 [3H]AzEPI binds to the alpha4beta2 nAChR at a single high-affinity site and photoaffinity-labels only the alpha4 subunit, presumably modifying Tyr225 spatially corresponding to Tyr195 of AChBP. azepi 4-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17614369-8 2007 Phe137 of the beta2 nAChR subunit, equivalent to Met116 of AChBP, conceivably lacks sufficient reactivity with the nitrene generated from the probe. achbp 59-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 17614369-9 2007 The present photoaffinity labeling in a physiologically relevant condition combined with the crystal structure of AChBP allows development of precise structural models for the AzEPI interactions with AChBP and alpha4beta2 nAChR. achbp 114-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 222-227 17614369-9 2007 The present photoaffinity labeling in a physiologically relevant condition combined with the crystal structure of AChBP allows development of precise structural models for the AzEPI interactions with AChBP and alpha4beta2 nAChR. azepi 176-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 222-227 17614369-10 2007 These findings enabled us to use AChBP as a structural surrogate to define the nAChR agonist site. achbp 33-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 17585748-2 2007 Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the alpha 4 beta 2 subtype, placing them with epibatidine among the most potent nAChR ligands described to date. bicyclic diamines 47-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 17585748-2 2007 Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the alpha 4 beta 2 subtype, placing them with epibatidine among the most potent nAChR ligands described to date. epibatidine 165-176 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 17585748-3 2007 Structure-activity studies have revealed that substitutions, particularly hydrophilic groups in the pyridine 5-position, differentially modulate the agonist activity at ganglionic vs central nAChR subtypes, so that improved subtype selectivity can be demonstrated in vitro. pyridine 100-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 17552523-5 2007 The very low water density in the middle of the nAChR pore indicated the existence of a hydrophobic constriction. Water 13-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 17656829-6 2007 The use of nAChR agonists and antagonists in some of these studies lends support to the proposed allosteric potentiating ligand activity of galantamine at nAChRs. Galantamine 140-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 18221220-7 2007 Initially identified nAChR allosteric modulators, including 5-hydroxyindole (5-HI), galantamine, bovine serum albumin, and SLURP-1, are weak and nonselective. 5-hydroxyindole 77-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 17595341-1 2007 The acetylcholine-binding protein (AChBP) is homologous to the ligand-binding domain of the nicotinic acetylcholine receptor (nAChR) and other members of the Cys-loop family of neurotransmitter receptors. Cysteine 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-124 17595341-1 2007 The acetylcholine-binding protein (AChBP) is homologous to the ligand-binding domain of the nicotinic acetylcholine receptor (nAChR) and other members of the Cys-loop family of neurotransmitter receptors. Cysteine 158-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 17481657-1 2007 Rapid neurotransmission is mediated through a superfamily of Cys-loop receptors that includes the nicotinic acetylcholine (nAChR), gamma-aminobutyric acid (GABA(A)), serotonin (5-HT(3)) and glycine receptors. nicotinic acetylcholine 98-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 17481657-10 2007 X-ray structures of cocaine and galanthamine bound to AChBP (1.8 A and 2.9 A resolution, respectively) reveal interactions deep within the subunit interface and the absence of a contact surface with the tip of loop C. Hence, in addition to channel blocking, non-competitive interactions with heteromeric neuronal nAChR appear to occur at the non-alpha subunit interface, a site presumed to be similar to that of modulating benzodiazepines on GABA(A) receptors. Cocaine 20-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 313-318 17481657-10 2007 X-ray structures of cocaine and galanthamine bound to AChBP (1.8 A and 2.9 A resolution, respectively) reveal interactions deep within the subunit interface and the absence of a contact surface with the tip of loop C. Hence, in addition to channel blocking, non-competitive interactions with heteromeric neuronal nAChR appear to occur at the non-alpha subunit interface, a site presumed to be similar to that of modulating benzodiazepines on GABA(A) receptors. Galantamine 32-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 313-318 18221220-4 2007 An attractive alternative approach to modulating alpha7 nAChR function is to enhance the effects of the endogenous neurotransmitter acetylcholine (ACh) through positive allosteric modulation (PAM). Acetylcholine 132-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18221220-7 2007 Initially identified nAChR allosteric modulators, including 5-hydroxyindole (5-HI), galantamine, bovine serum albumin, and SLURP-1, are weak and nonselective. 5-hydroxyindole 60-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 17686198-4 2007 Using choline as a nAChR partially subtype-specific agonist, we found that the majority of DS GCs demonstrated responses to choline while under synaptic blockade. Choline 6-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 17686198-4 2007 Using choline as a nAChR partially subtype-specific agonist, we found that the majority of DS GCs demonstrated responses to choline while under synaptic blockade. Choline 124-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 17434679-1 2007 Nicotine, the major psychoactive ingredient in tobacco interacting with nicotinic acetylcholine receptors (nAChR), is believed to have neuroprotective and neurotoxic effects on the developing brain. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 17434679-3 2007 Thus, developmental nicotine could have opposite effects in different brain regions, depending on nAChR subtype expression. Nicotine 20-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 17434679-4 2007 Here, we determined if chronic neonatal nicotine exposure (CNN), during a period of brain growth corresponding to the third human trimester, differentially regulates nAChR expression, cell death, and morphological properties in hippocampus and cerebellum, two structures maturing postnatally. Nicotine 40-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 17434679-11 2007 Thus, the hippocampus seems to be more sensitive than the cerebellum to CNN which could result from different nAChR subtype expression and might explain long-lasting altered cognitive functions correlated with gestational nicotine exposure due to changes in hippocampal cell morphology. Nicotine 222-230 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 18221220-7 2007 Initially identified nAChR allosteric modulators, including 5-hydroxyindole (5-HI), galantamine, bovine serum albumin, and SLURP-1, are weak and nonselective. Galantamine 84-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 17286989-8 2007 These results suggest that both SLURP-1 and SLURP-2 are expressed in various immune cells and organs, and that not only ACh but also SLURPs may be involved in regulating lymphocyte function via nAChR-mediated pathways. Acetylcholine 120-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 17314009-0 2007 JN403, in vitro characterization of a novel nicotinic acetylcholine receptor alpha7 selective agonist. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-76 17510389-1 2007 Nicotine and its derivatives, by binding to nicotinic acetylcholine receptors (nAChR) on bronchial epithelial cells, can regulate cellular proliferation and apoptosis via activating the Akt pathway. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 17510389-4 2007 Five nonmalignant HBECs were exposed to nicotine in vitro to study the variation of nAChR subunit gene expression with nicotine exposure and removal. Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 17510389-8 2007 nAChR alpha1, alpha5, and alpha7 showed significant reversible changes in expression levels in HBECs upon nicotine exposure. Nicotine 106-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 17510389-10 2007 Finally, nicotine exposure in HBECs resulted in reversible differences in nAChR subunit gene expression. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 17289799-9 2007 This effect was reversed by the nAChR antagonist mecamylamine. Mecamylamine 49-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (s)-(1-aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid 129-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-97 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (s)-(1-aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid 129-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 17391965-1 2007 (S)-Aporphine metho salts with the 1,2,9,10 oxygenation pattern displaced radioligands from recombinant human alpha7 and alpha4beta2 neuronal nicotinic acetylcholine receptors (nAChR) at low micromolar concentrations. (s)-aporphine metho salts 0-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-175 17391965-1 2007 (S)-Aporphine metho salts with the 1,2,9,10 oxygenation pattern displaced radioligands from recombinant human alpha7 and alpha4beta2 neuronal nicotinic acetylcholine receptors (nAChR) at low micromolar concentrations. (s)-aporphine metho salts 0-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 17391965-3 2007 At homomeric alpha7 nAChR, xanthoplanine had the highest affinity (K(i)=10 microM) vs [(125)I]alpha-bungarotoxin while the other three compounds displaced the radioligand with K(i) values between 15 and 21 microM. Xanthoplanine 27-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 17510389-1 2007 Nicotine and its derivatives, by binding to nicotinic acetylcholine receptors (nAChR) on bronchial epithelial cells, can regulate cellular proliferation and apoptosis via activating the Akt pathway. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-77 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (s)-1-(2-fluoro-phenyl)-ethyl ester 178-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-97 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (s)-1-(2-fluoro-phenyl)-ethyl ester 178-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 17314009-4 2007 Functionally, JN403 is a partial and potent agonist at human nAChR alpha7. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 14-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 17314009-5 2007 The compound stimulates calcium influx in GH3 cells recombinantly expressing the human nAChR with an pEC(50) of 7.0 and an E(max) of 85% (compared to the full agonist epibatidine). Calcium 24-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 122-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-97 17314009-5 2007 The compound stimulates calcium influx in GH3 cells recombinantly expressing the human nAChR with an pEC(50) of 7.0 and an E(max) of 85% (compared to the full agonist epibatidine). epibatidine 167-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 17314009-7 2007 In both recombinant systems JN403 is a partial agonist and the agonistic effects are blocked after pre-administration of methyllycaconitine (MLA, 100nM), a nAChR alpha7 antagonist. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 28-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 17314009-1 2007 This report describes the in vitro features of a novel selective nicotinic acetylcholine receptor (nAChR) alpha7 agonist, JN403, (S)-(1-Aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid (S)-1-(2-fluoro-phenyl)-ethyl ester. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 122-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 17314009-7 2007 In both recombinant systems JN403 is a partial agonist and the agonistic effects are blocked after pre-administration of methyllycaconitine (MLA, 100nM), a nAChR alpha7 antagonist. methyllycaconitine 121-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 17314009-7 2007 In both recombinant systems JN403 is a partial agonist and the agonistic effects are blocked after pre-administration of methyllycaconitine (MLA, 100nM), a nAChR alpha7 antagonist. methyllycaconitine 141-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 17300943-0 2007 Actions between neonicotinoids and key residues of insect nAChR based on an ab initio quantum chemistry study: hydrogen bonding and cooperative pi-pi interaction. Neonicotinoids 16-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 17314009-10 2007 Thus, JN403 is a potent and selective nAChR alpha7 agonist and will be a useful tool for the characterization of nAChR alpha7 mediated effects both in vitro and in vivo. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 6-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 17314009-10 2007 Thus, JN403 is a potent and selective nAChR alpha7 agonist and will be a useful tool for the characterization of nAChR alpha7 mediated effects both in vitro and in vivo. (S)-(1-azabicyclo(2.2.2)oct-3-yl)carbamic acid (S)-1-(2-fluorophenyl) ethyl ester 6-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 17300943-0 2007 Actions between neonicotinoids and key residues of insect nAChR based on an ab initio quantum chemistry study: hydrogen bonding and cooperative pi-pi interaction. Hydrogen 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 17300943-1 2007 Neonicotinoid insecticides show selective actions on insect nicotinic acetylcholine receptor (nAChR). Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 17300943-1 2007 Neonicotinoid insecticides show selective actions on insect nicotinic acetylcholine receptor (nAChR). Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 17300943-3 2007 To investigate the selective mechanism, a computational model was set up to simulate the interaction between residues (Trp and Arg) of insect nAChR and neonicotinoids by quantum chemistry method. Tryptophan 119-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 17300943-3 2007 To investigate the selective mechanism, a computational model was set up to simulate the interaction between residues (Trp and Arg) of insect nAChR and neonicotinoids by quantum chemistry method. Arginine 127-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 17465209-1 2007 BACKGROUND: Molecular events following nicotinic acetylcholine receptor (nAChR) activation by nicotine are poorly understood. Nicotine 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-71 17392029-10 2007 In summary, computer modeling visualized possible modes of binding for those weak toxins which interact with the nAChR, provided no solutions for those weak toxins whose targets are not the nAChRs, and demonstrated that the additional disulfide in loop I cannot be a sound criteria for joining all weak toxins into one group; the conclusion about the diversity of weak toxins made from computer modeling is in accord with the earlier phylogenetic analysis. Disulfides 235-244 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 17465209-1 2007 BACKGROUND: Molecular events following nicotinic acetylcholine receptor (nAChR) activation by nicotine are poorly understood. Nicotine 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 17142275-3 2007 In this study, we determined the structure and backbone dynamics of an extended segment encompassing the first TM domain (TM1e) of nAChR beta(2) subunit in dodecylphosphocholine micelles, using solution-state NMR and circular dichroism (CD) spectroscopy. dodecylphosphocholine 156-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 17065235-1 2007 5-(Trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1H-quinolin-2-one (TMAQ) is a novel nicotinic acetylcholine receptor (nAChR) agonist with strong selectivity for beta4-containing receptors. 5-(trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1h-quinolin-2-one 0-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 17329297-3 2007 The present study assessed the safety, tolerability and effect on cognition of ispronicline, a highly selective partial agonist at the 4beta2 nAChR, in elderly subjects (n =76) with age associated memory impairment (AAMI). ispronicline 79-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 332-337 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Nicotine 292-300 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Nicotine 292-300 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 17065235-1 2007 5-(Trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1H-quinolin-2-one (TMAQ) is a novel nicotinic acetylcholine receptor (nAChR) agonist with strong selectivity for beta4-containing receptors. 5-(trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1h-quinolin-2-one 0-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 17065235-1 2007 5-(Trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1H-quinolin-2-one (TMAQ) is a novel nicotinic acetylcholine receptor (nAChR) agonist with strong selectivity for beta4-containing receptors. tmaq 70-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-119 17065235-1 2007 5-(Trifluoromethyl)-6-(1-methyl-azepan-4-yl)methyl-1H-quinolin-2-one (TMAQ) is a novel nicotinic acetylcholine receptor (nAChR) agonist with strong selectivity for beta4-containing receptors. tmaq 70-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 17082486-4 2007 Unexpectedly, nAChR antagonism not only abolished nicotine-induced HMVEC migration but also abolished migration induced by bFGF and attenuated migration induced by VEGF. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-19 17082486-9 2007 CONCLUSIONS: Nicotine promotes angiogenesis via stimulation of nAChR-dependent endothelial cell migration. Nicotine 13-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 17103466-6 2007 This analysis revealed the peculiar behaviour of the ammonium moiety of nicotinic acetylcholine receptor (nAChR) ligands towards the picrate anion. Ammonium Compounds 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-104 17103466-6 2007 This analysis revealed the peculiar behaviour of the ammonium moiety of nicotinic acetylcholine receptor (nAChR) ligands towards the picrate anion. Ammonium Compounds 53-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 17103466-9 2007 The experimental and theoretical studies performed on the nicotine and ACh cations consistently show the significant HB ability of the acceptor site of nAChR agonists in their charged form. Nicotine 58-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 17103466-9 2007 The experimental and theoretical studies performed on the nicotine and ACh cations consistently show the significant HB ability of the acceptor site of nAChR agonists in their charged form. Acetylcholine 71-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 16906354-2 2007 In the present work we reviewed recent advances concerning neuroprotective/neurotrophic effects of acute or chronic nicotine exposure, and the signalling pathways mediating these effects, including mechanisms implicated in nicotine addiction and nAChR desensitization. Nicotine 116-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 246-251 16906354-3 2007 Experimental and clinical data largely indicate long-lasting effects of nicotine and nicotinic agonists that imply a neuroprotective/neurotrophic role of nAChR activation, involving mainly alpha7 and alpha4beta2 nAChR subtypes, as evidenced using selective nAChR agonists. Nicotine 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Nicotine 14-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. epibatidine 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. epibatidine 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. epibatidine 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Dopamine 177-185 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Dopamine 177-185 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17141870-5 2007 Comparison of nicotine and epibatidine, two nAChR agonists whose relative affinities for various nAChR subtypes differ, revealed differences in the nAChR-mediated regulation of dopaminergic activation between these dopamine systems. Dopamine 177-185 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 17105227-3 2006 To facilitate the purification of the nAChR labeled subunits, we tagged the ligand with a desthiobiotin moiety. desthiobiotin 90-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 20641870-8 2004 2-(+/-)-2-exo-(2"-Fluoro-3"-phenyl-pyridin-5"-yl)-7-azabicyclo[2.2.1]heptane (FPhEP) is a highly potent and selective alpha4beta2 nAChR antagonist with subnanomolar affinity (6, 7). 2-(+/-)-2-exo-(2"-fluoro-3"-phenyl-pyridin-5"-yl)-7-azabicyclo[2.2.1]heptane 0-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 16934977-1 2006 Binding affinities for a range of epibatidine isomers and analogues at the alpha4beta2 and alpha3beta4 nAChR subtypes are reported; compounds having similar N-N distances to epibatidine show similar, high potencies. epibatidine 34-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 17015027-0 2007 Nicotine activates cell-signaling pathways through muscle-type and neuronal nicotinic acetylcholine receptors in non-small cell lung cancer cells. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-109 17015027-1 2007 Nicotinic acetylcholine receptors (nAChR) are expressed on non-neuronal cell types, including normal bronchial epithelial cells, and nicotine has been reported to cause Akt activation in cultured normal airway cells. Nicotine 133-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 17015027-9 2007 Nicotine at a concentration of 10 microM caused phosphorylation of mitogen-activated protein kinase (MAPK) (p44/42) that could be inhibited using nAChR antagonists. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 17015027-11 2007 Akt was also phosphorylated in NSCLC cells after exposure to nicotine; this effect was inhibited by the PI3K inhibitor LY294002 and antagonists to the neuronal-type nAChR, but not to the muscle-type receptor. Nicotine 61-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 17015027-11 2007 Akt was also phosphorylated in NSCLC cells after exposure to nicotine; this effect was inhibited by the PI3K inhibitor LY294002 and antagonists to the neuronal-type nAChR, but not to the muscle-type receptor. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 17181167-1 2006 A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). 3,8-DIAZABICYCLO[4.2.0]OCTANE 88-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-60 17181167-1 2006 A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). 3,8-DIAZABICYCLO[4.2.0]OCTANE 88-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 17181167-1 2006 A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). Nicotine 220-228 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 17181167-1 2006 A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). halpha4beta2 247-259 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 17181167-1 2006 A series of potent neuronal nicotinic acetylcholine receptor (nAChR) ligands based on a 3,8-diazabicyclo[4.2.0]octane core have been synthesized and evaluated for affinity and agonist efficacy at the human high affinity nicotine recognition site (halpha4beta2) and in a rat model of persistent nociceptive pain (formalin model). Formaldehyde 312-320 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 21783722-4 2006 MEK1/2 specific inhibitor UO126 completely blocked NNK-induced ERK1/2 activation and cell proliferation, whereas nicotinic receptor nAchR antagonist mecamylamine partially and the selective alpha(7)-nAchR antagonist alpha-bungarotoxin essentially inhibited the NNK-induced ERK1/2 activation and cell proliferation. Mecamylamine 149-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 17034254-0 2006 Blocking of the nicotinic acetylcholine receptor ion channel by chlorpromazine, a noncompetitive inhibitor: A molecular dynamics simulation study. Chlorpromazine 64-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-48 16949557-2 2006 On a time course longer than that needed to activate nicotinic acetylcholine receptor (nAChR) function, nicotine exposure induces functional inactivation of nAChR, upregulation of nAChR radioligand binding sites, and other alterations of cellular functions. Nicotine 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-85 16949557-2 2006 On a time course longer than that needed to activate nicotinic acetylcholine receptor (nAChR) function, nicotine exposure induces functional inactivation of nAChR, upregulation of nAChR radioligand binding sites, and other alterations of cellular functions. Nicotine 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 16949557-2 2006 On a time course longer than that needed to activate nicotinic acetylcholine receptor (nAChR) function, nicotine exposure induces functional inactivation of nAChR, upregulation of nAChR radioligand binding sites, and other alterations of cellular functions. Nicotine 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 16949557-2 2006 On a time course longer than that needed to activate nicotinic acetylcholine receptor (nAChR) function, nicotine exposure induces functional inactivation of nAChR, upregulation of nAChR radioligand binding sites, and other alterations of cellular functions. Nicotine 104-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 16949557-3 2006 To identify possible mechanisms underlying nicotine-induced changes in nAChR numbers and function, we defined changes in gene expression in neuron-like, SH-SY5Y human neuroblastoma cells following 24 h of continuous exposure to 1 mM nicotine. Nicotine 43-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 16949557-7 2006 Inhibition or reversal of these effects by the general nAChR antagonist, d-tubocurarine, indicated that gene expression changes are dependent on nAChR activation. Tubocurarine 73-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 16949557-7 2006 Inhibition or reversal of these effects by the general nAChR antagonist, d-tubocurarine, indicated that gene expression changes are dependent on nAChR activation. Tubocurarine 73-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 16949557-9 2006 These results suggest that longer-term physiological and psychological effects of nicotine exposure and changes in nAChR expression may be due in part to effects on gene expression initiated by interactions with nAChR. Nicotine 82-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 212-217 17034254-1 2006 A large series of pharmacological agents, distinct from the typical competitive antagonists, block in a noncompetitive manner the permeability response of the nicotinic acetylcholine receptor (nAChR) to the neurotransmitter acetylcholine. Acetylcholine 169-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 17034254-2 2006 Taking the neuroleptic chlorpromazine (CPZ) as an example of such agents, the blocking mechanism of noncompetitive inhibitors to the ion channel pore of the nAChR has been explored at the atomic level using both conventional and steered molecular dynamics (MD) simulations. Chlorpromazine 23-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 17034254-2 2006 Taking the neuroleptic chlorpromazine (CPZ) as an example of such agents, the blocking mechanism of noncompetitive inhibitors to the ion channel pore of the nAChR has been explored at the atomic level using both conventional and steered molecular dynamics (MD) simulations. Chlorpromazine 39-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 17034254-6 2006 The cationic ammonium head of CPZ forms strong hydrogen bonds with Glu262 (alpha), Asp268 (beta), Glu272 (beta), Ser276 (beta), Glu280 (delta), Gln271 (gamma), Glu275 (gamma), and Asn279 (gamma) nAChR residues. Chlorpromazine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 16935422-1 2006 Nicotinic acetylcholine receptors (nAChR) are widely expressed throughout the nervous system, are involved in some fast excitatory neurotransmission, and play an important role in modulating the release of several neurotransmitters, including the major excitatory and inhibitory neurotransmitters, glutamate and GABA. Glutamic Acid 298-307 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 16935422-1 2006 Nicotinic acetylcholine receptors (nAChR) are widely expressed throughout the nervous system, are involved in some fast excitatory neurotransmission, and play an important role in modulating the release of several neurotransmitters, including the major excitatory and inhibitory neurotransmitters, glutamate and GABA. Glutamic Acid 298-307 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 16935422-1 2006 Nicotinic acetylcholine receptors (nAChR) are widely expressed throughout the nervous system, are involved in some fast excitatory neurotransmission, and play an important role in modulating the release of several neurotransmitters, including the major excitatory and inhibitory neurotransmitters, glutamate and GABA. gamma-Aminobutyric Acid 312-316 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-33 16935422-1 2006 Nicotinic acetylcholine receptors (nAChR) are widely expressed throughout the nervous system, are involved in some fast excitatory neurotransmission, and play an important role in modulating the release of several neurotransmitters, including the major excitatory and inhibitory neurotransmitters, glutamate and GABA. gamma-Aminobutyric Acid 312-316 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 16935422-2 2006 We used a recently characterised alpha4beta2 nAChR subunit selective partial agonist, TC-2559, to study the effect of alpha4beta2 nAChR activation on synaptic plasticity in the medio-dorsal perforant pathway input to the dentate gyrus, in the intact nervous system in vivo. TC 2559 86-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 16935422-3 2006 We show for the first time, that the selective activation of alpha4beta2 containing nAChR can reduce the level of long-term potentiation (LTP) induced by high frequency stimulation, an effect that was reversed by the selective antagonist, dihydro-beta-erythroidine (DbetaHE). Dihydro-beta-Erythroidine 239-264 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 16935422-3 2006 We show for the first time, that the selective activation of alpha4beta2 containing nAChR can reduce the level of long-term potentiation (LTP) induced by high frequency stimulation, an effect that was reversed by the selective antagonist, dihydro-beta-erythroidine (DbetaHE). Dihydro-beta-Erythroidine 266-273 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 20641387-8 2004 2-Fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine (nifene) is a highly potent and selective nAChR agonist with subnanomolar affinity (6). 2-fluoro-3-[2-((s)-3-pyrrolinyl)methoxy]pyridine 0-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 16942759-4 2006 Here we determined if chronic nicotine treatment during a developmental period corresponding to the human third trimester regulates nAChR expression. Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 16942759-7 2006 Expression of heteromeric and homomeric nAChR receptor was evaluated by autoradiography using (125)I-epibatidine and (125)I-alphabungarotoxin, respectively. i-epibatidine 99-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 20641387-8 2004 2-Fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine (nifene) is a highly potent and selective nAChR agonist with subnanomolar affinity (6). nifene 50-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 16782754-5 2006 The aim of this study was to assess the role of these proteins in the signaling pathways involved in the anti-inflammatory effect of dimethylphenylpiperazinium (DMPP), a synthetic nAChR agonist, on monocytes and macrophages. Dimethylphenylpiperazinium Iodide 133-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 16782754-5 2006 The aim of this study was to assess the role of these proteins in the signaling pathways involved in the anti-inflammatory effect of dimethylphenylpiperazinium (DMPP), a synthetic nAChR agonist, on monocytes and macrophages. Dimethylphenylpiperazinium Iodide 161-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 16782754-8 2006 Treatment with DMPP for 24 and 48 h provoked a mild PLC phosphorylation, which was blocked by the nAChR antagonist mecamylamine and reversed by PI3K inhibitors. Dimethylphenylpiperazinium Iodide 15-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 16782754-8 2006 Treatment with DMPP for 24 and 48 h provoked a mild PLC phosphorylation, which was blocked by the nAChR antagonist mecamylamine and reversed by PI3K inhibitors. Mecamylamine 115-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 16782754-11 2006 DMPP also inhibited the thapsigargin-provoked calcium release, indicating that the endoplasmic reticulum calcium stores might be depleted by treatment with the nAChR agonist. Dimethylphenylpiperazinium Iodide 0-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 16782754-11 2006 DMPP also inhibited the thapsigargin-provoked calcium release, indicating that the endoplasmic reticulum calcium stores might be depleted by treatment with the nAChR agonist. Thapsigargin 24-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 16782754-11 2006 DMPP also inhibited the thapsigargin-provoked calcium release, indicating that the endoplasmic reticulum calcium stores might be depleted by treatment with the nAChR agonist. Calcium 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 16782754-11 2006 DMPP also inhibited the thapsigargin-provoked calcium release, indicating that the endoplasmic reticulum calcium stores might be depleted by treatment with the nAChR agonist. Calcium 105-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 16943556-4 2006 Stimulation of nAChR induced activation of PKC-epsilon, and inhibition of PKC-epsilon by expression of the dominant-negative mutant of PKC-epsilon (DN-PKC-epsilon) or short interfering (siRNA) against PKC-epsilon abolished ADP via decreasing the frequency and quantal size of fused vesicles without affecting basal exocytosis, suggesting that PKC-epsilon is specifically involved in ADP. Adenosine Diphosphate 383-386 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 16835749-7 2006 Exposure of BEP2D cells to either NNK or NNN in both cases increased their proliferative potential which could be abolished in the presence of nAChR antagonists alpha-bungarotoxin, which worked most effectively against NNK, or mecamylamine, which was most efficient against NNN. Mecamylamine 227-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 16837557-2 2006 The present studies were done to determine whether long-term nicotine treatment also protected against striatal nicotinic receptor (nAChR) losses after nigrostriatal damage. Nicotine 61-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 16837557-7 2006 Chronic nicotine treatment led to a small decrease in alpha3/alpha6beta2* nAChR subtypes. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 16837557-11 2006 In addition, the results showing an improvement in striatal alpha4beta2* and select alpha3/alpha6beta2* nAChR subtypes, combined with previous work, demonstrate that chronic nicotine treatment restores and/or protects against the loss of multiple molecular markers after nigrostriatal damage. Nicotine 174-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 16857741-6 2006 Sazetidine-A competes with very high binding affinity (Ki approximately 0.5 nM) and selectivity for the alpha4beta2 nAChR subtype (Ki ratio alpha3beta4/alpha4beta2 approximately 24,000). sazetidine-A 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-121 16857741-8 2006 However, when it is pre-incubated for 10 min with the receptors, it potently blocks nicotine-stimulated alpha4beta2 nAChR function (IC50 approximately 30 nM). Nicotine 84-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 116-121 16943556-2 2006 We showed previously that repetitive stimulation of nicotinic acetylcholine receptor (nAChR) induced activity-dependent potentiation (ADP) of large dense-core vesicle (LDCV) exocytosis in chromaffin cells. Adenosine Diphosphate 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 16825297-1 2006 Naturally expressed nicotinic acetylcholine receptors (nAChR) containing alpha4 subunits (alpha4*-nAChR) in combination with beta2 subunits (alpha4beta2-nAChR) are among the most abundant, high-affinity nicotine binding sites in the mammalian brain. Nicotine 203-211 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-53 16825297-1 2006 Naturally expressed nicotinic acetylcholine receptors (nAChR) containing alpha4 subunits (alpha4*-nAChR) in combination with beta2 subunits (alpha4beta2-nAChR) are among the most abundant, high-affinity nicotine binding sites in the mammalian brain. Nicotine 203-211 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 16825297-11 2006 Diversity in alpha4*-nAChR is of potential relevance to nervous system function, disease, and nicotine dependence. Nicotine 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 16716265-5 2006 Crystal structures of AChBP, a homologue of the nAChR ligand binding domain, have now been solved in complex with alpha-cobratoxin, alpha-conotoxin PnIA and alpha-conotoxin ImI. achbp 22-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 16716265-6 2006 The orientation of all three toxins in the ACh binding site confirms many of the predictions obtained from mutagenesis and docking simulations on homology models of mammalian nAChR. Acetylcholine 43-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 175-180 16943556-2 2006 We showed previously that repetitive stimulation of nicotinic acetylcholine receptor (nAChR) induced activity-dependent potentiation (ADP) of large dense-core vesicle (LDCV) exocytosis in chromaffin cells. Adenosine Diphosphate 134-137 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Cysteine 78-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 16943556-4 2006 Stimulation of nAChR induced activation of PKC-epsilon, and inhibition of PKC-epsilon by expression of the dominant-negative mutant of PKC-epsilon (DN-PKC-epsilon) or short interfering (siRNA) against PKC-epsilon abolished ADP via decreasing the frequency and quantal size of fused vesicles without affecting basal exocytosis, suggesting that PKC-epsilon is specifically involved in ADP. Adenosine Diphosphate 223-226 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 16751247-1 2006 The electrostatic environments near the acetylcholine binding sites on the nicotinic acetylcholine receptor (nAChR) and acetylcholinesterase were measured by diffusion-enhanced fluorescence energy transfer (DEFET) to determine the influence of long-range electrostatic interactions on ligand binding kinetics and net binding energy. Acetylcholine 40-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-107 16751247-1 2006 The electrostatic environments near the acetylcholine binding sites on the nicotinic acetylcholine receptor (nAChR) and acetylcholinesterase were measured by diffusion-enhanced fluorescence energy transfer (DEFET) to determine the influence of long-range electrostatic interactions on ligand binding kinetics and net binding energy. Acetylcholine 40-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 16751247-2 2006 Changes in DEFET from variously charged Tb3+ -chelates revealed net potentials of -20 mV at the nAChR agonist sites and -14 mV at the entrance to the AChE active site, in physiological ionic strength conditions. tb3+ 40-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 16751247-3 2006 The potential at the alphadelta-binding site of the nAChR was determined independently in the presence of d-tubocurarine to be -14 mV; the calculated potential at the alphagamma-site was approximately threefold stronger than at the alphadelta-site. Tubocurarine 106-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 16751249-1 2006 The electrostatic potentials within the pore of the nicotinic acetylcholine receptor (nAChR) were determined using lanthanide-based diffusion-enhanced fluorescence energy transfer experiments. Lanthanoid Series Elements 115-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 16751249-1 2006 The electrostatic potentials within the pore of the nicotinic acetylcholine receptor (nAChR) were determined using lanthanide-based diffusion-enhanced fluorescence energy transfer experiments. Lanthanoid Series Elements 115-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 16751249-2 2006 Freely diffusing Tb3+ -chelates of varying charge constituted a set of energy transfer donors to the acceptor, crystal violet, a noncompetitive antagonist of the nAChR. tb3+ 17-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 16751249-2 2006 Freely diffusing Tb3+ -chelates of varying charge constituted a set of energy transfer donors to the acceptor, crystal violet, a noncompetitive antagonist of the nAChR. Gentian Violet 111-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 16751249-3 2006 Energy transfer from a neutral Tb3+ -chelate to nAChR-bound crystal violet was reduced 95% relative to the energy transfer to free crystal violet. tb3+ 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 16751249-3 2006 Energy transfer from a neutral Tb3+ -chelate to nAChR-bound crystal violet was reduced 95% relative to the energy transfer to free crystal violet. Gentian Violet 60-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 16751249-3 2006 Energy transfer from a neutral Tb3+ -chelate to nAChR-bound crystal violet was reduced 95% relative to the energy transfer to free crystal violet. Gentian Violet 131-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 16751249-4 2006 This result indicated that crystal violet was strongly shielded from solvent when bound to the nAChR. Gentian Violet 27-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 17105949-8 2006 Interestingly, when the neurons were pre-exposed to alpha-bungarotoxin (antagonist of alpha7 nAChR), exposure to 10 microM of nicotine resulted in significant increases not only in alpha7 nAChR (25.5%) but also in alpha3 nAChR (32.2%). Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 17105949-8 2006 Interestingly, when the neurons were pre-exposed to alpha-bungarotoxin (antagonist of alpha7 nAChR), exposure to 10 microM of nicotine resulted in significant increases not only in alpha7 nAChR (25.5%) but also in alpha3 nAChR (32.2%). Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 17105949-8 2006 Interestingly, when the neurons were pre-exposed to alpha-bungarotoxin (antagonist of alpha7 nAChR), exposure to 10 microM of nicotine resulted in significant increases not only in alpha7 nAChR (25.5%) but also in alpha3 nAChR (32.2%). Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 17105949-9 2006 These results show that exposure to nicotine alters the nAChR levels differently in the neonatal sympathetic neurons in a subunit specific manner and suggest that the level of alpha7 as well as alpha3 nAChR is linked to the functional status of alpha7 nAChR in these neurons. Nicotine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 17105949-9 2006 These results show that exposure to nicotine alters the nAChR levels differently in the neonatal sympathetic neurons in a subunit specific manner and suggest that the level of alpha7 as well as alpha3 nAChR is linked to the functional status of alpha7 nAChR in these neurons. Nicotine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 201-206 17105949-9 2006 These results show that exposure to nicotine alters the nAChR levels differently in the neonatal sympathetic neurons in a subunit specific manner and suggest that the level of alpha7 as well as alpha3 nAChR is linked to the functional status of alpha7 nAChR in these neurons. Nicotine 36-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 201-206 16848798-6 2006 In support of the hypothesis, microinjection into layer 4 of the nonspecific nAChR antagonist mecamylamine (10 microM) strongly reduced sound-evoked responses. Mecamylamine 94-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 16720757-1 2006 alpha4 and beta2 nicotinic acetylcholine receptor (nAChR) subunits expressed heterologously assemble into receptors with high (HS) and low (LS) sensitivity to acetylcholine (ACh); their relative proportions depend on the alpha4to beta2 ratio. Acetylcholine 27-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 20641288-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). 3-[2(s)-2-azetidinylmethoxy]pyridine 0-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 20641288-6 2004 3-[2(S)-2-Azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective alpha4beta2 nAChR agonist with subnanomolar affinity (4, 5). A 85380 38-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Cysteine 78-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Glycine 217-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Glycine 217-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. gamma-Aminobutyric Acid 226-249 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. gamma-Aminobutyric Acid 226-249 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Serotonin 254-263 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 16829701-1 2006 The nicotinic acetylcholine receptor (nAChR) is the prototypic member of the "Cys-loop" superfamily of ligand-gated ion channels which mediate synaptic neurotransmission, and whose other members include receptors for glycine, gamma-aminobutyric acid and serotonin. Serotonin 254-263 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 16958984-1 2006 A-85380 [3-(2(s)-azetidinylmethoxy) pyridine] is a neuronal nicotinic acetylcholine receptor (nAChR) agonist that has been a useful tool in the investigation of the function of nAChRs in both preclinical and clinical studies. 3-(2(s)-azetidinylmethoxy) pyridine 9-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 16958984-1 2006 A-85380 [3-(2(s)-azetidinylmethoxy) pyridine] is a neuronal nicotinic acetylcholine receptor (nAChR) agonist that has been a useful tool in the investigation of the function of nAChRs in both preclinical and clinical studies. 3-(2(s)-azetidinylmethoxy) pyridine 9-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 16431111-0 2006 QSAR modeling of mono- and bis-quaternary ammonium salts that act as antagonists at neuronal nicotinic acetylcholine receptors mediating dopamine release. mono- and bis-quaternary ammonium salts 17-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-126 16485261-4 2006 In this study, we have examined the effects of chronic nicotine treatment on alpha7 and beta2 nAChR subunits in vitro in cell lines and in vivo in mouse striatum. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 16575903-9 2006 These results indicated that SLURP-2 competes with acetylcholine predominantly at the alpha3 nAChR, and that receptor ligation with SLURP-2 delays keratinocyte differentiation and prevents apoptosis. Acetylcholine 51-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 16505153-9 2006 Overall, these functional data agree with previous binding and behavioral findings and suggest collectively that 4-nitro-PFEB is the most effective and selective antagonist of alpha4beta2 versus alpha3beta4 and alpha7 nAChRs among the tested analogs, acting on alpha4beta2 nAChR through a competitive mechanism with a potency 17-fold higher than that of dihydro-beta-erythroidine. 4-nitro-pfeb 113-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 218-223 16431111-11 2006 The application of the ANN QSAR model has led to the successful discovery of six new compounds in this study with experimental IC50 values of less than 0.1 microM at nAChR subtypes responsible for mediating nicotine-evoked dopamine release, demonstrating that the ANN QSAR model is a valuable aid to drug discovery. Nicotine 207-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 16431111-0 2006 QSAR modeling of mono- and bis-quaternary ammonium salts that act as antagonists at neuronal nicotinic acetylcholine receptors mediating dopamine release. Dopamine 137-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-126 16431111-11 2006 The application of the ANN QSAR model has led to the successful discovery of six new compounds in this study with experimental IC50 values of less than 0.1 microM at nAChR subtypes responsible for mediating nicotine-evoked dopamine release, demonstrating that the ANN QSAR model is a valuable aid to drug discovery. Dopamine 223-231 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 16431111-1 2006 Back-propagation artificial neural networks (ANNs) were trained on a dataset of 42 molecules with quantitative IC50 values to model structure-activity relationships of mono- and bis-quaternary ammonium salts as antagonists at neuronal nicotinic acetylcholine receptors (nAChR) mediating nicotine-evoked dopamine release. Dopamine 303-311 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-268 16431111-1 2006 Back-propagation artificial neural networks (ANNs) were trained on a dataset of 42 molecules with quantitative IC50 values to model structure-activity relationships of mono- and bis-quaternary ammonium salts as antagonists at neuronal nicotinic acetylcholine receptors (nAChR) mediating nicotine-evoked dopamine release. mono- and bis-quaternary ammonium salts 168-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-268 16431111-1 2006 Back-propagation artificial neural networks (ANNs) were trained on a dataset of 42 molecules with quantitative IC50 values to model structure-activity relationships of mono- and bis-quaternary ammonium salts as antagonists at neuronal nicotinic acetylcholine receptors (nAChR) mediating nicotine-evoked dopamine release. mono- and bis-quaternary ammonium salts 168-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 270-275 16431111-1 2006 Back-propagation artificial neural networks (ANNs) were trained on a dataset of 42 molecules with quantitative IC50 values to model structure-activity relationships of mono- and bis-quaternary ammonium salts as antagonists at neuronal nicotinic acetylcholine receptors (nAChR) mediating nicotine-evoked dopamine release. Nicotine 287-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-268 16641249-4 2006 Nigrostriatal damage increased nicotinic acetylcholine receptor (nAChR)-mediated fractional dopamine release from residual terminals, primarily through changes in alpha3*/alpha6* nAChRs. Dopamine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-63 16817863-1 2006 We examined the binding of the novel nicotinic acetylcholine receptor (nAChR) ligand [125I]iodomethyllycaconitine (iodoMLA) in the brains of M. cynomologous (macaque) monkeys. [125i]iodomethyllycaconitine 85-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-69 16817863-1 2006 We examined the binding of the novel nicotinic acetylcholine receptor (nAChR) ligand [125I]iodomethyllycaconitine (iodoMLA) in the brains of M. cynomologous (macaque) monkeys. [125i]iodomethyllycaconitine 85-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 16817863-1 2006 We examined the binding of the novel nicotinic acetylcholine receptor (nAChR) ligand [125I]iodomethyllycaconitine (iodoMLA) in the brains of M. cynomologous (macaque) monkeys. iodomla 115-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-69 16817863-1 2006 We examined the binding of the novel nicotinic acetylcholine receptor (nAChR) ligand [125I]iodomethyllycaconitine (iodoMLA) in the brains of M. cynomologous (macaque) monkeys. iodomla 115-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 16647046-3 2006 Recently, we found that Ipt blocked nicotinic acetylcholine receptor (nAChR)-mediated currents in a heterologously expressed SH-EP1 cell line and in native midbrain dopamine neurons. N-(1-methylethyl)-1,1,2-trimethylpropylamine 24-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-68 16641249-4 2006 Nigrostriatal damage increased nicotinic acetylcholine receptor (nAChR)-mediated fractional dopamine release from residual terminals, primarily through changes in alpha3*/alpha6* nAChRs. Dopamine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 16647046-3 2006 Recently, we found that Ipt blocked nicotinic acetylcholine receptor (nAChR)-mediated currents in a heterologously expressed SH-EP1 cell line and in native midbrain dopamine neurons. N-(1-methylethyl)-1,1,2-trimethylpropylamine 24-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 16571968-3 2006 The aim of this study was to investigate the effect of succinylcholine on human muscle and neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Succinylcholine 55-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-132 16647046-3 2006 Recently, we found that Ipt blocked nicotinic acetylcholine receptor (nAChR)-mediated currents in a heterologously expressed SH-EP1 cell line and in native midbrain dopamine neurons. Dopamine 165-173 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 16571968-9 2006 CONCLUSION: Succinylcholine activates the muscle-type nAChR followed by desensitization. Succinylcholine 12-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 16571968-3 2006 The aim of this study was to investigate the effect of succinylcholine on human muscle and neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Succinylcholine 55-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 16496293-8 2006 Mechanisms contributing to deficient hypoxia response include the ability of nicotine to act as a cholinergic stimulant through nicotinic acetylcholine receptor (nAChR) binding. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 128-160 16608406-3 2006 The neuronal nicotinic acetylcholine receptor (neuronal nAChR) belongs to the superfamily of ionic channel activated by ligand. Acetylcholine 23-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 16306081-6 2006 Electron microscope analysis revealed that nAChR stimulation resulted in LDCV translocation to the plasma membrane and increase of fused LDCVs in response to repetitive stimulation was observed by amperometry. ldcv 73-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 16306081-8 2006 MAPK signaling was activated by nAChR-induced calcium influx, and ADP as well as vesicle translocation was suppressed by inhibition of MAPK signaling with MAPK kinase blockers, such as PD 098059 and U0126. Calcium 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 16306081-8 2006 MAPK signaling was activated by nAChR-induced calcium influx, and ADP as well as vesicle translocation was suppressed by inhibition of MAPK signaling with MAPK kinase blockers, such as PD 098059 and U0126. U 0126 199-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 16337724-5 2006 Toluene is an abused solvent affecting neuronal signal transduction by influencing the function of ligand gated ion channel receptors, including nicotinic acetylcholine receptors (nAChR), P2X purinoceptors, [gamma]-aminobutyric acid type A (GABAA) receptors, etc. Toluene 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-178 16337724-5 2006 Toluene is an abused solvent affecting neuronal signal transduction by influencing the function of ligand gated ion channel receptors, including nicotinic acetylcholine receptors (nAChR), P2X purinoceptors, [gamma]-aminobutyric acid type A (GABAA) receptors, etc. Toluene 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 180-185 16496293-8 2006 Mechanisms contributing to deficient hypoxia response include the ability of nicotine to act as a cholinergic stimulant through nicotinic acetylcholine receptor (nAChR) binding. Nicotine 77-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 17192629-1 2006 Pentameric ligand-gated ion channels (LGICs) are fast-gating receptors, represented by cationic nicotinic acetylcholine (nAChR) and serotonin (5HT3R) receptors, and by anionic GABA and glycine (GlyR) receptors. Acetylcholine 106-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 16472136-2 2006 Over recent years, the application of newly developed molecular and cellular biological techniques has made it possible to correlate the subunit composition of nAChRs with specific nicotine-elicited behaviours, and refine some of the in vivo physiological functions of nAChR subtypes. Nicotine 181-189 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 16223869-3 2006 In the present study, we used patch-clamp whole-cell recording and pharmacological manipulations to evaluate effects of iptakalim hydrochloride (Ipt), which is a drug reported to act as an ATP-sensitive potassium (K(ATP)) channel opener, on selected human nAChRs heterologously expressed in the native nAChR-null SH-EP1 human epithelial cell line. Iptakalim (hydrochloride) 120-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 256-261 16223869-3 2006 In the present study, we used patch-clamp whole-cell recording and pharmacological manipulations to evaluate effects of iptakalim hydrochloride (Ipt), which is a drug reported to act as an ATP-sensitive potassium (K(ATP)) channel opener, on selected human nAChRs heterologously expressed in the native nAChR-null SH-EP1 human epithelial cell line. isoprothiolane 145-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 256-261 16223869-7 2006 Other studies discount effects of Ipt on nAChR internalization or involvement of K(ATP) channels in Ipt-induced inhibition of alpha4beta2-nAChR function. isoprothiolane 34-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 16223869-7 2006 Other studies discount effects of Ipt on nAChR internalization or involvement of K(ATP) channels in Ipt-induced inhibition of alpha4beta2-nAChR function. isoprothiolane 100-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 16430227-5 2006 The unprecedented binding selectivity for the fetal muscle nAChR, coupled with the kinetic diversity, should make alphaA(S)-conotoxins useful ligands for a diverse set of studies. alphaa(s)-conotoxins 114-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 16594641-2 2006 Nicotine is a lipophilic molecule whose effects on neuronal nicotinic acetylcholine receptors (nAChR) have been primarily focused on its physiologic impact within the confines of the brain and peripheral nervous system. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-93 16594641-2 2006 Nicotine is a lipophilic molecule whose effects on neuronal nicotinic acetylcholine receptors (nAChR) have been primarily focused on its physiologic impact within the confines of the brain and peripheral nervous system. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 17192656-0 2006 Structural and functional changes induced in the nicotinic acetylcholine receptor by membrane phospholipids. Phospholipids 94-107 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-81 16273122-2 2005 The present study investigated the effect of the novel cytisine dimer 1,2-bisN-cytisinylethane (CC4) on nAChR natively expressed by SH-SY5Y neuroblastoma cells in culture. cytisine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 17192677-2 2006 Recently, we have shown that 1,5-bis(4-allyldimethyl ammonium phenyl) pentan-3-one dibromide (BW284c51), a quaternary ammonium cholinesterase inhibitor (QChEI), selectively inhibits nicotinic currents (IACh) by blocking the nAChR channel (Olivera et al., 2005). 1,5-bis(4-allyldimethyl ammonium phenyl) pentan-3-one dibromide 29-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 224-229 17192677-2 2006 Recently, we have shown that 1,5-bis(4-allyldimethyl ammonium phenyl) pentan-3-one dibromide (BW284c51), a quaternary ammonium cholinesterase inhibitor (QChEI), selectively inhibits nicotinic currents (IACh) by blocking the nAChR channel (Olivera et al., 2005). Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 224-229 16273122-2 2005 The present study investigated the effect of the novel cytisine dimer 1,2-bisN-cytisinylethane (CC4) on nAChR natively expressed by SH-SY5Y neuroblastoma cells in culture. 1,2-bisn-cytisinylethane 70-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 16273122-2 2005 The present study investigated the effect of the novel cytisine dimer 1,2-bisN-cytisinylethane (CC4) on nAChR natively expressed by SH-SY5Y neuroblastoma cells in culture. CC4 96-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 16332175-0 2005 Polymorphisms of the CHRNA4 gene encoding the alpha4 subunit of nicotinic acetylcholine receptor as related to the oxidative DNA damage and the level of apoptotic proteins in lymphocytes of the patients with Alzheimer"s disease. Acetylcholine 74-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-27 16332175-1 2005 The study aimed at the analysis of polymorphisms in the gene coding for the nicotinic acetylcholine receptor alpha4 subunit (CHRNA4) and the evaluation of the extent of the oxidative damage to DNA (8-oxo2dG), as well as the level of proteins participating in DNA repair (p53, PARP) and DNA degradation (Bax:Bcl-2, 85-kDa fragment) in the peripheral blood lymphocytes of the patients suffering from Alzheimer"s disease (AD) and in the healthy individuals of the control group. Acetylcholine 86-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-131 16354194-3 2005 SLURP-1 ligated the conventional ligand-binding site of KC nAChR, showing a higher affinity to the [(3)H]nicotine-, compared with the [(3)H]epibatidine-sensitive nAChR. Nicotine 105-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 16332175-4 2005 In the AD patients with the CHRNA4 polymorphisms the highest level of 8-oxo2dG and of proteins involved in DNA repair were documented in patients with polymorphisms in exon 5, in contrast to the patients with polymorphisms in intron 5. 8-oxo2dg 70-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-34 16354194-7 2005 In the presence of the agonist carbachol, the effects of SLURP-1 on gene expression were augmented, which is in keeping with the notion that SLURP-1 acts as an allosteric agonist at the KC nAChR. Carbachol 31-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). Choline 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). Choline 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 152-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 152-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 172-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 16421212-4 2005 Choline (2.5, 5 and 10 mM), a highly specific but low potency agonist of the alpha7 nAChR initiated AR, with its effect blocked by the nAChR antagonist methyllycaconitine (MLA). methyllycaconitine 172-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 16421212-6 2005 The nAChR antagonists, alpha-bungarotoxin (alpha-BTX) and MLA, reduced the ACh-initiated Ca2+ rise by 75 and 78%, respectively, demonstrating the majority of the rise is mediated through nAChRs containing alpha7 or alpha9 subunits. methyllycaconitine 58-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 16251431-5 2005 Tyrosine kinase inhibition by genistein decreased alpha7 nAChR phosphorylation but strongly increased acetylcholine-evoked currents, whereas tyrosine phosphatase inhibition by pervanadate produced opposite effects. Genistein 30-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 16226123-3 2005 It binds to the acetylcholine binding site of the alpha-subunits of nicotinic acetylcholine receptors (nAChR). Acetylcholine 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-101 16226123-3 2005 It binds to the acetylcholine binding site of the alpha-subunits of nicotinic acetylcholine receptors (nAChR). Acetylcholine 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 16226123-9 2005 ACh is suggested to be an important placental signalling molecule that, through stimulation of nAChR, controls the uptake of nutrients, blood flow and fluid volume in placental vessels, and the vascularisation during placental development. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 16226123-10 2005 Chronic stimulation of nAChR by nicotine might result in unbalanced receptor activation or functional desensitisation followed by the known pathological effects of smoking. Nicotine 32-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 16194573-1 2005 The molecular determinants of the ionic selectivity and single-channel conductance of the Cys-loop family of transmitter-gated ion channels are beginning to be understood with increasing precision, in part, as a result of the recent availability of refined ultrastructural information for the archetype of the family, the nicotinic acetylcholine receptor (nAChR). Cysteine 90-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 322-354 16194573-1 2005 The molecular determinants of the ionic selectivity and single-channel conductance of the Cys-loop family of transmitter-gated ion channels are beginning to be understood with increasing precision, in part, as a result of the recent availability of refined ultrastructural information for the archetype of the family, the nicotinic acetylcholine receptor (nAChR). Cysteine 90-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 356-361 16353944-0 2005 Molecular modeling of mono- and bis-quaternary ammonium salts as ligands at the alpha4beta2 nicotinic acetylcholine receptor subtype using nonlinear techniques. mono- and bis-quaternary ammonium salts 22-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-124 16218635-1 2005 A variety of molecular modeling, molecular docking, and first-principles electronic structure calculations were performed to study how the alpha4beta2 nicotinic acetylcholine receptor (nAChR) binds with different species of two typical agonists, (S)-(-)-nicotine and (R)-(-)-deschloroepibatidine, each of which is distinguished by different free bases and protonation states. Nicotine 246-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 16218635-1 2005 A variety of molecular modeling, molecular docking, and first-principles electronic structure calculations were performed to study how the alpha4beta2 nicotinic acetylcholine receptor (nAChR) binds with different species of two typical agonists, (S)-(-)-nicotine and (R)-(-)-deschloroepibatidine, each of which is distinguished by different free bases and protonation states. (r)-(-)-deschloroepibatidine 267-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 16181622-7 2005 The nAChR subtypes that mediate the locomotor effects and hypothermic effects of nicotine appear to be less sensitive to TMPH than those which mediate analgetic effects and discriminative stimuli. Nicotine 81-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 16181622-7 2005 The nAChR subtypes that mediate the locomotor effects and hypothermic effects of nicotine appear to be less sensitive to TMPH than those which mediate analgetic effects and discriminative stimuli. 2,2,6,6-tetramethylpiperidin-4-yl heptanoate 121-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 16116270-4 2005 A rich diversity of neonicotinoid-nAChR interactions has been demonstrated using voltage-clamp electrophysiology. Neonicotinoids 20-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 16174432-6 2005 A total of 54 compounds, showing more than 60% competitive inhibition on [(3)H]cytisine binding to alpha4beta2 nAChR, were identified initially following an HTS campaign. [(3)h]cytisine 73-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 15970304-3 2005 Solitary wasp venoms caused significant voltage-dependent antagonism of nAChR responses to 10 microM ACh and NMDAR responses to 100 microM NMDA (+10 microM glycine) when co-applied at 1 microg/ml with the agonists. Glycine 156-163 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 15970304-6 2005 Of four social wasp venoms, one acted on nAChR by potentiating responses to 10 ACh, while another generated an ACh-like response when applied alone. Acetylcholine 79-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 15894420-3 2005 When receptor bound, on the other hand, significant differences in the conformational dynamics of the reporter groups were observed with the C-terminal Lys(69) derivative displaying by far the greatest mobility strongly suggesting that the C-terminal domain of the bound neurotoxin is highly mobile and does not participate in the toxin-nAChR binding surface. Lysine 152-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 337-342 16039849-0 2005 Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-121 16115980-0 2005 Antiemetics of the 5-hydroxytryptamine 3A antagonist class inhibit muscle nicotinic acetylcholine receptors. 5-hydroxytryptamine 3a 19-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-107 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Ondansetron 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Ondansetron 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Ondansetron 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. dolasetron 25-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 16115980-9 2005 Again, hydrodolasetron showed significantly (10 times) more inhibitory potency on the adult nAChR than the parent compound dolasetron. hydrodolasetron 7-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 16115980-9 2005 Again, hydrodolasetron showed significantly (10 times) more inhibitory potency on the adult nAChR than the parent compound dolasetron. dolasetron 12-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 15947037-9 2005 Surprisingly, alpha-bungarotoxin, a specific antagonist of the nicotinic acetylcholine receptor (nAChR), abolished these MDMA effects. N-Methyl-3,4-methylenedioxyamphetamine 121-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-95 15947037-9 2005 Surprisingly, alpha-bungarotoxin, a specific antagonist of the nicotinic acetylcholine receptor (nAChR), abolished these MDMA effects. N-Methyl-3,4-methylenedioxyamphetamine 121-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 15933214-4 2005 Initial characterization of nicotine-evoked [3H]dopamine release from monkey striatal synaptosomes revealed that release was calcium-dependent and inhibited by selective nAChR antagonists. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 15933214-4 2005 Initial characterization of nicotine-evoked [3H]dopamine release from monkey striatal synaptosomes revealed that release was calcium-dependent and inhibited by selective nAChR antagonists. 3H-dopamine 44-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 15933214-4 2005 Initial characterization of nicotine-evoked [3H]dopamine release from monkey striatal synaptosomes revealed that release was calcium-dependent and inhibited by selective nAChR antagonists. Calcium 125-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 15933214-8 2005 In contrast, alpha3*/alpha6* nAChR-evoked [3H]dopamine release was reduced in caudate but not putamen, demonstrating a dissociation between nAChR sites and function. 3h]dopamine 43-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 15933214-12 2005 These results show a selective preservation of alpha3*/alpha6* nAChR-mediated function in the nigrostriatal and mesolimbic dopamine systems after nigrostriatal damage. Dopamine 123-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. N-n-octylnicotinium 0-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. N-n-octylnicotinium 28-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. n-n-decylnicotinium iodide 38-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. ndni 66-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. Nicotine 135-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. Dopamine 160-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. Dopamine 170-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. Tritium 199-201 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 16146341-1 2005 N-n-octylnicotinium iodide (NONI) and N-n-decylnicotinium iodide (NDNI) are selective nicotinic receptor (nAChR) antagonists mediating nicotine-evoked striatal dopamine (DA) release, and inhibiting [3H]nicotine binding, respectively. Nicotine 202-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 15937519-1 2005 In this study, we have examined cellular responses of neuroblastoma SH-SY5Y cells after chronic treatment with galantamine, a drug used to treat Alzheimer"s disease that has a dual mechanism of action: inhibition of acetylcholinesterase and allosteric potentiation of nicotinic acetylcholine receptors (nAChR). Galantamine 111-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-301 15937519-1 2005 In this study, we have examined cellular responses of neuroblastoma SH-SY5Y cells after chronic treatment with galantamine, a drug used to treat Alzheimer"s disease that has a dual mechanism of action: inhibition of acetylcholinesterase and allosteric potentiation of nicotinic acetylcholine receptors (nAChR). Galantamine 111-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 303-308 15937519-8 2005 These observations support the hypothesis that chronic galantamine exerts its effects through interaction with nAChR in this cell line. Galantamine 55-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 15937519-11 2005 Thus, chronic galantamine acts at nAChR to decrease subsequent functional responses to acute stimulation with nicotine or KCl. Galantamine 14-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 15937519-11 2005 Thus, chronic galantamine acts at nAChR to decrease subsequent functional responses to acute stimulation with nicotine or KCl. Nicotine 110-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 15937519-11 2005 Thus, chronic galantamine acts at nAChR to decrease subsequent functional responses to acute stimulation with nicotine or KCl. Potassium Chloride 122-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 16116270-5 2005 Computational modeling of nAChR-imidacloprid interaction has assisted in the interpretation of these results. imidacloprid 32-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 15887955-4 2005 Varenicline displays high alpha4beta2 nAChR affinity and the desired in vivo dopaminergic profile. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 15772292-10 2005 nAChR beta4 subunit levels are significantly decreased after treatment with puromycin. Puromycin 76-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 15834443-6 2005 Galantamine, at a concentration of 0.1 microM, increased the amplitude of acetylcholine (ACh)-induced ion currents in the human alpha7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 15834443-6 2005 Galantamine, at a concentration of 0.1 microM, increased the amplitude of acetylcholine (ACh)-induced ion currents in the human alpha7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. Acetylcholine 74-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 15834443-6 2005 Galantamine, at a concentration of 0.1 microM, increased the amplitude of acetylcholine (ACh)-induced ion currents in the human alpha7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. Acetylcholine 89-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 15834443-9 2005 The same enhancing effect was obtained in oocytes transplanted with Torpedo nicotinic acetylcholine receptor (AChR) isolated from the electric organ, but in this case the optimal concentration of galantamine was 1 microM. Galantamine 196-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-108 15790597-0 2005 Ethnic- and gender-specific association of the nicotinic acetylcholine receptor alpha4 subunit gene (CHRNA4) with nicotine dependence. Nicotine 114-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-107 15741168-1 2005 The primary target for nicotine in the brain is the neuronal nicotinic acetylcholine receptor (nAChR). Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-93 15741168-1 2005 The primary target for nicotine in the brain is the neuronal nicotinic acetylcholine receptor (nAChR). Nicotine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 15741168-3 2005 In order to investigate the mechanism of nicotine-induced nAChR up-regulation, we have developed a cell culture system to assess membrane trafficking and nicotine-induced up-regulation of surface-expressed alpha(4)beta(2) nAChRs. Nicotine 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 58-63 15790597-8 2005 In summary, our findings provide convincing evidence for the involvement of the nAChR alpha4 subunit, but not of the nAChR beta2 subunit, in nicotine addiction. Nicotine 141-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 15858066-10 2005 Together, these results suggest that PNU-120596 represents a new class of molecule that enhances alpha7 nAChR function and thus has the potential to treat psychiatric and neurological disorders. N-neopentyl-N-nitrosourea 37-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15781147-1 2005 The alpha7 nicotinic acetylcholine receptor (nAChR)-selective partial agonist tropisetron is a conjugate of an indole and a tropane group. indole 111-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 15781147-1 2005 The alpha7 nicotinic acetylcholine receptor (nAChR)-selective partial agonist tropisetron is a conjugate of an indole and a tropane group. Tropanes 124-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 15808471-1 2005 A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as alpha7 neuronal nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore model. 2-(arylmethyl)-3-substituted quinuclidines 12-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 15808471-3 2005 One member of the series, (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan-2-carboxamide (+)-8l), has potent agonistic activity for the alpha7 nAChR (EC(50)=33nM, I(max)=1.0), at concentrations below those that result in desensitization. (+)-n-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan-2-carboxamide (+)-8l 26-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 15820238-2 2005 To investigate differences in sensitivity to smoking cues between schizophrenia and control subjects, we compared smoking cue reactivity (CR) in schizophrenia versus control smokers with and without pretreatment with the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine (MEC). Mecamylamine 273-285 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-253 15809354-2 2005 Based on recent studies showing that acetylcholine and other cholinergic mediators suppress the production of proinflammatory cytokines via the alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) expressed by macrophages and our observations that human microvascular endothelial cells express the alpha7 nAChR, we examined the effect of cholinergic stimulation on endothelial cell activation in vitro and in vivo. Acetylcholine 37-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 15809354-2 2005 Based on recent studies showing that acetylcholine and other cholinergic mediators suppress the production of proinflammatory cytokines via the alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) expressed by macrophages and our observations that human microvascular endothelial cells express the alpha7 nAChR, we examined the effect of cholinergic stimulation on endothelial cell activation in vitro and in vivo. Acetylcholine 37-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 307-312 15809354-5 2005 Mecamylamine, an nAChR antagonist, reversed the inhibition of endothelial cell activation by both cholinergic agonists, confirming the antiinflammatory role of the nAChR cholinergic pathway. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 15809354-5 2005 Mecamylamine, an nAChR antagonist, reversed the inhibition of endothelial cell activation by both cholinergic agonists, confirming the antiinflammatory role of the nAChR cholinergic pathway. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 15820238-2 2005 To investigate differences in sensitivity to smoking cues between schizophrenia and control subjects, we compared smoking cue reactivity (CR) in schizophrenia versus control smokers with and without pretreatment with the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine (MEC). Mecamylamine 273-285 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 255-260 15820238-9 2005 CONCLUSIONS: Our findings suggest that blockade of CR by MEC may be more robust in schizophrenia versus control smokers, possibly due to reduced nAChR levels in the brains of patients with schizophrenia. Chromium 51-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 15626708-2 2005 Gel shift assays and carbohydrate-specific staining show that the deglycosylation enzyme, Endo F1, removes at least 50% of membrane-reconstituted nAChR glycosylation. Carbohydrates 21-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. Acetylcholine 25-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. 6-chloropyridazine 221-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. 3,8-Diazabicyclo[3.2.1]octane 263-292 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. 2,5-diazabicyclo[2.2.1]heptane 294-324 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. Piperazine 334-344 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. 1,4-diazepane 349-363 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15813854-4 2005 Nicotine-induced adhesion of HSPC was inhibited by mecamylamine, a non-selective nicotinic acetylcholine receptor (nAchR) antagonist. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-113 15813854-4 2005 Nicotine-induced adhesion of HSPC was inhibited by mecamylamine, a non-selective nicotinic acetylcholine receptor (nAchR) antagonist. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 15813854-4 2005 Nicotine-induced adhesion of HSPC was inhibited by mecamylamine, a non-selective nicotinic acetylcholine receptor (nAchR) antagonist. Mecamylamine 51-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-113 15813854-4 2005 Nicotine-induced adhesion of HSPC was inhibited by mecamylamine, a non-selective nicotinic acetylcholine receptor (nAchR) antagonist. Mecamylamine 51-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 15813854-6 2005 Nicotine induced fast cytoskeletal reorganization and formation of filopodia in endothelial cells through interaction with the non-neuronal nAchR expressed by these cells. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 15770102-1 2005 BACKGROUND: The finding that most people with alcoholism are also heavy smokers prompted several research groups to evaluate the effects of ethanol on neuronal nicotinic acetylcholine receptor (nAChR) function. Ethanol 140-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 15770102-2 2005 Data collected in vitro indicate that physiologically relevant concentrations of ethanol inhibit the functional activation of homomeric alpha7 nAChRs, which are one of the most abundant nAChR subtypes expressed in the mammalian brain. Ethanol 81-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 15807510-1 2005 3-Pyridyl ethers are excellent nAChRs ligands, which show high subtype selectivity and binding affinity to alpha4beta2 nAChR. 3-pyridyl ethers 0-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-36 15588326-0 2004 Nicotine signals through muscle-type and neuronal nicotinic acetylcholine receptors in both human bronchial epithelial cells and airway fibroblasts. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-83 15356217-3 2005 Cells expressing subunits needed to form alpha6beta4beta3alpha5 nAChR exhibited saturable [(3)H]epibatidine binding (K(d) = 95.9 +/- 8.3 pM and B(max) = 84.5 +/- 1.6 fmol/mg of protein). epibatidine 96-107 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 15356217-5 2005 6-Hydroxydopamine lesioning studies indicated that beta3 and alpha5 subunits are likely partners of the alpha6 subunits in nAChR expressed in dopaminergic cell bodies. Oxidopamine 0-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 15617729-5 2005 MG 624, a novel selective nAChR antagonist, inhibited cortical [3H]DA by 53%, but had no effect on striatal release. triethyl-(beta-4-stilbenoxyethyl)ammonium 0-6 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 15679359-5 2005 The noncompetitive inhibitors (NCIs) of the nAChR (R)- and (S)-mecamylamine, phencylcidine, dextromethoprphan, and levomethorphan were also chromatographed on the columns using nonlinear chromatography techniques. Ranolazine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 15574706-7 2005 The model offers new insight into the water transport across the (alpha4)2(beta2)3 nAChR channel, and may lead to a better understanding of the structures, dynamics, and functions of this family of ion channels. Water 38-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 15725747-7 2005 Our data provide evidence that by targeting the nicotinic acetylcholine receptor (nAChR) nicotine interferes with the fetal development of the hematopoietic system. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 15725747-7 2005 Our data provide evidence that by targeting the nicotinic acetylcholine receptor (nAChR) nicotine interferes with the fetal development of the hematopoietic system. Nicotine 89-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 15639548-3 2005 Recent data suggest a role for cholinergic stimulation, especially the alpha7 nicotinic acetylcholine receptors (nAChR), in beta-amyloid-mediated neurotoxicity. Acetylcholine 88-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 15639548-4 2005 As galantamine is a modest acetylcholinesterase inhibitor in addition to being an allosteric modulator of nicotinic acetylcholine receptors, it is interesting to study the clinical effects of this compound in the light of its neurochemical properties to discern potential neuroprotective effects. Galantamine 3-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-139 15618790-9 2005 Isoflurane blocked the nAChR in both resting and activated states. Isoflurane 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 15618790-13 2005 CONCLUSIONS: Isoflurane, sevoflurane, and halothane potently blocked the alpha4beta2 nAChR. Isoflurane 13-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 15618790-13 2005 CONCLUSIONS: Isoflurane, sevoflurane, and halothane potently blocked the alpha4beta2 nAChR. Sevoflurane 25-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 15618790-13 2005 CONCLUSIONS: Isoflurane, sevoflurane, and halothane potently blocked the alpha4beta2 nAChR. Halothane 42-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 15983732-0 2005 Inhibition by 2,4-toluene diisocyanate of the calcium signaling of neuronal nicotinic acetylcholine receptors in human neuroblastoma SH-SY5Y cells. Toluene 2,4-Diisocyanate 14-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-109 15983732-0 2005 Inhibition by 2,4-toluene diisocyanate of the calcium signaling of neuronal nicotinic acetylcholine receptors in human neuroblastoma SH-SY5Y cells. Calcium 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-109 15983732-3 2005 TDI-induced asthma is related to its disturbance of acetylcholine in most affected workers but the actions of TDI on nicotinic acetylcholine receptors (nAChR) are unclear. Toluene 2,4-Diisocyanate 110-113 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 15983732-4 2005 In order to understand the role of TDI acting on nAChR, we used human neuroblastoma SH-SY5Y cells to investigate the effects of TDI on cytosolic free calcium concentration ([Ca2+]c) changes under the stimulation of nAChR. Toluene 2,4-Diisocyanate 35-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 15983732-7 2005 Our study of TDI acting on human nAChR suggests a possibility that the human nerve system plays some role in the toxicity of TDI in the pulmonary system. Toluene 2,4-Diisocyanate 13-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 15794887-6 2005 Prior treatment with antioxidant resulted in preventing the decrease of nAChR protein in cells exposed to the high doses of fluoride. Fluorides 124-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 72-77 15588326-12 2004 CONCLUSIONS: These results suggest that muscle-type and neuronal-type nAChRs are functional in airway fibroblasts and HBE cells, that prior tobacco exposure does not appear to be an important variable in nAChR expression, and that distinct signaling pathways are observed in response to nicotine. Nicotine 287-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 15519158-4 2004 This was used to identify the important atoms/fragments related to dispersive/van der Waals interactions of neonicotinoids with the nicotinic acetylcholine receptor (nAChR). Neonicotinoids 108-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 15519158-4 2004 This was used to identify the important atoms/fragments related to dispersive/van der Waals interactions of neonicotinoids with the nicotinic acetylcholine receptor (nAChR). Neonicotinoids 108-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 15519763-5 2004 Miyazawa, Fujiyoshi, and Unwin published a 4A resolution structure of the nAChR, and proposed that a single residue--valine 44 in Loop 2 of the extracellular domain--functions as a critical determinant of a "pin-into-socket" mechanism for receptor activation in nAChR. Valine 117-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 15798902-0 2004 Selection of 2"-fluoro-modified RNA aptamers for alleviation of cocaine and MK-801 inhibition of the nicotinic acetylcholine receptor. Dizocilpine Maleate 76-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-133 15798902-2 2004 Many therapeutic agents and abused drugs inhibit the nAChR, including the anti-convulsant MK-801 and the abused drug cocaine. Dizocilpine Maleate 90-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 15798902-2 2004 Many therapeutic agents and abused drugs inhibit the nAChR, including the anti-convulsant MK-801 and the abused drug cocaine. Cocaine 117-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 15798902-9 2004 The second class binds with equal or higher affinity to the cocaine-binding site on the open-channel form and, as predicted by the mechanism, does not inhibit the receptor, and does alleviate cocaine and MK-801 inhibition of the nAChR. Cocaine 60-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 229-234 15798902-9 2004 The second class binds with equal or higher affinity to the cocaine-binding site on the open-channel form and, as predicted by the mechanism, does not inhibit the receptor, and does alleviate cocaine and MK-801 inhibition of the nAChR. Cocaine 192-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 229-234 15798902-9 2004 The second class binds with equal or higher affinity to the cocaine-binding site on the open-channel form and, as predicted by the mechanism, does not inhibit the receptor, and does alleviate cocaine and MK-801 inhibition of the nAChR. Dizocilpine Maleate 204-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 229-234 15519763-2 2004 This gene superfamily includes the nicotinic acetylcholine (nAChR), GABA(A), 5-hydroxytryptamine type 3, and glycine receptors. Acetylcholine 45-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 15519763-5 2004 Miyazawa, Fujiyoshi, and Unwin published a 4A resolution structure of the nAChR, and proposed that a single residue--valine 44 in Loop 2 of the extracellular domain--functions as a critical determinant of a "pin-into-socket" mechanism for receptor activation in nAChR. Valine 117-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 262-267 15519763-7 2004 We mutated residues corresponding to nAChR valine 44 in the GABA(A) (alpha(1) histidine 56 and beta(2) valine 53) and glycine (alpha(1) threonine 54) receptors. Valine 43-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 15519763-7 2004 We mutated residues corresponding to nAChR valine 44 in the GABA(A) (alpha(1) histidine 56 and beta(2) valine 53) and glycine (alpha(1) threonine 54) receptors. gamma-Aminobutyric Acid 60-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 15519763-7 2004 We mutated residues corresponding to nAChR valine 44 in the GABA(A) (alpha(1) histidine 56 and beta(2) valine 53) and glycine (alpha(1) threonine 54) receptors. Histidine 78-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 15519763-7 2004 We mutated residues corresponding to nAChR valine 44 in the GABA(A) (alpha(1) histidine 56 and beta(2) valine 53) and glycine (alpha(1) threonine 54) receptors. Valine 103-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 15519763-7 2004 We mutated residues corresponding to nAChR valine 44 in the GABA(A) (alpha(1) histidine 56 and beta(2) valine 53) and glycine (alpha(1) threonine 54) receptors. Threonine 136-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 15902904-1 2004 Findings obtained from several studies indicate that ethanol enhances the activity of alpha4beta2 neuronal nicotinic acetylcholine receptor and support the possibility that a polymorphism of the nicotinic acetylcholine receptor alpha4 subunit gene (CHRNA4) modulates enhancement of nicotinic receptor function by ethanol. Ethanol 53-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 249-255 15902904-1 2004 Findings obtained from several studies indicate that ethanol enhances the activity of alpha4beta2 neuronal nicotinic acetylcholine receptor and support the possibility that a polymorphism of the nicotinic acetylcholine receptor alpha4 subunit gene (CHRNA4) modulates enhancement of nicotinic receptor function by ethanol. Ethanol 313-320 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 249-255 15336274-1 2004 Phenylcarbamate derivatives were synthesized and evaluated in radioligand binding assays for different nicotinic acetylcholine receptor (nAChR) subtypes. Phenylcarbamates 0-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 15474055-1 2004 The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. epibatidine 45-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-180 15474055-1 2004 The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. epibatidine 45-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 15474055-1 2004 The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. fluoronorchloroepibatidine 76-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-180 15474055-1 2004 The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. fluoronorchloroepibatidine 76-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 15474055-3 2004 The binding affinity of (+)-NCFHEB (K(i): 0.064 nM) and (-)-NCFHEB (K(i): 0.112 nM) to human alpha4beta2 nAChR is in the same order of magnitude as that of epibatidine (K(i): 0.014 nM). epibatidine 156-167 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 15336274-1 2004 Phenylcarbamate derivatives were synthesized and evaluated in radioligand binding assays for different nicotinic acetylcholine receptor (nAChR) subtypes. Phenylcarbamates 0-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 15336274-2 2004 Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. Carbamates 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-117 15336274-2 2004 Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. pyrrolidine 32-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-117 15336274-2 2004 Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. piperidine 47-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-117 15336274-2 2004 Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. Quinuclidines 144-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-117 15336274-3 2004 Furthermore, in contrast to the quinuclidine analogues 21-25, all (S)-pyrrolidine derivatives 8-12 and the piperidine analogues 15 and 16 exhibited higher affinities for alpha4beta2* nAChR. pyrrolidine 66-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 15336274-3 2004 Furthermore, in contrast to the quinuclidine analogues 21-25, all (S)-pyrrolidine derivatives 8-12 and the piperidine analogues 15 and 16 exhibited higher affinities for alpha4beta2* nAChR. piperidine 107-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 15234980-10 2004 Sensitivity to Abeta(1-42) antagonism at 1 nm was evident for halpha4beta2-nAChRs, but not for heterologously expressed human alpha7-nAChRs, although both nAChR subtypes were functionally inhibited by 100 nm Abeta(1-42), with the magnitude of functional block being higher for 100 nm Abeta(1-42) acting on halpha7-nAChRs. UNII-042A8N37WH 15-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 15347712-4 2004 123I-5IA shows higher affinity toward the nAChR alpha4beta2 subtype, enhanced receptor subtype selectivity, good safety, and low nonspecific binding. 123i-5ia 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 15223309-3 2004 Resting membrane potentials of muscle fibres exposed to the toxin were similar to control values, and the binding of FITC-labelled alpha-bungarotoxin to nAChR at the neuromuscular junction was unchanged. Fluorescein-5-isothiocyanate 117-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-158 15212808-3 2004 In this study, we investigated the effects of eight phthalates on the calcium signaling of human nAChR by using human neuroblastoma SH-SY5Y cells. Calcium 70-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 15212808-4 2004 All eight phthalates, with different potency, have inhibitory roles on the calcium signaling coupled with human nAChR, but not muscarinic acetylcholine receptors (mAChRs). Calcium 75-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 15212808-7 2004 At as low as 0.1 microM, DPP, DBP, BBP, DCHP and DHP significantly inhibited the calcium signaling of human nAChR. di-n-pentyl phthalate 25-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 15212808-7 2004 At as low as 0.1 microM, DPP, DBP, BBP, DCHP and DHP significantly inhibited the calcium signaling of human nAChR. Dibutyl Phthalate 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 15212808-7 2004 At as low as 0.1 microM, DPP, DBP, BBP, DCHP and DHP significantly inhibited the calcium signaling of human nAChR. butylbenzyl phthalate 35-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 15212808-7 2004 At as low as 0.1 microM, DPP, DBP, BBP, DCHP and DHP significantly inhibited the calcium signaling of human nAChR. di-n-hexyl phthalate 49-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 15212808-7 2004 At as low as 0.1 microM, DPP, DBP, BBP, DCHP and DHP significantly inhibited the calcium signaling of human nAChR. Calcium 81-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 15212808-9 2004 We suggest that some phthalates effectively inhibit the calcium signaling of human nAChR, and these nongenomic effects are cause for concern. Calcium 56-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 15322260-6 2004 The effects of bupropion and enantiomers of hydroxybupropion on human nAChR subtypes indicate that the (2S,3S) isomer is more potent than the (2S,3R) isomer or racemic bupropion as an antagonist of alpha(4)beta(2) (functional IC(50) = 3.3 microM). Bupropion 15-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 15322260-6 2004 The effects of bupropion and enantiomers of hydroxybupropion on human nAChR subtypes indicate that the (2S,3S) isomer is more potent than the (2S,3R) isomer or racemic bupropion as an antagonist of alpha(4)beta(2) (functional IC(50) = 3.3 microM). hydroxybupropion 44-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 15322260-6 2004 The effects of bupropion and enantiomers of hydroxybupropion on human nAChR subtypes indicate that the (2S,3S) isomer is more potent than the (2S,3R) isomer or racemic bupropion as an antagonist of alpha(4)beta(2) (functional IC(50) = 3.3 microM). Saccharin 103-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 15322260-6 2004 The effects of bupropion and enantiomers of hydroxybupropion on human nAChR subtypes indicate that the (2S,3S) isomer is more potent than the (2S,3R) isomer or racemic bupropion as an antagonist of alpha(4)beta(2) (functional IC(50) = 3.3 microM). Bupropion 51-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 15203153-3 2004 We have prepared and evaluated a number of simpler analogues of the norditerpeniod alkaloid methyllycaconitine (MLA) in an effort to understand molecular determinants of nAChR*small molecule interactions. methyllycaconitine 92-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 15050621-1 2004 Epibatidine is a potent but nonselective nAChR agonist. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 15154117-5 2004 Univariate (single-marker) family-based association tests (FBATs) demonstrated that variant alleles at two SNPs, rs1044396 and rs1044397, in exon 5 of the CHRNA4 gene were significantly associated with a protective effect against nicotine addiction as either a dichotomized trait or a quantitative phenotype (i.e., age-adjusted FTND and RTQ scores), which was consistent with the results of the global haplotype FBAT. Nicotine 230-238 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-161 15154117-6 2004 Furthermore, the haplotype-specific FBAT showed a common (22.5%) CHRNA4 haplotype, GCTATA, which was significantly associated with both a protective effect against nicotine addiction as a dichotomized trait (Z=-3.04, P<.005) and significant decreases of age-adjusted FTND (Z=-3.31, P<.005) or RTQ scores (Z=-2.73, P=.006). Nicotine 164-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-71 15154117-7 2004 Our findings provide strong evidence suggesting a common CHRNA4 haplotype might be protective against vulnerability to nicotine addiction in men. Nicotine 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-63 15240454-6 2004 We have also obtained explanations for the complex mechanisms underlying inhibition of nAChR by philanthotoxins (PhTXs). philanthotoxins 96-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 15240454-6 2004 We have also obtained explanations for the complex mechanisms underlying inhibition of nAChR by philanthotoxins (PhTXs). phtxs 113-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 15240454-7 2004 PhTX-343, containing a spermine moiety with a charge of +3, binds deep in the pore near the Serine ring where classical open channel blockers of nAChR bind. phtx 0-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 15240454-7 2004 PhTX-343, containing a spermine moiety with a charge of +3, binds deep in the pore near the Serine ring where classical open channel blockers of nAChR bind. Spermine 23-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 15240454-7 2004 PhTX-343, containing a spermine moiety with a charge of +3, binds deep in the pore near the Serine ring where classical open channel blockers of nAChR bind. Serine 92-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 15359928-1 2004 Recently, 5-[123I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([123I]5IA) was developed as a ligand for imaging the nicotinic acetylcholine receptor (nAChR) in human brain using single photon emission computed tomography (SPECT). 5-[123i]iodo-3-(2(s)-azetidinylmethoxy)pyridine 10-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-144 15359928-1 2004 Recently, 5-[123I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([123I]5IA) was developed as a ligand for imaging the nicotinic acetylcholine receptor (nAChR) in human brain using single photon emission computed tomography (SPECT). 5-[123i]iodo-3-(2(s)-azetidinylmethoxy)pyridine 10-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 15359928-1 2004 Recently, 5-[123I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([123I]5IA) was developed as a ligand for imaging the nicotinic acetylcholine receptor (nAChR) in human brain using single photon emission computed tomography (SPECT). [123i]5ia 59-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-144 15359928-1 2004 Recently, 5-[123I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([123I]5IA) was developed as a ligand for imaging the nicotinic acetylcholine receptor (nAChR) in human brain using single photon emission computed tomography (SPECT). [123i]5ia 59-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 15248455-1 2004 A series of hitherto unknown enantiopure (-)-ferruginine analogues of type 8 and 9 was prepared and tested for the affinity toward the nicotinic acetylcholine receptor (nAChR) subtypes (alpha4)2(beta2)3, alpha7*, alpha3beta4*, and (alpha1)2beta1gamma delta. ferruginine 41-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 14764638-4 2004 Using immunohistochemistry and RT-PCR, we have demonstrated in lung bronchial epithelial cells (BECs) expression of choline acetyltransferase, the vesicular ACh transporter, the choline high-affinity transporter, alpha7, alpha4, and beta2 nicotinic ACh receptor (nAChR) subunits, and the nAChR accessory protein lynx1. Choline 116-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 263-268 14764638-4 2004 Using immunohistochemistry and RT-PCR, we have demonstrated in lung bronchial epithelial cells (BECs) expression of choline acetyltransferase, the vesicular ACh transporter, the choline high-affinity transporter, alpha7, alpha4, and beta2 nicotinic ACh receptor (nAChR) subunits, and the nAChR accessory protein lynx1. Choline 116-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 288-293 14761946-0 2004 Identification of binding sites in the nicotinic acetylcholine receptor for [3H]azietomidate, a photoactivatable general anesthetic. CHEMBL23812 76-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-71 14761946-1 2004 To identify binding domains in a ligand-gated ion channel for etomidate, an intravenous general anesthetic, we photolabeled nicotinic acetylcholine receptor (nAChR)-rich membranes from Torpedo electric organ with a photoactivatable analog, [(3)H]azietomidate. Etomidate 62-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-156 14761946-4 2004 UV irradiation resulted in preferential [(3)H]azietomidate photoincorporation into the nAChR alpha and delta subunits. azietomidate 46-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 14761946-6 2004 Within the nAChR ion channel in the desensitized state, there was labeling of alphaGlu-262 and deltaGln-276 at the extracellular end and deltaSer-258 and deltaSer-262 toward the cytoplasmic end. alphaglu 78-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 14761946-6 2004 Within the nAChR ion channel in the desensitized state, there was labeling of alphaGlu-262 and deltaGln-276 at the extracellular end and deltaSer-258 and deltaSer-262 toward the cytoplasmic end. deltagln 95-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 14761946-6 2004 Within the nAChR ion channel in the desensitized state, there was labeling of alphaGlu-262 and deltaGln-276 at the extracellular end and deltaSer-258 and deltaSer-262 toward the cytoplasmic end. deltaser 137-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 14761946-6 2004 Within the nAChR ion channel in the desensitized state, there was labeling of alphaGlu-262 and deltaGln-276 at the extracellular end and deltaSer-258 and deltaSer-262 toward the cytoplasmic end. deltaser 154-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 14761946-9 2004 The state dependence and subunit selectivity of [(3)H]azietomidate photolabeling are discussed in terms of the structures of the nAChR transmembrane and extracellular domains. [(3)h]azietomidate 48-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 15227641-6 2004 These docking experiments show that ImI and PnIB bind to the ACh binding pocket via a small cavity located above the beta9/beta10 hairpin of the (+)alpha7 nAChR subunit. pnib 44-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 15227641-6 2004 These docking experiments show that ImI and PnIB bind to the ACh binding pocket via a small cavity located above the beta9/beta10 hairpin of the (+)alpha7 nAChR subunit. Acetylcholine 61-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 15228589-4 2004 First, it modulates acutely the effect of acetylcholine (ACh) on Xenopus oocytes transfected with human alpha7, but not alpha4/beta2, nAChR. Acetylcholine 57-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-139 15228589-8 2004 Thirdly, in organotypic cultures of rat hippocampus, long-term exposure to peptide attenuates neurite outgrowth: this chronic, functional effect is selectively blocked by the alpha7 nAChR antagonists, alpha-BgTx and methyllycaconitine, but not by the alpha4/beta2-preferring blocker dihydro-beta-ethroidine. methyllycaconitine 216-234 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 15099589-2 2004 Using a modified patch-clamp technique in combination with an ultrafast system for solution exchange we investigated the functional interaction of gentamicin, penicillin G, tetracycline, erythromycin and ceftriaxone with nAChR transiently transfected into HEK293 cells as a potential molecular target. Gentamicins 147-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-226 15099589-2 2004 Using a modified patch-clamp technique in combination with an ultrafast system for solution exchange we investigated the functional interaction of gentamicin, penicillin G, tetracycline, erythromycin and ceftriaxone with nAChR transiently transfected into HEK293 cells as a potential molecular target. Penicillin G 159-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-226 15099589-2 2004 Using a modified patch-clamp technique in combination with an ultrafast system for solution exchange we investigated the functional interaction of gentamicin, penicillin G, tetracycline, erythromycin and ceftriaxone with nAChR transiently transfected into HEK293 cells as a potential molecular target. Tetracycline 173-185 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-226 15099589-2 2004 Using a modified patch-clamp technique in combination with an ultrafast system for solution exchange we investigated the functional interaction of gentamicin, penicillin G, tetracycline, erythromycin and ceftriaxone with nAChR transiently transfected into HEK293 cells as a potential molecular target. Erythromycin 187-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-226 15099589-2 2004 Using a modified patch-clamp technique in combination with an ultrafast system for solution exchange we investigated the functional interaction of gentamicin, penicillin G, tetracycline, erythromycin and ceftriaxone with nAChR transiently transfected into HEK293 cells as a potential molecular target. Ceftriaxone 204-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 221-226 15099589-3 2004 Gentamicin, penicillin G, tetracycline and erythromycin induced a combination of open channel and competitive block of nAChR channel currents whereas ceftriaxone had no effect. Gentamicins 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 15099589-3 2004 Gentamicin, penicillin G, tetracycline and erythromycin induced a combination of open channel and competitive block of nAChR channel currents whereas ceftriaxone had no effect. Penicillin G 12-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 15099589-3 2004 Gentamicin, penicillin G, tetracycline and erythromycin induced a combination of open channel and competitive block of nAChR channel currents whereas ceftriaxone had no effect. Tetracycline 26-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 15099589-3 2004 Gentamicin, penicillin G, tetracycline and erythromycin induced a combination of open channel and competitive block of nAChR channel currents whereas ceftriaxone had no effect. Erythromycin 43-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 15070329-1 2004 A concise synthesis of the potent nAChR agonist (+)-anatoxin-a (1) has been completed in a series of only nine chemical operations and 27% overall yield from commercially available D-methyl pyroglutamate (4). anatoxin a 48-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 14752108-0 2004 Phosphatidic acid and phosphatidylserine have distinct structural and functional interactions with the nicotinic acetylcholine receptor. Phosphatidic Acids 0-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 14752108-0 2004 Phosphatidic acid and phosphatidylserine have distinct structural and functional interactions with the nicotinic acetylcholine receptor. Phosphatidylserines 22-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidylcholines 20-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-168 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidylcholines 20-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidylcholines 41-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-168 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidylcholines 41-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidic Acids 67-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-168 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidic Acids 67-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidic Acids 86-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-168 14752108-1 2004 Bilayers containing phosphatidylcholine (PC) and the anionic lipid phosphatidic acid (PA) are particularly effective at stabilizing the nicotinic acetylcholine receptor (nAChR) in a functional conformation that undergoes agonist-induced conformational change. Phosphatidic Acids 86-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 14752108-2 2004 The physical properties of PC membranes containing PA are also substantially altered upon incorporation of the nAChR. Phosphatidylcholines 27-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 14752108-2 2004 The physical properties of PC membranes containing PA are also substantially altered upon incorporation of the nAChR. Phosphatidic Acids 51-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 14752108-6 2004 These results show that a net negative charge alone is not sufficient to account for the unique interactions that occur between the nAChR and PC/PA membranes. Phosphatidylcholines 142-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 14752108-8 2004 The results show that the nAChR has complex and unique interactions with both PA and PS. Phosphatidic Acids 78-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14752108-8 2004 The results show that the nAChR has complex and unique interactions with both PA and PS. Phosphatidylserines 85-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14752108-9 2004 The interactions between the nAChR and PS may be bridged by divalent cations, such as calcium. Phosphatidylserines 39-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 14752108-9 2004 The interactions between the nAChR and PS may be bridged by divalent cations, such as calcium. Calcium 86-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 15070329-1 2004 A concise synthesis of the potent nAChR agonist (+)-anatoxin-a (1) has been completed in a series of only nine chemical operations and 27% overall yield from commercially available D-methyl pyroglutamate (4). d-methyl pyroglutamate 181-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 15102504-6 2004 Gold conjugation does not significantly decrease binding affinity, and gold alphaBgt specifically labels alpha7* nAChR in both unfixed and aldehyde-fixed tissue at the light and electron microscope levels, labelling being abolished in the presence of excess competing toxin. Aldehydes 139-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-118 14717603-0 2004 Mechanism-based approach to the successful prevention of cocaine inhibition of the neuronal (alpha 3 beta 4) nicotinic acetylcholine receptor. Cocaine 57-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-141 14717603-2 2004 A minimum mechanism of inhibition of the muscle-type nAChR (1) by the noncompetitive inhibitors cocaine and MK-801 [(+)-dizocilpine, an anticonvulsant] indicated they bind to a regulatory site, with higher affinity for the closed-channel form than for the open-channel form, thus shifting the equilibrium toward the closed-channel form and inhibiting receptor function. Cocaine 96-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 14717603-2 2004 A minimum mechanism of inhibition of the muscle-type nAChR (1) by the noncompetitive inhibitors cocaine and MK-801 [(+)-dizocilpine, an anticonvulsant] indicated they bind to a regulatory site, with higher affinity for the closed-channel form than for the open-channel form, thus shifting the equilibrium toward the closed-channel form and inhibiting receptor function. Dizocilpine Maleate 108-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 14717603-2 2004 A minimum mechanism of inhibition of the muscle-type nAChR (1) by the noncompetitive inhibitors cocaine and MK-801 [(+)-dizocilpine, an anticonvulsant] indicated they bind to a regulatory site, with higher affinity for the closed-channel form than for the open-channel form, thus shifting the equilibrium toward the closed-channel form and inhibiting receptor function. Dizocilpine Maleate 116-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 14717603-5 2004 The mechanism of inhibition of the neuronal nAChR by cocaine and MK-801 using rapid chemical kinetic techniques was investigated. Cocaine 53-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 14717603-5 2004 The mechanism of inhibition of the neuronal nAChR by cocaine and MK-801 using rapid chemical kinetic techniques was investigated. Dizocilpine Maleate 65-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 13680077-3 2004 OBJECTIVE: In these experiments, we investigated whether acute nicotine would influence responding with conditioned reinforcement and the degree to which pretreatment with the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine would modify any nicotine-induced behavioral effects. Mecamylamine 228-240 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 176-208 14715938-5 2004 As evident in the presence of atropine, the non-muscarinic component was mimicked by epibatidine, a nonselective nicotinic ACh receptor (nAChR) agonist and was blocked by dihydro-beta-erythroidine, a nonselective nAChR antagonist. epibatidine 85-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-135 14715938-5 2004 As evident in the presence of atropine, the non-muscarinic component was mimicked by epibatidine, a nonselective nicotinic ACh receptor (nAChR) agonist and was blocked by dihydro-beta-erythroidine, a nonselective nAChR antagonist. epibatidine 85-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 14715938-5 2004 As evident in the presence of atropine, the non-muscarinic component was mimicked by epibatidine, a nonselective nicotinic ACh receptor (nAChR) agonist and was blocked by dihydro-beta-erythroidine, a nonselective nAChR antagonist. epibatidine 85-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 14715938-5 2004 As evident in the presence of atropine, the non-muscarinic component was mimicked by epibatidine, a nonselective nicotinic ACh receptor (nAChR) agonist and was blocked by dihydro-beta-erythroidine, a nonselective nAChR antagonist. Dihydro-beta-Erythroidine 171-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 14715938-5 2004 As evident in the presence of atropine, the non-muscarinic component was mimicked by epibatidine, a nonselective nicotinic ACh receptor (nAChR) agonist and was blocked by dihydro-beta-erythroidine, a nonselective nAChR antagonist. Dihydro-beta-Erythroidine 171-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 5-(2-azetidinylmethoxy)-2-chloropyridine 50-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 63-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. epibatidine 93-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 14983978-4 2004 This review describes the nAChR agonists A-85380, tebanicline, ABT-366833, ABT-202, ABT-894, epibatidine analogs and SIB-1663, of which ABT-366833, ABT-202 and ABT-894 are currently undergoing development as pain therapeutics. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 75-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 15019421-4 2004 Accumulating evidence from electrophysiological, pharmacological and neurochemical studies suggest that ethanol may interact with the nicotinic acetylcholine receptor (nAChR). Ethanol 104-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-166 15019421-4 2004 Accumulating evidence from electrophysiological, pharmacological and neurochemical studies suggest that ethanol may interact with the nicotinic acetylcholine receptor (nAChR). Ethanol 104-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 15019421-7 2004 Studies aimed at defining the nAChR subpopulation(s) involved in mediating ethanol-induced locomotor stimulation and accumbal dopamine overflow as well as ethanol-intake have revealed that alpha(3)beta(2) or alpha(6) (using alpha-Conotoxin MII) but not alpha(4)beta(2) (using dihydro-beta-erythroidine) or alpha(7) (using methyllycaconitine), could represent targets for developing new drugs in the treatment of alcoholism. Ethanol 75-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 15019421-7 2004 Studies aimed at defining the nAChR subpopulation(s) involved in mediating ethanol-induced locomotor stimulation and accumbal dopamine overflow as well as ethanol-intake have revealed that alpha(3)beta(2) or alpha(6) (using alpha-Conotoxin MII) but not alpha(4)beta(2) (using dihydro-beta-erythroidine) or alpha(7) (using methyllycaconitine), could represent targets for developing new drugs in the treatment of alcoholism. Dihydro-beta-Erythroidine 276-301 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 15019421-7 2004 Studies aimed at defining the nAChR subpopulation(s) involved in mediating ethanol-induced locomotor stimulation and accumbal dopamine overflow as well as ethanol-intake have revealed that alpha(3)beta(2) or alpha(6) (using alpha-Conotoxin MII) but not alpha(4)beta(2) (using dihydro-beta-erythroidine) or alpha(7) (using methyllycaconitine), could represent targets for developing new drugs in the treatment of alcoholism. methyllycaconitine 322-340 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 14754452-9 2004 Undesirable side effects of nicotine are well known, but as we will discuss in detail, these effects are not produced by all neuronal nAChR agonists and the existence of neuronal nAChR subtypes may provide a basis for separating therapeutic effects from toxicities. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 14965298-1 2004 The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-124 14965298-1 2004 The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. Nicotine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 14965298-1 2004 The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. epibatidine 47-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-124 14965298-1 2004 The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. epibatidine 47-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 14965300-2 2004 Recently, we constructed three-dimensional models of the N-terminal part of nAChR and docked in the putative ligand-binding pocket, different agonists (acetylcholine, nicotine and epibatidine) and antagonist (snake alpha-bungarotoxin). Acetylcholine 152-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 14965300-2 2004 Recently, we constructed three-dimensional models of the N-terminal part of nAChR and docked in the putative ligand-binding pocket, different agonists (acetylcholine, nicotine and epibatidine) and antagonist (snake alpha-bungarotoxin). Nicotine 167-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 14965300-2 2004 Recently, we constructed three-dimensional models of the N-terminal part of nAChR and docked in the putative ligand-binding pocket, different agonists (acetylcholine, nicotine and epibatidine) and antagonist (snake alpha-bungarotoxin). epibatidine 180-191 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 13680077-3 2004 OBJECTIVE: In these experiments, we investigated whether acute nicotine would influence responding with conditioned reinforcement and the degree to which pretreatment with the nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine would modify any nicotine-induced behavioral effects. Mecamylamine 228-240 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 210-215 14636070-5 2003 Interestingly, we found that both the overall and the water-accessible nAChR secondary structures were nearly identical to those of 5-HT(3)R, in agreement with predicted structures of this class of receptors. Water 54-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 14596621-1 2003 Structure and backbone dynamics of a selectively [(15)N]Leu-labeled 28-residue segment of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit were studied by (1)H and (15)N solution-state NMR in dodecylphosphocholine micelles. 15)n 51-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 14645658-1 2003 Naturally expressed nicotinic acetylcholine receptors composed of alpha4 and beta2 subunits (alpha4beta2-nAChR) are the predominant form of high affinity nicotine binding site in the brain implicated in nicotine reward, mediation of nicotinic cholinergic transmission, modulation of signaling through other chemical messages, and a number of neuropsychiatric disorders. Nicotine 203-211 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 14645658-3 2003 Heterologously expressed alpha4beta2-nAChR engage in high-affinity, specific binding of 3H-labeled epibatidine (H-EBDN; macroscopic KD = 10 pM; kon = 0.74/min/nM, koff = 0.013/min). Tritium 88-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 14645658-3 2003 Heterologously expressed alpha4beta2-nAChR engage in high-affinity, specific binding of 3H-labeled epibatidine (H-EBDN; macroscopic KD = 10 pM; kon = 0.74/min/nM, koff = 0.013/min). epibatidine 99-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 14645658-3 2003 Heterologously expressed alpha4beta2-nAChR engage in high-affinity, specific binding of 3H-labeled epibatidine (H-EBDN; macroscopic KD = 10 pM; kon = 0.74/min/nM, koff = 0.013/min). h-ebdn 112-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 14621991-0 2003 Identification of nicotinic acetylcholine receptor amino acids photolabeled by the volatile anesthetic halothane. Halothane 103-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-50 14621991-1 2003 To identify inhalational anesthetic binding domains in a ligand-gated ion channel, we photolabeled nicotinic acetylcholine receptor (nAChR)-rich membranes from Torpedo electric organ with [(14)C]halothane and determined by Edman degradation some of the photolabeled amino acids in nAChR subunit fragments isolated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and high-performance liquid chromatography. Halothane 195-204 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-131 14621991-2 2003 Irradiation at 254 nm for 60 s in the presence of 1 mM [(14)C]halothane resulted in incorporation of approximately 0.5 mol of (14)C/mol of subunit, with photolabeling distributed within the nAChR extracellular and transmembrane domains, primarily at tyrosines. [(14)c]halothane 55-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 190-195 14621991-8 2003 Within the structure of the nAChR transmembrane domain, deltaTyr-228 projects into an extracellular, water accessible pocket formed by amino acids from the deltaM1-deltaM3 alpha-helices. Water 101-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 14621991-9 2003 Halothane photolabeling of deltaTyr-228 provides initial evidence that halothane and isoflurane bind within this pocket with occupancy or access increased in the nAChR desensitized state compared to the closed channel state. Halothane 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 14621991-9 2003 Halothane photolabeling of deltaTyr-228 provides initial evidence that halothane and isoflurane bind within this pocket with occupancy or access increased in the nAChR desensitized state compared to the closed channel state. deltatyr 27-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 14621991-9 2003 Halothane photolabeling of deltaTyr-228 provides initial evidence that halothane and isoflurane bind within this pocket with occupancy or access increased in the nAChR desensitized state compared to the closed channel state. Halothane 71-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 14621991-9 2003 Halothane photolabeling of deltaTyr-228 provides initial evidence that halothane and isoflurane bind within this pocket with occupancy or access increased in the nAChR desensitized state compared to the closed channel state. Isoflurane 85-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 14523584-1 2003 The purpose of this study was to assess the utility of a new single-photon emission tomography ligand, [123I]5-iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-I-A-85380), to measure regional nAChR binding in human brain. 5-iodo-3-(2-azetidinylmethoxy)pyridine 103-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 14523584-1 2003 The purpose of this study was to assess the utility of a new single-photon emission tomography ligand, [123I]5-iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-I-A-85380), to measure regional nAChR binding in human brain. 5-i-a 154-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-193 14645658-1 2003 Naturally expressed nicotinic acetylcholine receptors composed of alpha4 and beta2 subunits (alpha4beta2-nAChR) are the predominant form of high affinity nicotine binding site in the brain implicated in nicotine reward, mediation of nicotinic cholinergic transmission, modulation of signaling through other chemical messages, and a number of neuropsychiatric disorders. Nicotine 154-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 14630163-0 2003 Enantioselective interactions of dextromethorphan and levomethorphan with the alpha 3 beta 4-nicotinic acetylcholine receptor: comparison of chromatographic and functional data. Dextromethorphan 33-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-125 14630163-0 2003 Enantioselective interactions of dextromethorphan and levomethorphan with the alpha 3 beta 4-nicotinic acetylcholine receptor: comparison of chromatographic and functional data. Dextromethorphan 54-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-125 14596621-1 2003 Structure and backbone dynamics of a selectively [(15)N]Leu-labeled 28-residue segment of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit were studied by (1)H and (15)N solution-state NMR in dodecylphosphocholine micelles. 15)n 51-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 14596621-1 2003 Structure and backbone dynamics of a selectively [(15)N]Leu-labeled 28-residue segment of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit were studied by (1)H and (15)N solution-state NMR in dodecylphosphocholine micelles. Leucine 56-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 14596621-1 2003 Structure and backbone dynamics of a selectively [(15)N]Leu-labeled 28-residue segment of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit were studied by (1)H and (15)N solution-state NMR in dodecylphosphocholine micelles. Leucine 56-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 14596621-1 2003 Structure and backbone dynamics of a selectively [(15)N]Leu-labeled 28-residue segment of the extended second transmembrane domain (TM2e) of the human neuronal nicotinic acetylcholine receptor (nAChR) beta(2) subunit were studied by (1)H and (15)N solution-state NMR in dodecylphosphocholine micelles. dodecylphosphocholine 270-291 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 14500743-3 2003 In this study, 12 homologous analogs of DMCC and its corresponding tertiary amine, N,N-dimethylcarbamoyl-N,N-dimethylaminoethanol, were synthesized and their binding affinities to native mAChR and nAChR sites estimated. dimethylcarbamylcholine 40-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 14573772-0 2003 The allosteric potentiation of nicotinic acetylcholine receptors by galantamine is transduced into cellular responses in neurons: Ca2+ signals and neurotransmitter release. Galantamine 68-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-64 14573772-4 2003 The aim of this study was to establish whether the allosteric potentiation of nAChR currents is transduced in downstream cellular responses to nAChR activation, namely increases in intracellular Ca2+ and [3H]noradrenaline release. Tritium 205-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 14573772-4 2003 The aim of this study was to establish whether the allosteric potentiation of nAChR currents is transduced in downstream cellular responses to nAChR activation, namely increases in intracellular Ca2+ and [3H]noradrenaline release. Tritium 205-207 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 14573772-4 2003 The aim of this study was to establish whether the allosteric potentiation of nAChR currents is transduced in downstream cellular responses to nAChR activation, namely increases in intracellular Ca2+ and [3H]noradrenaline release. Norepinephrine 208-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 14573772-4 2003 The aim of this study was to establish whether the allosteric potentiation of nAChR currents is transduced in downstream cellular responses to nAChR activation, namely increases in intracellular Ca2+ and [3H]noradrenaline release. Norepinephrine 208-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 14573772-9 2003 nAChR-mediated [3H]noradrenaline release from hippocampal slices was also potentiated by galantamine, with an additional component attributable to acetylcholinesterase inhibition and subsequent increase in acetylcholine. Tritium 16-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 14573772-9 2003 nAChR-mediated [3H]noradrenaline release from hippocampal slices was also potentiated by galantamine, with an additional component attributable to acetylcholinesterase inhibition and subsequent increase in acetylcholine. Norepinephrine 19-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 14573772-9 2003 nAChR-mediated [3H]noradrenaline release from hippocampal slices was also potentiated by galantamine, with an additional component attributable to acetylcholinesterase inhibition and subsequent increase in acetylcholine. Galantamine 89-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 14573772-9 2003 nAChR-mediated [3H]noradrenaline release from hippocampal slices was also potentiated by galantamine, with an additional component attributable to acetylcholinesterase inhibition and subsequent increase in acetylcholine. Acetylcholine 147-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 14500752-0 2003 Contrasting actions of philanthotoxin-343 and philanthotoxin-(12) on human muscle nicotinic acetylcholine receptors. Philanthotoxin 46-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-115 14500752-1 2003 Whole-cell recordings and outside-out patch recordings from TE671 cells were made to investigate antagonism of human muscle nicotinic acetylcholine receptors (nAChR) by the philanthotoxins, PhTX-343 and PhTX-(12). philanthotoxins 173-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-157 14500743-3 2003 In this study, 12 homologous analogs of DMCC and its corresponding tertiary amine, N,N-dimethylcarbamoyl-N,N-dimethylaminoethanol, were synthesized and their binding affinities to native mAChR and nAChR sites estimated. n,n-dimethylcarbamoyl-n,n-dimethylaminoethanol 83-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 14500752-1 2003 Whole-cell recordings and outside-out patch recordings from TE671 cells were made to investigate antagonism of human muscle nicotinic acetylcholine receptors (nAChR) by the philanthotoxins, PhTX-343 and PhTX-(12). philanthotoxins 173-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 14500752-8 2003 The different voltage-dependencies of the two modes of action of these philanthotoxins suggest two binding sites, one deep in the nAChR pore, the other near the extracellular entrance to the pore. philanthotoxins 71-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 12920198-1 2003 Nicotinic acetylcholine receptor (nAChR) activation is well known to stimulate dopamine release in the striatum. Dopamine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 14579511-6 2003 Sterols and steroids, in particular, are among the ligands that act on this functionally relevant moiety of the nAChR. Sterols 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 14579511-6 2003 Sterols and steroids, in particular, are among the ligands that act on this functionally relevant moiety of the nAChR. Steroids 12-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 12920198-1 2003 Nicotinic acetylcholine receptor (nAChR) activation is well known to stimulate dopamine release in the striatum. Dopamine 79-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 12920198-4 2003 Because the dopamine precursor l-DOPA is the most commonly used therapeutic agent for Parkinson"s disease, we investigated the effects of l-DOPA treatment on striatal nAChR expression in unlesioned and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned monkeys. Levodopa 138-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 12920198-9 2003 In summary, these data show that l-DOPA treatment decreases nAChR expression, in contrast with the well established up-regulation of these sites by chronic nicotine exposure. Levodopa 33-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-65 12755612-0 2003 Reversing the action of noncompetitive inhibitors (MK-801 and cocaine) on a protein (nicotinic acetylcholine receptor)-mediated reaction. Dizocilpine Maleate 51-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-117 12721323-0 2003 The subtype-selective nicotinic acetylcholine receptor agonist SIB-1553A improves both attention and memory components of a spatial working memory task in chronic low dose 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated monkeys. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 172-216 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-54 12649296-1 2003 Galantamine (Reminyl), an approved treatment for Alzheimer"s disease (AD), is a potent allosteric potentiating ligand (APL) of human alpha 3 beta 4, alpha 4 beta 2, and alpha 6 beta 4 nicotinic receptors (nAChRs), and of the chicken/mouse chimeric alpha 7/5-hydroxytryptamine3 receptor, as was shown by whole-cell patch-clamp studies of human embryonic kidney-293 cells stably expressing a single nAChR subtype. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 12649296-2 2003 Galantamine potentiates agonist responses of the four nAChR subtypes studied in the same window of concentrations (i.e., 0.1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg. At concentrations >10 microM, galantamine acts as an nAChR inhibitor. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 12649296-2 2003 Galantamine potentiates agonist responses of the four nAChR subtypes studied in the same window of concentrations (i.e., 0.1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg. At concentrations >10 microM, galantamine acts as an nAChR inhibitor. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 312-317 12649296-3 2003 The other presently approved AD drugs, donepezil and rivastigmine, are devoid of the nicotinic APL action; at micromolar concentrations they also block nAChR activity. Donepezil 39-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 12649296-3 2003 The other presently approved AD drugs, donepezil and rivastigmine, are devoid of the nicotinic APL action; at micromolar concentrations they also block nAChR activity. Rivastigmine 53-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 12755612-0 2003 Reversing the action of noncompetitive inhibitors (MK-801 and cocaine) on a protein (nicotinic acetylcholine receptor)-mediated reaction. Cocaine 62-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-117 12779043-4 2003 Despite obvious structural similarities with the potent alkaloids pinnamine (5) and (-)-ferruginine (4) the pyranotropanes 6a and 6c exhibited distinctly lower nAChR affinities. ferruginine 84-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 12747776-8 2003 Hence, physicochemical determinants of binding, such as steric and electrostatic and, for the first time, hydrophobic, hydrogen bond donor, and hydrogen bond acceptor properties, were mapped back onto the molecular structures of a set of nAChR modulators. Hydrogen 119-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 238-243 12588870-2 2003 Up-regulation, an increase in numbers of radioligand-binding nicotinic acetylcholine receptors (nAChR), occurs on exposure to nicotine at high concentrations. Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 12588870-6 2003 Further, the general nAChR antagonist, d-tubocurarine, blocked all but two of the observed changes in gene expression, indicating that these changes are dependent on nAChR activation. Tubocurarine 39-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 12588870-6 2003 Further, the general nAChR antagonist, d-tubocurarine, blocked all but two of the observed changes in gene expression, indicating that these changes are dependent on nAChR activation. Tubocurarine 39-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 12694384-2 2003 In this study, we determined effects of lowered temperature or of exposure to the protein synthesis inhibitor cycloheximide (CHX) on cell surface expression of homomeric alpha7-nAChR in transfected SH-EP1 human epithelial cells. Cycloheximide 110-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 12694384-2 2003 In this study, we determined effects of lowered temperature or of exposure to the protein synthesis inhibitor cycloheximide (CHX) on cell surface expression of homomeric alpha7-nAChR in transfected SH-EP1 human epithelial cells. Cycloheximide 125-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 12779043-4 2003 Despite obvious structural similarities with the potent alkaloids pinnamine (5) and (-)-ferruginine (4) the pyranotropanes 6a and 6c exhibited distinctly lower nAChR affinities. pyranotropanes 108-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 12549904-0 2003 Mutational analysis of roles for extracellular cysteine residues in the assembly and function of human alpha 7-nicotinic acetylcholine receptors. Cysteine 47-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-144 12606407-2 2003 Recently, we reported the results of antagonist studies suggesting that a nicotinic acetylcholine receptor (nAChR) containing an alpha7 subunit (alpha7nAChR) plays a role in the human sperm AR initiated by recombinant human ZP3 or by acetylcholine (ACh). Acetylcholine 84-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 12606407-2 2003 Recently, we reported the results of antagonist studies suggesting that a nicotinic acetylcholine receptor (nAChR) containing an alpha7 subunit (alpha7nAChR) plays a role in the human sperm AR initiated by recombinant human ZP3 or by acetylcholine (ACh). Acetylcholine 109-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-106 12628470-3 2003 Epithelial cell adhesion is under control of the local cytotransmitter acetylcholine (ACh) working through the muscarinic and nicotinic receptor, mAChR and nAChR, classes expressed by epithelial cells. Acetylcholine 71-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 12628470-3 2003 Epithelial cell adhesion is under control of the local cytotransmitter acetylcholine (ACh) working through the muscarinic and nicotinic receptor, mAChR and nAChR, classes expressed by epithelial cells. Acetylcholine 86-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 12628473-4 2003 In addition, we examined the long-term effect of nicotine on the expression of selected nAChR subunits using semiquantitative reverse transcription-polymerase chain reaction analysis. Nicotine 49-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 12628473-6 2003 This effect was concentration-dependently inhibited by the alpha7 nAChR subunit antagonists, alpha-bungarotoxin (0.01-10 microM) and methyllycaconitine (0.01-10 mM), suggesting that the alpha7 nAChR subunit mediates Ca(2+) signaling in T-lymphocytes. methyllycaconitine 133-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 12628473-6 2003 This effect was concentration-dependently inhibited by the alpha7 nAChR subunit antagonists, alpha-bungarotoxin (0.01-10 microM) and methyllycaconitine (0.01-10 mM), suggesting that the alpha7 nAChR subunit mediates Ca(2+) signaling in T-lymphocytes. methyllycaconitine 133-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 12628473-7 2003 Nicotine (0.01-10 microM) also concentration-dependently down-regulated expression of mRNAs for all the nAChR subunits tested: expression of the alpha6 and alpha7 subunits was down-regulated within 1 week, while expression of the alpha3 and alpha5 subunits declined gradually throughout the 8-week experimental period. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 12628473-8 2003 These findings indicate that nicotine--and therefore likely smoking--affects immune function by suppressing expression of the neuronal nAChR subtype involved in Ca(2+) signaling in lymphocytes. Nicotine 29-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 12620422-3 2003 The possibility that subtype-selective ligands be used in the treatment of CNS disorders promoted the synthesis of a large number of structural analogues of nicotine and epibatidine, two very potent nAChR agonists. Nicotine 157-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 12620422-3 2003 The possibility that subtype-selective ligands be used in the treatment of CNS disorders promoted the synthesis of a large number of structural analogues of nicotine and epibatidine, two very potent nAChR agonists. epibatidine 170-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-204 12620422-4 2003 Pursuing our long standing research on the structural modification of quinolizidine alkaloids, we devoted our attention to cytisine, another very potent ligand for many nAChR subtypes. cytisine 123-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 12620422-5 2003 Thus a systematic structural modification of cytisine was undertaken in order to obtain compounds of potential therapeutic interest at peripheral as well as central level, with a particular concern for achieving nAChR subtype selective ligands. cytisine 45-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 212-217 12604094-3 2003 Intrahippocampal administration of a high dose of nicotine (1 micro g, 4.3 mM) had an anxiogenic effect in the social interaction test that was reversed by co-administration of a behaviourally inactive dose (1.9 ng, 4.3 micro M) of methyllycaconitine (MLA), which is an antagonist at alpha7 and alpha3 nAChR subunits. Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 302-307 12549904-3 2003 All ionotropic glycine receptor, GABA(A) receptor, 5-HT(3) receptor, and nAChR subunits contain a pair of highly conserved cysteine residues (C150 and C164 for alpha7 subunits) in their N-terminal extracellular domain. Cysteine 123-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-78 12549904-5 2003 However, nAChR alpha7 (and alpha8) subunits also contain a third cysteine residue, C138, N-terminal to the conserved cysteine pair. Cysteine 65-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 12549904-5 2003 However, nAChR alpha7 (and alpha8) subunits also contain a third cysteine residue, C138, N-terminal to the conserved cysteine pair. Cysteine 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 12525154-0 2003 Identification of amino acids in the nicotinic acetylcholine receptor agonist binding site and ion channel photolabeled by 4-[(3-trifluoromethyl)-3H-diazirin-3-yl]benzoylcholine, a novel photoaffinity antagonist. 4-((3-trifluoromethyl)-3H-diazirin-3-yl)benzoylcholine 123-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-69 12525154-1 2003 [(3)H]4-[(3-trifluoromethyl)-3H-diazirin-3-yl]benzoylcholine (TDBzcholine) was synthesized and used as a photoaffinity probe to map the orientation of an aromatic choline ester within the agonist binding sites of the Torpedo nicotinic acetylcholine receptor (nAChR). [(3)h]4-[(3-trifluoromethyl)-3h-diazirin-3-yl]benzoylcholine 0-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-257 12525154-1 2003 [(3)H]4-[(3-trifluoromethyl)-3H-diazirin-3-yl]benzoylcholine (TDBzcholine) was synthesized and used as a photoaffinity probe to map the orientation of an aromatic choline ester within the agonist binding sites of the Torpedo nicotinic acetylcholine receptor (nAChR). [(3)h]4-[(3-trifluoromethyl)-3h-diazirin-3-yl]benzoylcholine 0-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 259-264 12525154-1 2003 [(3)H]4-[(3-trifluoromethyl)-3H-diazirin-3-yl]benzoylcholine (TDBzcholine) was synthesized and used as a photoaffinity probe to map the orientation of an aromatic choline ester within the agonist binding sites of the Torpedo nicotinic acetylcholine receptor (nAChR). 4-((3-trifluoromethyl)-3H-diazirin-3-yl)benzoylcholine 62-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-257 12525154-1 2003 [(3)H]4-[(3-trifluoromethyl)-3H-diazirin-3-yl]benzoylcholine (TDBzcholine) was synthesized and used as a photoaffinity probe to map the orientation of an aromatic choline ester within the agonist binding sites of the Torpedo nicotinic acetylcholine receptor (nAChR). 4-((3-trifluoromethyl)-3H-diazirin-3-yl)benzoylcholine 62-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 259-264 12525154-2 2003 TDBzcholine acts as a nAChR competitive antagonist that binds at equilibrium with equal affinity to both agonist sites (K(D) approximately 10 microM). 4-((3-trifluoromethyl)-3H-diazirin-3-yl)benzoylcholine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 12525154-7 2003 The photolabeling of these amino acids suggests that when the antagonist TDBzcholine occupies the agonist binding sites, the Cys-192-193 disulfide and Pro-194 from the alpha subunit Segment C are oriented toward the agonist site and are in proximity to gammaLeu-109/deltaLeu-111 in Segment E, a conclusion consistent with the structure of the binding site in the molluscan acetylcholine binding protein, a soluble protein that is homologous to the nAChR extracellular domain. 4-((3-trifluoromethyl)-3H-diazirin-3-yl)benzoylcholine 73-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 448-453 12525154-7 2003 The photolabeling of these amino acids suggests that when the antagonist TDBzcholine occupies the agonist binding sites, the Cys-192-193 disulfide and Pro-194 from the alpha subunit Segment C are oriented toward the agonist site and are in proximity to gammaLeu-109/deltaLeu-111 in Segment E, a conclusion consistent with the structure of the binding site in the molluscan acetylcholine binding protein, a soluble protein that is homologous to the nAChR extracellular domain. Cysteine 125-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 448-453 12525154-7 2003 The photolabeling of these amino acids suggests that when the antagonist TDBzcholine occupies the agonist binding sites, the Cys-192-193 disulfide and Pro-194 from the alpha subunit Segment C are oriented toward the agonist site and are in proximity to gammaLeu-109/deltaLeu-111 in Segment E, a conclusion consistent with the structure of the binding site in the molluscan acetylcholine binding protein, a soluble protein that is homologous to the nAChR extracellular domain. Disulfides 137-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 448-453 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). imidacloprid 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 12503081-2 2003 We first tested whether phorbol esters, which activate PKCs, regulate agrin-induced nAChR clustering in C(2)C(12) cells. Phorbol Esters 24-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 12503081-3 2003 We found that extended phorbol ester treatment (6 hr) increased nAChR clustering by two-fold. Phorbol Esters 23-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 12503081-9 2003 Phorbol ester treatment reduced preexisting nAChR cluster numbers in nPKC theta-GFP compared to GFP-overexpressing myotubes, suggesting that stimulating nPKC theta activity disrupts nAChR clusters in the presence of maximal clustering concentrations of agrin. Phorbol Esters 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 12503081-9 2003 Phorbol ester treatment reduced preexisting nAChR cluster numbers in nPKC theta-GFP compared to GFP-overexpressing myotubes, suggesting that stimulating nPKC theta activity disrupts nAChR clusters in the presence of maximal clustering concentrations of agrin. Phorbol Esters 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 12537063-8 2003 Moreover, our identification of nAChR subunit mRNAs in the nasal mucosa extends the findings of other functional studies of nAChRs in nasal epithelial cells and implies that nicotine from tobacco products such as cigarette smoke and nicotine nasal spray may have direct cellular effects on nasal mucosa cells through activation of homogeneous or heterogeneous nAChRs. Nicotine 174-182 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 12537063-8 2003 Moreover, our identification of nAChR subunit mRNAs in the nasal mucosa extends the findings of other functional studies of nAChRs in nasal epithelial cells and implies that nicotine from tobacco products such as cigarette smoke and nicotine nasal spray may have direct cellular effects on nasal mucosa cells through activation of homogeneous or heterogeneous nAChRs. Nicotine 233-241 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). imidacloprid 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). nitenpyram 38-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). nitenpyram 38-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). acetamiprid 50-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). acetamiprid 50-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). thiacloprid 63-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). thiacloprid 63-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). Thiamethoxam 76-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-163 12208819-2 2003 Imidacloprid (the principal example), nitenpyram, acetamiprid, thiacloprid, thiamethoxam, and others act as agonists at the insect nicotinic acetylcholine receptor (nAChR). Thiamethoxam 76-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 165-170 12208819-5 2003 Whereas ionized nicotine binds at an anionic subsite in the mammalian nAChR, the negatively tipped ("magic" nitro or cyano) neonicotinoids interact with a proposed unique subsite consisting of cationic amino acid residue(s) in the insect nAChR. Nicotine 16-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 12490593-2 2003 Magnitudes of acute, nAChR-mediated, specific 86Rb+ efflux responses to 1 mM carbamylcholine were reduced after pretreatment with specific nAChR ligands in effects that depended on pretreatment drug dose, duration of drug pretreatment, and duration of drug-free recovery. Rubidium-86 46-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 14675945-2 2003 Fundamental differences between the nicotinic acetylcholine receptors (nAChRs) of insects and mammals confer remarkable selectivity of the neonicotinoids at insect nAChR over mammalian nAChR. Neonicotinoids 139-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 14675945-2 2003 Fundamental differences between the nicotinic acetylcholine receptors (nAChRs) of insects and mammals confer remarkable selectivity of the neonicotinoids at insect nAChR over mammalian nAChR. Neonicotinoids 139-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 14675945-3 2003 To identify pharmacophoric requirements of azidopyridinyl neonicotinoids for their efficacy and selectivity towards the insect nAChR over the mammalian one, quantitative structure-activity relationship (QSAR) study was performed using electrotopological state atom (ETSA) indices. azidopyridinyl neonicotinoids 43-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 12490593-2 2003 Magnitudes of acute, nAChR-mediated, specific 86Rb+ efflux responses to 1 mM carbamylcholine were reduced after pretreatment with specific nAChR ligands in effects that depended on pretreatment drug dose, duration of drug pretreatment, and duration of drug-free recovery. Rubidium-86 46-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 12490593-2 2003 Magnitudes of acute, nAChR-mediated, specific 86Rb+ efflux responses to 1 mM carbamylcholine were reduced after pretreatment with specific nAChR ligands in effects that depended on pretreatment drug dose, duration of drug pretreatment, and duration of drug-free recovery. Carbachol 77-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 12490593-2 2003 Magnitudes of acute, nAChR-mediated, specific 86Rb+ efflux responses to 1 mM carbamylcholine were reduced after pretreatment with specific nAChR ligands in effects that depended on pretreatment drug dose, duration of drug pretreatment, and duration of drug-free recovery. Carbachol 77-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 12490593-3 2003 Fifty percent inhibition of alpha4beta2-nAChR function following 5 min of recovery occurred after 1 min of pretreatment with 1 mM nicotine but also after 1-h pretreatment at 10 nM nicotine. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 12490593-3 2003 Fifty percent inhibition of alpha4beta2-nAChR function following 5 min of recovery occurred after 1 min of pretreatment with 1 mM nicotine but also after 1-h pretreatment at 10 nM nicotine. Nicotine 180-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 12490593-6 2003 alpha4beta4-nAChR was similarly sensitive to persistent inactivation by prolonged nicotine exposure. Nicotine 82-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 14870853-2 2003 Palladium supported on charcoal (Pd/C) has been used to produce libraries of pyrazole compounds for screening in COX II studies via Suzuki cross coupling reactions, while the same catalyst has been used also to produce styryl-based nAChR compounds using analogous chemistry. Palladium 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 232-237 12559123-1 2003 Voltage-dependent, non-competitive inhibition by philanthotoxin-343 (PhTX-343) analogues, with reduced charge or length, of nicotinic acetylcholine receptors (nAChR) of TE671 cells and ionotropic glutamate receptors (N-methyl-D-aspartate receptors (NMDAR) and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPAR)) expressed in Xenopus oocytes from rat brain RNA was investigated. Philanthotoxin 49-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-157 12559123-1 2003 Voltage-dependent, non-competitive inhibition by philanthotoxin-343 (PhTX-343) analogues, with reduced charge or length, of nicotinic acetylcholine receptors (nAChR) of TE671 cells and ionotropic glutamate receptors (N-methyl-D-aspartate receptors (NMDAR) and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPAR)) expressed in Xenopus oocytes from rat brain RNA was investigated. Philanthotoxin 49-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 12559123-1 2003 Voltage-dependent, non-competitive inhibition by philanthotoxin-343 (PhTX-343) analogues, with reduced charge or length, of nicotinic acetylcholine receptors (nAChR) of TE671 cells and ionotropic glutamate receptors (N-methyl-D-aspartate receptors (NMDAR) and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPAR)) expressed in Xenopus oocytes from rat brain RNA was investigated. phtx 69-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 124-157 12559123-1 2003 Voltage-dependent, non-competitive inhibition by philanthotoxin-343 (PhTX-343) analogues, with reduced charge or length, of nicotinic acetylcholine receptors (nAChR) of TE671 cells and ionotropic glutamate receptors (N-methyl-D-aspartate receptors (NMDAR) and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPAR)) expressed in Xenopus oocytes from rat brain RNA was investigated. phtx 69-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 12559123-7 2003 These studies show that PhTX-(12) is a selective nAChR inhibitor and PhTX-83 is a selective AMPAR antagonist. phtx-( 24-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 12424289-5 2002 This study presents evidence for nicotinic acetylcholine receptor (nAChR)-mediated enhancement of GABAergic, but not of purinergic, transmission despite the co-transmission of ATP and GABA at LH synapses in vitro. Adenosine Triphosphate 176-179 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-65 12436427-8 2002 We will also present hypotheses that might address the mechanisms underlying the ability of nAChR function to protect against neurodegeneration or improve cognition, two potentially distinct actions of nicotine. Nicotine 202-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 12436413-5 2002 This type of mechanism can be extended to explain how the continuous occupation of desensitized receptors during chronic nicotine exposure contributes to drug addiction, and highlights the potential significance of prolonged nAChR desensitization that would also occur as a result of extended acetylcholine lifetime during treatment of Alzheimer"s disease with cholinesterase inhibitors. Nicotine 121-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-230 12436413-5 2002 This type of mechanism can be extended to explain how the continuous occupation of desensitized receptors during chronic nicotine exposure contributes to drug addiction, and highlights the potential significance of prolonged nAChR desensitization that would also occur as a result of extended acetylcholine lifetime during treatment of Alzheimer"s disease with cholinesterase inhibitors. Acetylcholine 293-306 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-230 12451118-6 2002 It is also apparent that nicotine-induced nAChR upregulation is very strongly dependent on subunit composition and subunit domains. Nicotine 25-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 12244045-2 2002 In this study we provide evidence that nicotine stimulation of alpha7 nAChR transduces signals to phosphatidylinositol 3-kinase and Akt via Janus kinase 2 (JAK2) in a cascade, which results in neuroprotection. Nicotine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 12244045-5 2002 We also found that pretreatment of cells with angiotensin II blocks the nicotine-induced activation of JAK2 via the AT(2) receptor and completely prevents alpha7 nAChR-mediated neuroprotective effects further suggesting a pivotal role for JAK2. Nicotine 72-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 162-167 12417371-5 2002 Galantamine is both a moderate, reversible, competitive acetylcholinesterase inhibitor, and an allosteric modulator of nAChR. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 12235129-2 2002 To ascertain whether the AChBP exhibits the recognition properties and functional states of the nAChR, we have expressed the protein in milligram quantities from a synthetic cDNA transfected into human embryonic kidney (HEK) cells. achbp 25-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 12424289-5 2002 This study presents evidence for nicotinic acetylcholine receptor (nAChR)-mediated enhancement of GABAergic, but not of purinergic, transmission despite the co-transmission of ATP and GABA at LH synapses in vitro. Adenosine Triphosphate 176-179 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 12424289-5 2002 This study presents evidence for nicotinic acetylcholine receptor (nAChR)-mediated enhancement of GABAergic, but not of purinergic, transmission despite the co-transmission of ATP and GABA at LH synapses in vitro. gamma-Aminobutyric Acid 98-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-65 12424289-5 2002 This study presents evidence for nicotinic acetylcholine receptor (nAChR)-mediated enhancement of GABAergic, but not of purinergic, transmission despite the co-transmission of ATP and GABA at LH synapses in vitro. gamma-Aminobutyric Acid 98-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 12424289-6 2002 Facilitation of GABAergic transmission by nicotine is inhibited by antagonists of (alphabeta)*-containing nAChRs, but is unaffected by an alpha7-selective antagonist, consistent with a nAChR-mediated enhancement of GABA release mediated by non-alpha7-containing nAChRs. Nicotine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 12424289-6 2002 Facilitation of GABAergic transmission by nicotine is inhibited by antagonists of (alphabeta)*-containing nAChRs, but is unaffected by an alpha7-selective antagonist, consistent with a nAChR-mediated enhancement of GABA release mediated by non-alpha7-containing nAChRs. gamma-Aminobutyric Acid 16-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 12361403-9 2002 2,3-Disubstituted epibatidine analogues possessing a 2"-amino group combined with a 3"-bromo or 3"-iodo group showed in vitro and in vivo nAChR properties similar to nicotine. 2,3-disubstituted epibatidine 0-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 12392404-0 2002 A perturbed pK(a) at the binding site of the nicotinic acetylcholine receptor: implications for nicotine binding. Nicotine 96-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-77 12392404-1 2002 A series of tethered quaternary ammonium derivatives of Tyr have been incorporated into the binding site of the nicotinic acetylcholine receptor (nAChR) using the in vivo nonsense suppression method, producing constitutively active (self-gating) receptors. quaternary ammonium 21-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-144 12392404-1 2002 A series of tethered quaternary ammonium derivatives of Tyr have been incorporated into the binding site of the nicotinic acetylcholine receptor (nAChR) using the in vivo nonsense suppression method, producing constitutively active (self-gating) receptors. quaternary ammonium 21-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 12392404-1 2002 A series of tethered quaternary ammonium derivatives of Tyr have been incorporated into the binding site of the nicotinic acetylcholine receptor (nAChR) using the in vivo nonsense suppression method, producing constitutively active (self-gating) receptors. Tyrosine 56-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-144 12392404-1 2002 A series of tethered quaternary ammonium derivatives of Tyr have been incorporated into the binding site of the nicotinic acetylcholine receptor (nAChR) using the in vivo nonsense suppression method, producing constitutively active (self-gating) receptors. Tyrosine 56-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 12392404-4 2002 Tertiary and secondary tethered amines, TyrO3T and TyrO3S, have been successfully incorporated at alpha149 in the nAChR. Amines 32-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 12392404-4 2002 Tertiary and secondary tethered amines, TyrO3T and TyrO3S, have been successfully incorporated at alpha149 in the nAChR. tyro3t 40-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 12392404-7 2002 This local pKa perturbation has substantial implications for pharmacological research on the nAChR: of the tertiary agonists considered, noracetylcholine experiences this pKa perturbation, while nicotine does not. noracetylcholine 137-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 12392404-7 2002 This local pKa perturbation has substantial implications for pharmacological research on the nAChR: of the tertiary agonists considered, noracetylcholine experiences this pKa perturbation, while nicotine does not. Nicotine 195-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 12190802-6 2002 The nAChR from these tissue specimens were solubilized and incubated with 125I-alpha-bungarotoxin. 125i-alpha-bungarotoxin 74-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 12189247-3 2002 In an in vitro angiogenesis model, increasing concentrations of the nonselective nAChR antagonist mecamylamine completely and reversibly inhibited endothelial network formation. Mecamylamine 98-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. Isoflurane 12-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. Isoflurane 12-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. alkanols 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. alkanols 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. cyclopropane 193-205 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 12145051-1 2002 UNLABELLED: Isoflurane and normal alkanols reduce the apparent agonist dissociation constant (Kd) of the nicotinic acetylcholine receptor (nAChR) at clinically relevant concentrations, whereas cyclopropane and butane do not. butane 210-216 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 12145051-3 2002 To further define the nature of these interactions, we quantified the potencies with which a heterologous group of general anesthetics reduces the nAChR"s apparent Kd for acetylcholine. Acetylcholine 171-184 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 12145051-6 2002 These results suggest that anesthetics reduce the apparent agonist Kd of the nAChR by binding to a site that has a dipolarity and ability to accept hydrogen bonds that are similar to those of water, but a hydrogen bond-donating capacity that is less. Hydrogen 148-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 12145051-6 2002 These results suggest that anesthetics reduce the apparent agonist Kd of the nAChR by binding to a site that has a dipolarity and ability to accept hydrogen bonds that are similar to those of water, but a hydrogen bond-donating capacity that is less. Water 192-197 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 12145051-6 2002 These results suggest that anesthetics reduce the apparent agonist Kd of the nAChR by binding to a site that has a dipolarity and ability to accept hydrogen bonds that are similar to those of water, but a hydrogen bond-donating capacity that is less. Hydrogen 205-213 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 12145051-7 2002 IMPLICATIONS: Anesthetics representing a wide range of chemical classes reduce the apparent agonist dissociation constant of the Torpedo nicotinic acetylcholine receptor with aqueous potencies that are governed by their molecular volumes and hydrogen bond basicities. Hydrogen 242-250 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-169 12446934-5 2002 Studies that show nicotine-induced increases in nicotinic acetylcholine receptors (nAChR) and protection against age-related nAChR decline contrast, perhaps in a functionally relevant way, to losses of nAChR in AD. Nicotine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-81 12446934-5 2002 Studies that show nicotine-induced increases in nicotinic acetylcholine receptors (nAChR) and protection against age-related nAChR decline contrast, perhaps in a functionally relevant way, to losses of nAChR in AD. Nicotine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-88 12446934-5 2002 Studies that show nicotine-induced increases in nicotinic acetylcholine receptors (nAChR) and protection against age-related nAChR decline contrast, perhaps in a functionally relevant way, to losses of nAChR in AD. Nicotine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 12446934-5 2002 Studies that show nicotine-induced increases in nicotinic acetylcholine receptors (nAChR) and protection against age-related nAChR decline contrast, perhaps in a functionally relevant way, to losses of nAChR in AD. Nicotine 18-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 12446934-8 2002 More work is needed to ascertain whether acute or repetitive activation of nAChR with acute or intermittent exposure to nicotine or the persistent inactivation of nAChR with chronic nicotine exposure is a therapeutic objective and/or explains any pro-cognitive effects of those drugs. Nicotine 120-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 12446934-8 2002 More work is needed to ascertain whether acute or repetitive activation of nAChR with acute or intermittent exposure to nicotine or the persistent inactivation of nAChR with chronic nicotine exposure is a therapeutic objective and/or explains any pro-cognitive effects of those drugs. Nicotine 182-190 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 12193385-8 2002 The inhibition of the ACh-initiated and rhZP3-initiated AR by these nAChR antagonists strongly suggests the involvement of an alpha7 subunit-containing nAChR in the AR initiated by both ligands. Acetylcholine 22-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 12193385-8 2002 The inhibition of the ACh-initiated and rhZP3-initiated AR by these nAChR antagonists strongly suggests the involvement of an alpha7 subunit-containing nAChR in the AR initiated by both ligands. Acetylcholine 22-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 12193385-10 2002 In vitro results show for the first time that ACh can initiate the human sperm AR and strongly suggest that a human sperm alpha7 subunit-containing nAChR plays a role in the rhZP3-initiated AR. Acetylcholine 46-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 12198092-6 2002 Concentration dependence of closed-times is not predicted by sequential models of channel block, suggesting that tacrine blocks the nAChR by an unusual mechanism. Tacrine 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 12769608-4 2002 Non-specific nAChR agonists like nicotine and epibatidine, have been shown to have interesting pharmacology but their clinical value is limited by their undesirable side effects. Nicotine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 12769608-4 2002 Non-specific nAChR agonists like nicotine and epibatidine, have been shown to have interesting pharmacology but their clinical value is limited by their undesirable side effects. epibatidine 46-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 12769612-3 2002 In the present review we discuss the evidence that nicotine and subtype selective nAChR ligands can provide neuroprotection in in vitro cell culture systems and in in vivo studies in animal models of such disorders. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 12769612-9 2002 A variety of cellular mechanisms ranging from the production of growth factors through to inactivation of toxins and antioxidant actions of nicotine have been proposed to underlie the nAChR-mediated neuroprotection in vitro and in vivo. Nicotine 140-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 184-189 12130694-7 2002 The impairment of channel opening increases when the number of phenylalanine residues at 8" increases from two (wild-type nAChR) to five. Phenylalanine 63-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 12114323-6 2002 Furthermore, the relaxation was blocked by methyllycaconitine and alpha-bungarotoxin (preferential alpha7-nAChR antagonists) and mecamylamine but was not affected by dihydro-beta-erythroidine (a preferential alpha4-nAChR antagonist). methyllycaconitine 43-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 12109907-0 2002 Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. (2-chloro-5-pyridyl)-9-azabicyclo(4.2.1)non-2-ene 114-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 73-105 12109907-4 2002 Deschloro UB-165 (4) displayed a 2-3-fold decrease in affinity at alpha4beta2 and alpha3beta4 nAChR subtypes, as compared with (+/-)-UB-165, while at the alpha7 subtype a 31-fold increase in affinity was observed. deschloro ub 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 12109907-5 2002 At each of the nAChR subtypes, high affinity binding was dependent on the presence of a 3-substituted pyridine, and the other isomers, 5 and 6, resulted in marked decreases in binding affinities. 3-substituted pyridine 88-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 15-20 12109907-7 2002 Modest reductions in binding affinity were observed for all of the diazine ligands at all nAChR subtypes, with the exception of 7, which retained potency comparable to that of 4 in binding to alpha7 nAChR. sulfadiazine 67-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 12151749-4 2002 The paradoxical effects of nicotine on emotionality are likely due to the broad expression of nAChRs throughout the brain, the large number of nAChR subtypes that have been identified and the ability of nicotine treatment to both activate and desensitize nAChRs. Nicotine 27-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 12021403-2 2002 Nicotine has full efficacy on the alpha4beta2 nAChR and partial efficacy on the alpha3beta2 nAChR. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 12061885-2 2002 We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian alpha4beta2 nAChR whereas the negatively charged (delta(-)) tip of the neonicotinoid insecticides interacts with a putative cationic subsite of the insect nAChR. Neonicotinoids 16-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 12061885-2 2002 We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian alpha4beta2 nAChR whereas the negatively charged (delta(-)) tip of the neonicotinoid insecticides interacts with a putative cationic subsite of the insect nAChR. Neonicotinoids 16-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 299-304 12061885-2 2002 We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian alpha4beta2 nAChR whereas the negatively charged (delta(-)) tip of the neonicotinoid insecticides interacts with a putative cationic subsite of the insect nAChR. n-unsubstituted imine 49-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 12061885-2 2002 We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian alpha4beta2 nAChR whereas the negatively charged (delta(-)) tip of the neonicotinoid insecticides interacts with a putative cationic subsite of the insect nAChR. Neonicotinoids 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 12061885-2 2002 We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian alpha4beta2 nAChR whereas the negatively charged (delta(-)) tip of the neonicotinoid insecticides interacts with a putative cationic subsite of the insect nAChR. Neonicotinoids 16-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 299-304 12088062-0 2002 Cytisine derivatives as high affinity nAChR ligands: synthesis and comparative molecular field analysis. cytisine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 12021403-2 2002 Nicotine has full efficacy on the alpha4beta2 nAChR and partial efficacy on the alpha3beta2 nAChR. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 12021403-8 2002 When the residue located at position 258 in the M2 region of the alpha subunit was valine (as in the alpha3 subunit), the resulting nAChR exhibited partial efficacy for nicotine that was voltage-dependent. Valine 83-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 12021403-8 2002 When the residue located at position 258 in the M2 region of the alpha subunit was valine (as in the alpha3 subunit), the resulting nAChR exhibited partial efficacy for nicotine that was voltage-dependent. Nicotine 169-177 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 12021403-9 2002 Therefore, we believe that these M2 amino acids contribute to the formation of a binding site for nicotine in the alpha3beta2 nAChR channel, which results in a low-affinity channel block, causing the lower efficacy of nicotine on this nAChR. Nicotine 98-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 12021403-9 2002 Therefore, we believe that these M2 amino acids contribute to the formation of a binding site for nicotine in the alpha3beta2 nAChR channel, which results in a low-affinity channel block, causing the lower efficacy of nicotine on this nAChR. Nicotine 98-106 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 12021403-9 2002 Therefore, we believe that these M2 amino acids contribute to the formation of a binding site for nicotine in the alpha3beta2 nAChR channel, which results in a low-affinity channel block, causing the lower efficacy of nicotine on this nAChR. Nicotine 218-226 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 12021403-9 2002 Therefore, we believe that these M2 amino acids contribute to the formation of a binding site for nicotine in the alpha3beta2 nAChR channel, which results in a low-affinity channel block, causing the lower efficacy of nicotine on this nAChR. Nicotine 218-226 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-240 12065669-8 2002 Thus, nAChR subtypes are differentially coupled to specific sources of Ca2+: activation of nAChR induces a sustained elevation of intracellular Ca2+ levels which is highly dependent on the activation of VOCC, and also involves Ca2+ release from ryanodine and IP3-dependent intracellular stores. Ryanodine 245-254 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 11877392-2 2002 Nicotinic acetylcholine receptor (nAChR) gene expression is regulated by both muscle activity and increased intracellular calcium. Calcium 122-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-32 11877392-2 2002 Nicotinic acetylcholine receptor (nAChR) gene expression is regulated by both muscle activity and increased intracellular calcium. Calcium 122-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 12065669-4 2002 Nicotine (30 microm) generated a rapid elevation in cytoplasmic Ca2+ that was partially and additively inhibited (40%) by alpha7 and alpha3beta2* nAChR subtype selective antagonists; alpha3beta4* nAChR probably account for the remaining response (60%). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 12065669-8 2002 Thus, nAChR subtypes are differentially coupled to specific sources of Ca2+: activation of nAChR induces a sustained elevation of intracellular Ca2+ levels which is highly dependent on the activation of VOCC, and also involves Ca2+ release from ryanodine and IP3-dependent intracellular stores. Ryanodine 245-254 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 12065669-4 2002 Nicotine (30 microm) generated a rapid elevation in cytoplasmic Ca2+ that was partially and additively inhibited (40%) by alpha7 and alpha3beta2* nAChR subtype selective antagonists; alpha3beta4* nAChR probably account for the remaining response (60%). Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 196-201 12065669-6 2002 The elevation of intracellular Ca2+ levels provoked by nicotine was sustained for at least 10 min and required the persistent activation of nAChR throughout the response. Nicotine 55-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 12065669-8 2002 Thus, nAChR subtypes are differentially coupled to specific sources of Ca2+: activation of nAChR induces a sustained elevation of intracellular Ca2+ levels which is highly dependent on the activation of VOCC, and also involves Ca2+ release from ryanodine and IP3-dependent intracellular stores. Inositol 1,4,5-Trisphosphate 259-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 12065669-8 2002 Thus, nAChR subtypes are differentially coupled to specific sources of Ca2+: activation of nAChR induces a sustained elevation of intracellular Ca2+ levels which is highly dependent on the activation of VOCC, and also involves Ca2+ release from ryanodine and IP3-dependent intracellular stores. Inositol 1,4,5-Trisphosphate 259-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 11906697-3 2002 Nicotine enhances GABAergic transmission transiently, which is followed by a persistent depression of these inhibitory inputs due to nAChR desensitization. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 11840479-4 2002 The purpose of this study was to use double-labeling in situ hybridization to identify nAChR subunit mRNAs expressed within dopamine neurons of the SN/VTA, by using a digoxigenin-labeled riboprobe for tyrosine hydroxylase as the dopamine cell marker and (35)S-labeled riboprobes for nAChR subunits. Dopamine 124-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 11840479-4 2002 The purpose of this study was to use double-labeling in situ hybridization to identify nAChR subunit mRNAs expressed within dopamine neurons of the SN/VTA, by using a digoxigenin-labeled riboprobe for tyrosine hydroxylase as the dopamine cell marker and (35)S-labeled riboprobes for nAChR subunits. Digoxigenin 167-178 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 11840479-4 2002 The purpose of this study was to use double-labeling in situ hybridization to identify nAChR subunit mRNAs expressed within dopamine neurons of the SN/VTA, by using a digoxigenin-labeled riboprobe for tyrosine hydroxylase as the dopamine cell marker and (35)S-labeled riboprobes for nAChR subunits. Dopamine 229-237 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 11840479-5 2002 The results reveal a heterogeneous population of nAChR subunit mRNAs within midbrain dopamine neurons. Dopamine 85-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 11840479-6 2002 Within the SN, almost all dopamine neurons express alpha2, alpha4, alpha5, alpha6, beta2, and beta3 nAChR mRNAs, with more than half also expressing alpha3 and alpha7 mRNAs. Dopamine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 11961141-5 2002 Exogenous application of ACh indicated that high and low levels of nAChR activation in the Schaffer collaterals inhibit and facilitate, respectively, glutamate release onto CA1 neurons. Acetylcholine 25-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 11961141-5 2002 Exogenous application of ACh indicated that high and low levels of nAChR activation in the Schaffer collaterals inhibit and facilitate, respectively, glutamate release onto CA1 neurons. Glutamic Acid 150-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 11961141-6 2002 The finding then that the nAChR antagonists methyllycaconitine and dihydro-beta-erythroidine facilitated glutamatergic transmission between Schaffer collaterals and CA1 neurons indicated that in a single hippocampal slice, the inhibitory action of strongly, tonically activated nAChRs in some glutamatergic fibers prevails over the facilitatory action of weakly, tonically activated nAChRs in other glutamatergic fibers synapsing onto a given neuron. methyllycaconitine 44-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 11961141-6 2002 The finding then that the nAChR antagonists methyllycaconitine and dihydro-beta-erythroidine facilitated glutamatergic transmission between Schaffer collaterals and CA1 neurons indicated that in a single hippocampal slice, the inhibitory action of strongly, tonically activated nAChRs in some glutamatergic fibers prevails over the facilitatory action of weakly, tonically activated nAChRs in other glutamatergic fibers synapsing onto a given neuron. Dihydro-beta-Erythroidine 67-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 11961141-6 2002 The finding then that the nAChR antagonists methyllycaconitine and dihydro-beta-erythroidine facilitated glutamatergic transmission between Schaffer collaterals and CA1 neurons indicated that in a single hippocampal slice, the inhibitory action of strongly, tonically activated nAChRs in some glutamatergic fibers prevails over the facilitatory action of weakly, tonically activated nAChRs in other glutamatergic fibers synapsing onto a given neuron. nachrs 278-284 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 11961141-6 2002 The finding then that the nAChR antagonists methyllycaconitine and dihydro-beta-erythroidine facilitated glutamatergic transmission between Schaffer collaterals and CA1 neurons indicated that in a single hippocampal slice, the inhibitory action of strongly, tonically activated nAChRs in some glutamatergic fibers prevails over the facilitatory action of weakly, tonically activated nAChRs in other glutamatergic fibers synapsing onto a given neuron. nachrs 383-389 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 11953457-2 2002 Here, we study the effects of nAChR agonists on [3 H]-d-aspartate ([3 H]-d-ASP) release from synaptosomes superfused in conditions known to prevent indirect effects. [3 h]-d-aspartate 48-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 11952537-13 2002 The altered nAChR staining pattern in PPP skin may indicate a possible role for nicotine in the pathogenesis of PPP. Nicotine 80-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 11861446-1 2002 BACKGROUND: Autoantibodies against nicotinic acetylcholine receptor (nAChR) in myasthenia gravis (MG) patients are usually detected by radioimmunoprecipitation assays using extracted acetylcholine receptors labeled irreversibly with 125I-alpha-bungarotoxin (alpha-BuTx). Acetylcholine 45-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 11861446-1 2002 BACKGROUND: Autoantibodies against nicotinic acetylcholine receptor (nAChR) in myasthenia gravis (MG) patients are usually detected by radioimmunoprecipitation assays using extracted acetylcholine receptors labeled irreversibly with 125I-alpha-bungarotoxin (alpha-BuTx). 125i-alpha-bungarotoxin 233-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 11861446-1 2002 BACKGROUND: Autoantibodies against nicotinic acetylcholine receptor (nAChR) in myasthenia gravis (MG) patients are usually detected by radioimmunoprecipitation assays using extracted acetylcholine receptors labeled irreversibly with 125I-alpha-bungarotoxin (alpha-BuTx). 125i-alpha-bungarotoxin 233-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 11861446-1 2002 BACKGROUND: Autoantibodies against nicotinic acetylcholine receptor (nAChR) in myasthenia gravis (MG) patients are usually detected by radioimmunoprecipitation assays using extracted acetylcholine receptors labeled irreversibly with 125I-alpha-bungarotoxin (alpha-BuTx). alpha-butx 258-268 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 11861446-1 2002 BACKGROUND: Autoantibodies against nicotinic acetylcholine receptor (nAChR) in myasthenia gravis (MG) patients are usually detected by radioimmunoprecipitation assays using extracted acetylcholine receptors labeled irreversibly with 125I-alpha-bungarotoxin (alpha-BuTx). alpha-butx 258-268 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 11953457-2 2002 Here, we study the effects of nAChR agonists on [3 H]-d-aspartate ([3 H]-d-ASP) release from synaptosomes superfused in conditions known to prevent indirect effects. [3 h]-d-asp 67-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 11928712-9 2002 Thus, it appears likely that pre-synaptic nAChR on monoaminergic fibers are composed of alpha3 or alpha4 subunits in combination with the beta2 subunit, and these subunit compositions mediate dopaminergic and noradrenergic release, and glutamate is mainly controlled by the alpha7 subunit. Glutamic Acid 236-245 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 12829413-1 2002 While nicotine, through stimulation of a specific sub-population of nicotinic acetylcholine receptors (nAChR) appears to protect cells in culture against a variety of insults, studies in vivo show controversial results. Nicotine 6-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-101 12829413-1 2002 While nicotine, through stimulation of a specific sub-population of nicotinic acetylcholine receptors (nAChR) appears to protect cells in culture against a variety of insults, studies in vivo show controversial results. Nicotine 6-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 11752225-10 2002 These results show that nAChRs expressed in the primate striatum have similar affinities for nicotine, cytisine, and A85380, that alpha-conotoxin MII discriminates between nAChR populations in the caudate and putamen, and that alpha-conotoxin MII-sensitive nAChRs are selectively decreased after MPTP-induced nigrostriatal damage. Nicotine 93-101 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 11860617-3 2002 RESULTS: Based on the recent crystal structure of a soluble acetylcholine binding protein from snails, we have built atomic models of acetylcholine and nicotine bound to the pocket of four different human nAChR subtypes. Acetylcholine 60-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 11860617-3 2002 RESULTS: Based on the recent crystal structure of a soluble acetylcholine binding protein from snails, we have built atomic models of acetylcholine and nicotine bound to the pocket of four different human nAChR subtypes. Acetylcholine 134-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 11860617-3 2002 RESULTS: Based on the recent crystal structure of a soluble acetylcholine binding protein from snails, we have built atomic models of acetylcholine and nicotine bound to the pocket of four different human nAChR subtypes. Nicotine 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 205-210 11756485-3 2002 With ionotropic glutamate and GABA(A) transmission blocked, this stimulation evoked fast, atropine-insensitive EPSPs that were sensitive to nAChR antagonists. Glutamic Acid 16-25 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 11756485-3 2002 With ionotropic glutamate and GABA(A) transmission blocked, this stimulation evoked fast, atropine-insensitive EPSPs that were sensitive to nAChR antagonists. gamma-Aminobutyric Acid 30-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 11756485-3 2002 With ionotropic glutamate and GABA(A) transmission blocked, this stimulation evoked fast, atropine-insensitive EPSPs that were sensitive to nAChR antagonists. Atropine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 11756485-8 2002 ACh, nicotine, and choline (a selective alpha7 nAChR agonist) were effective in evoking action potentials and repetitive firing with synaptic transmission blocked by low Ca2+, high Mg2+ medium. Acetylcholine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 11756485-8 2002 ACh, nicotine, and choline (a selective alpha7 nAChR agonist) were effective in evoking action potentials and repetitive firing with synaptic transmission blocked by low Ca2+, high Mg2+ medium. Nicotine 5-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 11756485-8 2002 ACh, nicotine, and choline (a selective alpha7 nAChR agonist) were effective in evoking action potentials and repetitive firing with synaptic transmission blocked by low Ca2+, high Mg2+ medium. Choline 19-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 11756485-11 2002 This is the first demonstration that synaptically released ACh results in fast, alpha7 nAChR-mediated EPSPs in hypothalamic neurons. Acetylcholine 59-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 12140772-4 2002 In support of this hypothesis, preliminary evidence is presented suggesting that the potent, centrally acting nAChR antagonist, mecamylamine, which is devoid of monoamine reuptake inhibition, may reduce symptoms of depression and mood instability in patients with comorbid depression and bipolar disorder. Mecamylamine 128-140 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 11752225-10 2002 These results show that nAChRs expressed in the primate striatum have similar affinities for nicotine, cytisine, and A85380, that alpha-conotoxin MII discriminates between nAChR populations in the caudate and putamen, and that alpha-conotoxin MII-sensitive nAChRs are selectively decreased after MPTP-induced nigrostriatal damage. cytisine 103-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 11752225-10 2002 These results show that nAChRs expressed in the primate striatum have similar affinities for nicotine, cytisine, and A85380, that alpha-conotoxin MII discriminates between nAChR populations in the caudate and putamen, and that alpha-conotoxin MII-sensitive nAChRs are selectively decreased after MPTP-induced nigrostriatal damage. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 296-300 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 11741432-3 2001 The cysteinyl-cysteine ring is located in a region implicated in ligand binding, and conformational changes involving this ring may be important for modulation of nAChR function. cysteinylcysteine 4-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 11741432-12 2001 These conformational preferences are also observed in tetrapeptide and undecapeptide fragments of the human alpha7 subtype of the nAChR that contains the ox-[Cys-Cys] unit. cysteinylcysteine 158-165 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 11597489-2 2001 An efficient radiochemical synthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[(11)C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed. 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[(11)c]methyl-2-(s)-pyrrolidinylmethoxy)pyridine 40-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 11714893-5 2001 Of the LAs tested, those with structures containing two separated aromatic rings (e.g., proadifen and adiphenine) had the greatest inhibition potency (IC(50) values between 0.34 and 6.3 microM) but lowest selectivity (approximately 4-fold) across the four nAChR subtypes examined. Proadifen 88-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 256-261 11714893-5 2001 Of the LAs tested, those with structures containing two separated aromatic rings (e.g., proadifen and adiphenine) had the greatest inhibition potency (IC(50) values between 0.34 and 6.3 microM) but lowest selectivity (approximately 4-fold) across the four nAChR subtypes examined. adiphenine 102-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 256-261 11714893-6 2001 From the fused, two-ring (isoquinoline backbone) class of LAs, dimethisoquin had comparatively moderate inhibition potency (IC(50) values between 2.4 and 61 microM) and approximately 30-fold selectivity across nAChR subtypes. dimethisoquin 63-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 210-215 11714893-7 2001 Lidocaine, a commonly used LA from the single ring category of LAs, blocked nAChR function with IC(50) values of between 52 and 250 microM and had only approximately 5-fold selectivity across nAChR subtypes. Lidocaine 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 11714893-7 2001 Lidocaine, a commonly used LA from the single ring category of LAs, blocked nAChR function with IC(50) values of between 52 and 250 microM and had only approximately 5-fold selectivity across nAChR subtypes. Lidocaine 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 192-197 11557356-1 2001 In this structure-affinity relationship (SAFIR) study, the bioisosteric potential of diazines in the field of ferruginine-type nAChR ligands was investigated. diazines 85-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 11698101-4 2001 Electrostatic interactions of the nitroimine group and bridgehead nitrogen in imidacloprid with particular nAChR amino acid residues are likely to have key roles in determining the selective toxicity of imidacloprid. nitroimine 34-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 11698101-4 2001 Electrostatic interactions of the nitroimine group and bridgehead nitrogen in imidacloprid with particular nAChR amino acid residues are likely to have key roles in determining the selective toxicity of imidacloprid. Nitrogen 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 11698101-4 2001 Electrostatic interactions of the nitroimine group and bridgehead nitrogen in imidacloprid with particular nAChR amino acid residues are likely to have key roles in determining the selective toxicity of imidacloprid. imidacloprid 78-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 11557356-1 2001 In this structure-affinity relationship (SAFIR) study, the bioisosteric potential of diazines in the field of ferruginine-type nAChR ligands was investigated. ferruginine 110-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 11557356-4 2001 The bioisosteric replacement of the acetyl moiety as structural part of the lead compound 3 with the pyridazine, pyrimidine and pyrazine nucleus resulted in ligands with high to moderate affinity for the central alpha4beta2 and remarkably low affinity for the alpha7* nAChR subtypes. Cysteine 36-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-273 11557356-4 2001 The bioisosteric replacement of the acetyl moiety as structural part of the lead compound 3 with the pyridazine, pyrimidine and pyrazine nucleus resulted in ligands with high to moderate affinity for the central alpha4beta2 and remarkably low affinity for the alpha7* nAChR subtypes. pyridazine 101-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-273 11557356-4 2001 The bioisosteric replacement of the acetyl moiety as structural part of the lead compound 3 with the pyridazine, pyrimidine and pyrazine nucleus resulted in ligands with high to moderate affinity for the central alpha4beta2 and remarkably low affinity for the alpha7* nAChR subtypes. Pyrazines 128-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 268-273 11669505-13 2001 Galantamine has positive effects on nAChR expression, which are likely to contribute to its sustained efficacy in the treatment of AD patients. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 11690625-2 2001 Because this gene (CHRNA4) codes for a neuronal nicotinic acetylcholine receptor subunit, functional studies could be designed to evaluate the alterations caused by this mutation. Acetylcholine 58-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-25 11561100-3 2001 (+/-)-methadone inhibited nicotine-stimulated 86Rb+ efflux from the cells in a concentration-dependent manner with an IC50 value of 1.9 +/- 0.2 microM, indicating that it is a potent nAChR antagonist. Methadone 0-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 11561100-3 2001 (+/-)-methadone inhibited nicotine-stimulated 86Rb+ efflux from the cells in a concentration-dependent manner with an IC50 value of 1.9 +/- 0.2 microM, indicating that it is a potent nAChR antagonist. Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 11561100-3 2001 (+/-)-methadone inhibited nicotine-stimulated 86Rb+ efflux from the cells in a concentration-dependent manner with an IC50 value of 1.9 +/- 0.2 microM, indicating that it is a potent nAChR antagonist. Rubidium-86 46-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 11606328-10 2001 Ketamine is a noncompetitive inhibitor at both the alpha7 and alpha4beta2 nAChR. Ketamine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 11606328-11 2001 In contrast, BCl causes a parallel shift in the ACh dose-response curve at the alpha7 nAChR suggesting competitive inhibition. Acetylcholine 48-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 11606328-12 2001 Ketamine causes both voltage-dependent and use-dependent inhibition, only in the alpha4beta2 nAChR. Ketamine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 11772288-2 2001 During the 1990s, the discovery of the antinociceptive properties of the potent nAChR agonist epibatidine in rodents sparked interest in the analgesic potential of this class of compounds. epibatidine 94-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 11846996-0 2001 Effect of dimethoate on the function and expression of nicotinic acetylcholine receptor in primary skeletal muscle cell culture. Dimethoate 10-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 11846996-1 2001 To investigate the molecular mechanism of intermediate myasthenia syndrome (IMS), we analyzed the toxic effects of the representative organophosphate dimethoate on the function and expression of the nicotinic acetylcholine receptor (nAChR) in primary skeletal muscle cell culture. organophosphate dimethoate 134-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 199-231 11846996-1 2001 To investigate the molecular mechanism of intermediate myasthenia syndrome (IMS), we analyzed the toxic effects of the representative organophosphate dimethoate on the function and expression of the nicotinic acetylcholine receptor (nAChR) in primary skeletal muscle cell culture. organophosphate dimethoate 134-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 233-238 11846996-2 2001 The results showed that the expression of nAChR on the muscle cell membrane was significantly increased after cells were exposed to dimethoate (130 microM). Dimethoate 132-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 11846996-3 2001 AChR function measured by carbachol-induced (22)Na+ influx demonstrated that dimethoate may inhibit the nAChR function either by binding to a noncompetitive site and changing the conformational state of nAChR or by blocking the nAChR channel directly. Carbachol 26-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 11846996-3 2001 AChR function measured by carbachol-induced (22)Na+ influx demonstrated that dimethoate may inhibit the nAChR function either by binding to a noncompetitive site and changing the conformational state of nAChR or by blocking the nAChR channel directly. Dimethoate 77-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 11846996-3 2001 AChR function measured by carbachol-induced (22)Na+ influx demonstrated that dimethoate may inhibit the nAChR function either by binding to a noncompetitive site and changing the conformational state of nAChR or by blocking the nAChR channel directly. Dimethoate 77-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 11846996-3 2001 AChR function measured by carbachol-induced (22)Na+ influx demonstrated that dimethoate may inhibit the nAChR function either by binding to a noncompetitive site and changing the conformational state of nAChR or by blocking the nAChR channel directly. Dimethoate 77-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 11846996-4 2001 This study also demonstrated that dimethoate could rapidly induce the expression of c-fos, with a maximal effect at about 40 min, and c-fos might act as a transcriptional factor in regulating the expression of nAChR in the primary skeletal muscle cell culture following organophosphate exposure. Organophosphates 270-285 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 210-215 11695184-6 2001 The insect nAChR is the primary target site for the neonicotinoid insecticides, thereby providing an incentive to explore its functional architecture with neonicotinoid radioligands, photoaffinity probes and affinity chromatography matrices. Neonicotinoids 52-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 11695184-6 2001 The insect nAChR is the primary target site for the neonicotinoid insecticides, thereby providing an incentive to explore its functional architecture with neonicotinoid radioligands, photoaffinity probes and affinity chromatography matrices. Neonicotinoids 155-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 11587984-2 2001 The recent identification of nicotinic acetylcholine receptors (nAChR) in fetal lung suggests that the direct interaction between nicotine and nAChR in fetal lung may underlie the postnatal pulmonary abnormalities seen in such infants. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-62 11587984-2 2001 The recent identification of nicotinic acetylcholine receptors (nAChR) in fetal lung suggests that the direct interaction between nicotine and nAChR in fetal lung may underlie the postnatal pulmonary abnormalities seen in such infants. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 11587984-11 2001 This suggests that the interaction of nicotine with nAChR in developing lung is responsible for the altered pulmonary mechanics observed in human infants whose mothers smoked during pregnancy. Nicotine 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 11535018-4 2001 In addition, FITC-alpha-BT-neuromuscular junction complexes could also bind to the mesangial cells, and preincubation with unlabeled nAChR inhibited the binding. fitc-alpha-bt 13-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 11506765-1 2001 Molecular identification of the genes and resulting protein sequences for a large number of nicotinic acetylcholine receptor (nAChR) subunits has stimulated numerous studies highlighting their role in several human behaviors including neurological disorders and nicotine addiction. Nicotine 262-270 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-124 11466420-7 2001 These findings may indicate that most or all of (125)I-alpha-CtxMII-labeled nAChR subtypes in the basal ganglia are present on nigrostriatal dopaminergic neurons, in contrast to (125)I-epibatidine sites. ctxmii 61-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 11455009-1 2001 Quinacrine has been shown to act as a noncompetitive inhibitor of the nicotinic acetylcholine receptor (nAChR). Quinacrine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-102 11455009-1 2001 Quinacrine has been shown to act as a noncompetitive inhibitor of the nicotinic acetylcholine receptor (nAChR). Quinacrine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 11455009-9 2001 Results from both single-channel and macroscopic current recordings indicate that quinacrine increases the rate of nAChR desensitization and stabilizes the desensitized state. Quinacrine 82-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 11506765-1 2001 Molecular identification of the genes and resulting protein sequences for a large number of nicotinic acetylcholine receptor (nAChR) subunits has stimulated numerous studies highlighting their role in several human behaviors including neurological disorders and nicotine addiction. Nicotine 262-270 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 11408533-4 2001 The nAChR subtype mediating nicotine-induced dilation in isolated porcine basilar arterial rings denuded of endothelium was therefore examined pharmacologically and immunohistochemically. Nicotine 28-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 11350961-1 2001 Nerve-induced muscle activity suppresses nicotinic acetylcholine receptor (nAChR) gene expression by increasing intracellular calcium levels. Calcium 126-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 11350961-1 2001 Nerve-induced muscle activity suppresses nicotinic acetylcholine receptor (nAChR) gene expression by increasing intracellular calcium levels. Calcium 126-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 11350961-3 2001 How muscle depolarization or increased calcium mediates changes in nAChR promoter activity is not well understood. Calcium 39-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 11408533-5 2001 Results from using an in vitro tissue bath technique indicated that relaxation induced by nicotine (100 microM) was blocked by preferential alpha7-nAChR antagonists (methyllycaconitine and alpha-bungarotoxin) and nonspecific nAChR antagonist (mecamylamine) in a concentration-dependent manner, but was not affected by dihydro-beta-erythroidine (a preferential alpha4-nAChR antagonist). Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 11408533-5 2001 Results from using an in vitro tissue bath technique indicated that relaxation induced by nicotine (100 microM) was blocked by preferential alpha7-nAChR antagonists (methyllycaconitine and alpha-bungarotoxin) and nonspecific nAChR antagonist (mecamylamine) in a concentration-dependent manner, but was not affected by dihydro-beta-erythroidine (a preferential alpha4-nAChR antagonist). Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-230 11408533-5 2001 Results from using an in vitro tissue bath technique indicated that relaxation induced by nicotine (100 microM) was blocked by preferential alpha7-nAChR antagonists (methyllycaconitine and alpha-bungarotoxin) and nonspecific nAChR antagonist (mecamylamine) in a concentration-dependent manner, but was not affected by dihydro-beta-erythroidine (a preferential alpha4-nAChR antagonist). Nicotine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-230 11353813-1 2001 3-(Trifluoromethyl)-3-(m-[(125)I]iodophenyl)diazirine ([(125)I]TID) and [(3)H]tetracaine, an aromatic amine, are noncompetitive antagonists (NCAs) of the Torpedo species nicotinic acetylcholine receptor (nAChR), which have been shown by photoaffinity labeling to bind to a common site in the ion channel in the closed state. 3-(trifluoromethyl)-3-(m-[(125)i]iodophenyl)diazirine 0-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 11408602-2 2001 Whereas cocaine itself is a general nAChR noncompetitive antagonist, we report here the characterization of cocaine methiodide, a novel selective agonist for the alpha 7 subtype of nAChR. cocaine methiodide 108-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 11408602-3 2001 Data from (125)I-alpha-bungarotoxin binding assays indicate that cocaine methiodide binds to alpha 7 nAChR with a K(i) value of approximately 200 nM while electrophysiology studies indicate that the addition of a methyl group at the amine moiety of cocaine changes the drug"s activity profile from inhibitor to agonist. cocaine methiodide 65-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 11408602-3 2001 Data from (125)I-alpha-bungarotoxin binding assays indicate that cocaine methiodide binds to alpha 7 nAChR with a K(i) value of approximately 200 nM while electrophysiology studies indicate that the addition of a methyl group at the amine moiety of cocaine changes the drug"s activity profile from inhibitor to agonist. Cocaine 65-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 11408602-4 2001 Cocaine methiodide activates alpha 7 nAChR with an EC(50) value of approximately 50 microM and shows comparable efficacy to ACh in oocyte experiments. cocaine methiodide 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 11357122-2 2001 This superfamily of allosteric transmembrane proteins includes the nicotinic acetylcholine (nAChR), serotonin 5-HT3, gamma-aminobutyric-acid (GABAA and GABAC) and glycine receptors. nicotinic acetylcholine 67-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 11303054-3 2001 The selectivity of mecamylamine for neuronal nAChR was manifested primarily in terms of slow recovery rates from mecamylamine-induced inhibition. Mecamylamine 19-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 11303054-3 2001 The selectivity of mecamylamine for neuronal nAChR was manifested primarily in terms of slow recovery rates from mecamylamine-induced inhibition. Mecamylamine 113-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 11303054-6 2001 Mecamylamine inhibition of neuronal nAChR was noncompetitive and voltage dependent. Mecamylamine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 11245666-1 2001 Widely expressed in the brain, the alpha4beta2 nicotinic acetylcholine receptor (nAChR) is proposed to play a major role in the mechanisms that lead to and maintain nicotine addiction. Nicotine 165-173 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 11305656-3 2001 The nicotinic acetylcholine receptor (nAChr) agonists acetylcholine, carbachol, and (-)-nicotine were fractionated and detected by patch-clamped pheochromcytoma detector cells. Acetylcholine 14-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 11305656-3 2001 The nicotinic acetylcholine receptor (nAChr) agonists acetylcholine, carbachol, and (-)-nicotine were fractionated and detected by patch-clamped pheochromcytoma detector cells. Carbachol 69-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 11305656-3 2001 The nicotinic acetylcholine receptor (nAChr) agonists acetylcholine, carbachol, and (-)-nicotine were fractionated and detected by patch-clamped pheochromcytoma detector cells. Nicotine 84-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 11305656-3 2001 The nicotinic acetylcholine receptor (nAChr) agonists acetylcholine, carbachol, and (-)-nicotine were fractionated and detected by patch-clamped pheochromcytoma detector cells. Nicotine 84-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 11087759-5 2001 Within the coiled-coil domain neutralization of the charged side chains was tolerated, while alanine substitutions of large hydrophobic residues resulted in the loss of nAChR clustering. Alanine 93-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 169-174 11181898-2 2001 In the present studies, the effects of alcohols were characterized on defined combinations of human neuronal nAChR subunits heterologously expressed in Xenopus oocytes. Alcohols 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 11181898-6 2001 For the alpha(2)beta(4) receptor subunit combination, butanol clearly potentiated while pentanol inhibited ACh-induced current, whereas for alpha(4)beta(4) nAChR, propanol potentiated, butanol had no discernable effect, and pentanol inhibited receptor function. 1-Propanol 163-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 156-161 11181898-8 2001 The experimental results support the hypothesis that for both alpha(2)beta(4) and alpha(4)beta(4) receptor subtypes, molecular volume appears to be the most important determinant of both the potency as well as the direction of modulation of nAChR function by n-alcohols and related compounds. n-alcohols 259-269 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 11141083-1 2001 The lipophilic photoactivatable probe 3-(trifluoromethyl)-3-(m-iodophenyl) diazirine (TID) is a noncompetitive, resting-state inhibitor of the nicotinic acetylcholine receptor (nAChR) that requires tens of milliseconds of preincubation to inhibit agonist-induced cation efflux. 3-(trifluoromethyl)-3-(3-iodophenyl)diazirine 38-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-175 11141083-1 2001 The lipophilic photoactivatable probe 3-(trifluoromethyl)-3-(m-iodophenyl) diazirine (TID) is a noncompetitive, resting-state inhibitor of the nicotinic acetylcholine receptor (nAChR) that requires tens of milliseconds of preincubation to inhibit agonist-induced cation efflux. 3-(trifluoromethyl)-3-(3-iodophenyl)diazirine 38-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 11141083-1 2001 The lipophilic photoactivatable probe 3-(trifluoromethyl)-3-(m-iodophenyl) diazirine (TID) is a noncompetitive, resting-state inhibitor of the nicotinic acetylcholine receptor (nAChR) that requires tens of milliseconds of preincubation to inhibit agonist-induced cation efflux. 3-(trifluoromethyl)-3-(3-iodophenyl)diazirine 86-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-175 11141083-1 2001 The lipophilic photoactivatable probe 3-(trifluoromethyl)-3-(m-iodophenyl) diazirine (TID) is a noncompetitive, resting-state inhibitor of the nicotinic acetylcholine receptor (nAChR) that requires tens of milliseconds of preincubation to inhibit agonist-induced cation efflux. 3-(trifluoromethyl)-3-(3-iodophenyl)diazirine 86-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 11101308-4 2000 Using both single-channel and rapid patch perfusion electrophysiology, we measured how these mutations affect nAChR sensitivity to ethanol and hexanol. Ethanol 131-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 11135003-3 2001 Pretreatment of cultures with the nAChR antagonist dihydro-beta-erythroidine (DHBE) attenuated nicotine-induced changes in DNA abundance and synthesis. Dihydro-beta-Erythroidine 51-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 11135003-3 2001 Pretreatment of cultures with the nAChR antagonist dihydro-beta-erythroidine (DHBE) attenuated nicotine-induced changes in DNA abundance and synthesis. Dihydro-beta-Erythroidine 78-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 11135003-3 2001 Pretreatment of cultures with the nAChR antagonist dihydro-beta-erythroidine (DHBE) attenuated nicotine-induced changes in DNA abundance and synthesis. Nicotine 95-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 11135003-10 2001 The pharmacology of [3H]-epibatidine displacement from EGL neurons also suggested an interaction with the alpha3-nAChR subunits. Tritium 21-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 11135003-10 2001 The pharmacology of [3H]-epibatidine displacement from EGL neurons also suggested an interaction with the alpha3-nAChR subunits. epibatidine 25-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 11725817-4 2001 NAChR binding was assayed using 3H-epibatidine [3H-EPI]. 3h-epibatidine 32-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 11725817-4 2001 NAChR binding was assayed using 3H-epibatidine [3H-EPI]. 3h-epi 48-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 11101308-4 2000 Using both single-channel and rapid patch perfusion electrophysiology, we measured how these mutations affect nAChR sensitivity to ethanol and hexanol. Hexanols 143-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 110-115 11101308-6 2000 These results support the existence of a large inhibitory patch in the nAChR pore lining where interactions with alcohols are primarily due to hydrophobic forces. Alcohols 113-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 11101308-9 2000 The location and extent of this site can explain why small alcohols occupy the nAChR pore at the same time as larger alcohols or charged blockers, while two large alcohols bind in a mutually exclusive manner. Alcohols 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 11101308-9 2000 The location and extent of this site can explain why small alcohols occupy the nAChR pore at the same time as larger alcohols or charged blockers, while two large alcohols bind in a mutually exclusive manner. Alcohols 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 11101308-9 2000 The location and extent of this site can explain why small alcohols occupy the nAChR pore at the same time as larger alcohols or charged blockers, while two large alcohols bind in a mutually exclusive manner. Alcohols 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 10900197-1 2000 Recent work has shown that the nicotinic acetylcholine receptor (nAChR) can be fixed in distinct conformations by chemical cross-linking with glutardialdehyde, which abolishes allosteric transitions in the protein. Glutaral 142-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-63 11062464-8 2000 8), whose gene product, the beta 2 nicotinic acetylcholine receptor (nAChR) subunit, co-assembles with the alpha 4 nAChR subunit to form the active receptor. Acetylcholine 45-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 11082844-0 2000 An alternative improved synthesis of (-)-norferruginine, a potent nAChR agonist. ferruginine 37-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 11087577-5 2000 The thus obtained philanthotoxins were tested electrophysiologically for their antagonist properties on human muscle-type nicotinic acetylcholine receptors (nAChR) expressed in TE671 cells and on rat brain non-NMDA glutamate receptors (non-NMDAR) expressed in Xenopus oocytes. philanthotoxins 18-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 11087577-10 2000 Since the acyl group alterations in PhTX-343 and 4,9-dioxa-PhTX-12 have a similar effect on potency, which is distinctly different from that observed for PhTX-12, the two former compounds may bind to nAChR in a similar fashion but differently from that of PhTX-12. phtx 36-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 11087577-10 2000 Since the acyl group alterations in PhTX-343 and 4,9-dioxa-PhTX-12 have a similar effect on potency, which is distinctly different from that observed for PhTX-12, the two former compounds may bind to nAChR in a similar fashion but differently from that of PhTX-12. 4,9-dioxa-phtx-12 49-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 11087577-10 2000 Since the acyl group alterations in PhTX-343 and 4,9-dioxa-PhTX-12 have a similar effect on potency, which is distinctly different from that observed for PhTX-12, the two former compounds may bind to nAChR in a similar fashion but differently from that of PhTX-12. phTX 12 59-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 11087577-10 2000 Since the acyl group alterations in PhTX-343 and 4,9-dioxa-PhTX-12 have a similar effect on potency, which is distinctly different from that observed for PhTX-12, the two former compounds may bind to nAChR in a similar fashion but differently from that of PhTX-12. phTX 12 154-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 200-205 11044745-7 2000 The calmodulin antagonist fluphenazine prevented inhibition of the NMDA-receptor current by nAChR activity, suggesting that a Ca(2+)-calmodulin-dependent process mediated the effect of nicotine. Fluphenazine 26-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 11044745-7 2000 The calmodulin antagonist fluphenazine prevented inhibition of the NMDA-receptor current by nAChR activity, suggesting that a Ca(2+)-calmodulin-dependent process mediated the effect of nicotine. Nicotine 185-193 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 11044750-5 2000 Nicotine protection was prevented by 1 microM MLA, confirming that it was mediated by nAChR, and by 1 microM alpha-bungarotoxin, demonstrating that the alpha7 nAChR subtype was responsible. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 11044750-5 2000 Nicotine protection was prevented by 1 microM MLA, confirming that it was mediated by nAChR, and by 1 microM alpha-bungarotoxin, demonstrating that the alpha7 nAChR subtype was responsible. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 11044753-8 2000 These results suggest that the loss of nicotine binding in the putamen in Parkinson"s disease may involve an nAChR subunit (e.g., alpha5 and/or alpha6) other than those investigated. Nicotine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 10900197-1 2000 Recent work has shown that the nicotinic acetylcholine receptor (nAChR) can be fixed in distinct conformations by chemical cross-linking with glutardialdehyde, which abolishes allosteric transitions in the protein. Glutaral 142-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 10900197-3 2000 The same ligands were tested for their ability to convert the nAChR from a conformation with low affinity to a conformation with high affinity for acetylcholine. Acetylcholine 147-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 10900197-7 2000 With a similar approach we could show that the non-competitive inhibitor ethidium is displaced in a non-allosteric manner by other well characterized channel blockers from the cross-linked nAChR. Ethidium 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 10859324-1 2000 Most general anesthetics including long chain aliphatic alcohols act as noncompetitive antagonists of the nicotinic acetylcholine receptor (nAChR). Alcohols 56-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-138 10880991-13 2000 These results indicate that [(3)H]cytisine and [(125)I]alpha-bungarotoxin identify distinct nAChR subtypes in the tectum that likely contain non-alpha7 and alpha7 subunits, respectively. cytisine 34-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 10859324-1 2000 Most general anesthetics including long chain aliphatic alcohols act as noncompetitive antagonists of the nicotinic acetylcholine receptor (nAChR). Alcohols 56-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. Alcohols 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. Alcohols 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. Alcohols 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. alcohol 3-[(3)h]azioctanol 117-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 76-81 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. alcohol 3-[(3)h]azioctanol 117-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 10859324-2 2000 To locate the sites of interaction of a long chain alcohol with the Torpedo nAChR, we have used the photoactivatible alcohol 3-[(3)H]azioctanol, which inhibits the nAChR and photoincorporates into nAChR subunits. alcohol 3-[(3)h]azioctanol 117-143 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 10859324-3 2000 At 1 and 275 microm, 3-[(3)H]azioctanol photoincorporated into nAChR subunits with increased incorporation in the alpha-subunit in the desensitized state. 3-[(3)h]azioctanol 21-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 10971047-9 2000 This allosteric interaction amplifies the actions of ACh at post- and presynaptic nAChR. Acetylcholine 53-56 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 10971047-10 2000 In particular, presynaptic nAChR are capable of modulating the release of ACh and other neurotransmitters, such as glutamate, serotonin and GABA, which may contribute to symptoms of the illness. Glutamic Acid 115-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 10971047-10 2000 In particular, presynaptic nAChR are capable of modulating the release of ACh and other neurotransmitters, such as glutamate, serotonin and GABA, which may contribute to symptoms of the illness. Serotonin 126-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 10971047-10 2000 In particular, presynaptic nAChR are capable of modulating the release of ACh and other neurotransmitters, such as glutamate, serotonin and GABA, which may contribute to symptoms of the illness. gamma-Aminobutyric Acid 140-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 10971047-16 2000 Galantamine"s modulatory effects on nAChR may influence transcriptional regulation, resulting in an increased synthesis of nAChR. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 10971047-16 2000 Galantamine"s modulatory effects on nAChR may influence transcriptional regulation, resulting in an increased synthesis of nAChR. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 11089431-1 2000 Myasthenia gravis (MG) is an antigen-specific autoimmune disease in which antibodies directed against nicotinic acetylcholine receptors of the postsynaptic muscle membrane (nAChR) impair neuromuscular transmission. Acetylcholine 112-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 173-178 10942040-3 2000 Evidence is provided that functional alpha7- and alpha4beta2-like nAChRs are present on somatodendritic and/or preterminal/terminal regions of interneurons in the CA1 field of the rat hippocampus and in the human cerebral cortex and that activation of the different nAChR subtypes present in the preterminal/terminal areas of the interneurons triggers the tetrodotoxin-sensitive release of GABA. Tetrodotoxin 356-368 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 10942040-3 2000 Evidence is provided that functional alpha7- and alpha4beta2-like nAChRs are present on somatodendritic and/or preterminal/terminal regions of interneurons in the CA1 field of the rat hippocampus and in the human cerebral cortex and that activation of the different nAChR subtypes present in the preterminal/terminal areas of the interneurons triggers the tetrodotoxin-sensitive release of GABA. gamma-Aminobutyric Acid 390-394 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 10942046-4 2000 Due to the resulting increase in synaptic acetylcholine levels, both in concentration and time, additional nAChR molecules, e.g. those more distant from the ACh release sites, could be activated. Acetylcholine 42-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 10942029-4 2000 Taken together experimental and clinical data largely indicate a neuroprotective/trophic role of nAChR activation involving mainly alpha7 and alpha4beta2 nAChR subtypes, as evidenced using selective nAChR antagonists, and by potent nAChR agonists recently found displaying efficacy and/or larger selective affinities than (-)-nicotine for neuronal nAChR subtypes. Nicotine 322-334 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 10860932-3 2000 Here, another commonly abused drug, cocaine, is shown to selectively inhibit particular nAChR subtypes with a potency in the low micromolar range by interacting with separate sites associated with the alpha4 and beta4 nAChR subunits. Cocaine 36-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 10860932-3 2000 Here, another commonly abused drug, cocaine, is shown to selectively inhibit particular nAChR subtypes with a potency in the low micromolar range by interacting with separate sites associated with the alpha4 and beta4 nAChR subunits. Cocaine 36-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 218-223 10938474-0 2000 Synthesis and evaluation of 6-[(18)F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine as a PET tracer for nicotinic acetylcholine receptors. 6-[(18)f]fluoro-3-(2(s)-azetidinylmethoxy)pyridine 28-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-132 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). Nicotine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 10867984-2 2000 OBJECTIVE: The present study sought to examine the effects of the nAchR antagonist mecamylamine on inspection time. Mecamylamine 83-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-71 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). Nicotine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). epibatidine 124-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). epibatidine 124-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). methyllycaconitine 185-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 10773216-5 2000 This inhibition was sensitive to, and reversed by, not only nicotinic acetylcholine receptor (nAChR) agonists (nicotine and epibatidine), but also the alpha7 nAChR-selective antagonist methyllycaconitine (MLA). methyllycaconitine 205-208 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 10735809-0 2000 Pentobarbital has curare-like effects on adult-type nicotinic acetylcholine receptor channel currents. Pentobarbital 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 10735809-2 2000 We investigated block of nicotinic acetylcholine receptor (nAChR) channel currents by PB using the patch-clamp technique in combination with an ultrafast system for solution exchange. Pentobarbital 86-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-57 10735809-2 2000 We investigated block of nicotinic acetylcholine receptor (nAChR) channel currents by PB using the patch-clamp technique in combination with an ultrafast system for solution exchange. Pentobarbital 86-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 10735809-6 2000 Preincubation of nAChR channels with PB led to a decrease of the peak current amplitude without alteration of activation and desensitization kinetics caused by competitive block of nAChR channels. Pentobarbital 37-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 10735809-6 2000 Preincubation of nAChR channels with PB led to a decrease of the peak current amplitude without alteration of activation and desensitization kinetics caused by competitive block of nAChR channels. Pentobarbital 37-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 181-186 10735809-7 2000 In conclusion, similar to the effect of d-Tubocurarine, block of nAChR channel currents by PB can be explained by a combination of open-channel and competitive block. Pentobarbital 91-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 10735809-9 2000 PB elicited open-channel block and competitive block of nicotinic acetylcholine receptor channel currents, whereas the latter seems to be effective in clinically relevant concentrations. Pentobarbital 0-2 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-88 10812948-0 2000 Recombinant human receptors and functional assays in the discovery of altinicline (SIB-1508Y), a novel acetylcholine-gated ion channel (nAChR) agonist. altinicline maleate 70-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 10812948-0 2000 Recombinant human receptors and functional assays in the discovery of altinicline (SIB-1508Y), a novel acetylcholine-gated ion channel (nAChR) agonist. Acetylcholine 103-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 10812948-2 2000 The discovery that neuronal nAChRs are further subdivided into multiple subtypes suggests that drugs which act selectively at specific nAChR subtypes might effectively treat Parkinson"s disease (PD), Alzheimer"s disease (AD), schizophrenia, ADHD, depression, anxiety or pain without the accompanying adverse side effects associated with non-selective agents such as nicotine (1) and epibatidine. Nicotine 366-374 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 10812948-2 2000 The discovery that neuronal nAChRs are further subdivided into multiple subtypes suggests that drugs which act selectively at specific nAChR subtypes might effectively treat Parkinson"s disease (PD), Alzheimer"s disease (AD), schizophrenia, ADHD, depression, anxiety or pain without the accompanying adverse side effects associated with non-selective agents such as nicotine (1) and epibatidine. epibatidine 383-394 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. dioleoylphosphatidic acid 83-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-161 10653787-5 2000 After correcting for nonspecific partitioning into the lipid, the equilibrium dissociation constant, K(d), of isoflurane binding to nAChR at 15 degrees C was found to be 0.36 +/- 0.03 mM. Isoflurane 110-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. Cholesterol 15-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-161 10668717-8 2000 For the block of nAChR channel currents with a-bungarotoxin, a similar mechanism of block was found. a-bungarotoxin 45-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. dioleoylphosphatidic acid 83-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. Cholesterol 28-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-161 10625607-2 2000 The difference between spectra recorded in the presence and absence of agonist from the nAChR reconstituted into 3:1:1 egg phosphatidylcholine (EPC)/DOPA/Chol membranes exhibits positive and negative bands that serve as markers of the structural changes associated with the resting to desensitized conformational change. Phosphatidylcholines 123-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. dioleoylphosphatidic acid 56-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-161 10625607-1 2000 The effects of cholesterol (Chol) and an anionic lipid, dioleoylphosphatidic acid (DOPA) on the conformational equilibria of the nicotinic acetylcholine receptor (nAChR) have been investigated using Fourier transform infrared difference spectroscopy. dioleoylphosphatidic acid 56-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 163-168 10625607-2 2000 The difference between spectra recorded in the presence and absence of agonist from the nAChR reconstituted into 3:1:1 egg phosphatidylcholine (EPC)/DOPA/Chol membranes exhibits positive and negative bands that serve as markers of the structural changes associated with the resting to desensitized conformational change. epc 144-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 10625607-2 2000 The difference between spectra recorded in the presence and absence of agonist from the nAChR reconstituted into 3:1:1 egg phosphatidylcholine (EPC)/DOPA/Chol membranes exhibits positive and negative bands that serve as markers of the structural changes associated with the resting to desensitized conformational change. dioleoylphosphatidic acid 149-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 10625607-2 2000 The difference between spectra recorded in the presence and absence of agonist from the nAChR reconstituted into 3:1:1 egg phosphatidylcholine (EPC)/DOPA/Chol membranes exhibits positive and negative bands that serve as markers of the structural changes associated with the resting to desensitized conformational change. Cholesterol 154-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. Cholesterol 27-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. Cholesterol 27-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. dioleoylphosphatidic acid 35-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. dioleoylphosphatidic acid 155-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. dioleoylphosphatidic acid 155-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. dioleoylphosphatidic acid 155-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. dioleoylphosphatidic acid 155-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 191-196 10625607-5 2000 At higher levels of either Chol or DOPA, the nAChR is stabilized in a conformation that is capable of undergoing agonist-induced desensitization, although DOPA appears to be required for the nAChR to adopt a conformation fully equivalent to that found in native and 3:1:1 EPC/DOPA/Chol membranes. Cholesterol 281-285 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 10601857-0 2000 Structure-activity relationship and site of binding of polyamine derivatives at the nicotinic acetylcholine receptor. Polyamines 55-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-116 11261802-1 2000 The neuronal nicotinic acetylcholine receptors (nAChR) are involved in functional processes in brain including cognitive function and memory. Acetylcholine 23-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 11261802-4 2000 (S) [11C]Nicotine, has so far been the only nAChR ligand used in positron emission tomography (PET) studies for visualizing nAChRs in human brain. Nicotine 9-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 11261802-9 2000 Due to a probably high alpha4beta2 nAChR selectivity combined with low toxicity, the A-85380 analogs presently seem to be the most promising nAChR ligand imaging of subtypes of nAChRs in human brain. A 85380 85-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 11261802-9 2000 Due to a probably high alpha4beta2 nAChR selectivity combined with low toxicity, the A-85380 analogs presently seem to be the most promising nAChR ligand imaging of subtypes of nAChRs in human brain. A 85380 85-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 11261808-0 2000 Galantamine is an allosterically potentiating ligand of the human alpha4/beta2 nAChR. Galantamine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 11261808-2 2000 Originally established as a reversible inhibitor of the acetylcholine-degrading enzyme acetylcholinesterase (AChE), galantamine also acts as an allosterically potentiating ligand (APL) on nicotinic acetylcholine receptors (nAChR). Galantamine 116-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 188-221 11261808-2 2000 Originally established as a reversible inhibitor of the acetylcholine-degrading enzyme acetylcholinesterase (AChE), galantamine also acts as an allosterically potentiating ligand (APL) on nicotinic acetylcholine receptors (nAChR). Galantamine 116-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 223-228 11261808-4 2000 This nAChR-sensitizing action is not a common property of all, or most, AChE inhibitors, as is shown by the absence of this effect for other therapeutically applied AChE inhibitors including tacrine, metrifonate, rivastigmine and donepezil. Rivastigmine 213-225 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 11261808-4 2000 This nAChR-sensitizing action is not a common property of all, or most, AChE inhibitors, as is shown by the absence of this effect for other therapeutically applied AChE inhibitors including tacrine, metrifonate, rivastigmine and donepezil. Donepezil 230-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). philanthotoxins 28-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). philanthotoxins 28-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). phtxs 45-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). phtxs 45-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). polyamine amides 61-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 10601857-1 2000 Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). polyamine amides 61-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 10601857-9 2000 To elucidate the site of PhTX binding, a photolabile, radioactive PhTX derivative was photocross-linked to the nAChR in its closed channel conformation resulting in labeling yields for the two alpha and the beta, gamma and delta subunits of 10.4, 11.1, 4.0 and 7.4%, respectively. phtx 25-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 10601857-9 2000 To elucidate the site of PhTX binding, a photolabile, radioactive PhTX derivative was photocross-linked to the nAChR in its closed channel conformation resulting in labeling yields for the two alpha and the beta, gamma and delta subunits of 10.4, 11.1, 4.0 and 7.4%, respectively. phtx 66-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 11205143-3 2000 This neuroprotective/trophic role of nAChR activation has been mainly mediated by alpha7 and alpha4beta2 nAChR subtypes, as evidenced using selective nAChR antagonists, and by potent nAChR agonists recently found displaying efficacy and/or larger selective affinities than (-)-nicotine for neuronal nAChR subtypes. Nicotine 277-285 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 10563623-10 1999 C755T replaced serine 252 (Ser252) in the second membrane-spanning domain (M2) of CHRNA4 with a leucine. Leucine 96-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-88 10627582-3 2000 The whole-cell mode of the patch-clamp technique was used to record responses triggered by U-tube application of the nonselective agonist ACh and of the alpha7-nAChR-selective agonist choline to interneurons visualized by means of infrared-assisted videomicroscopy in slices of the human cerebral cortex. Choline 184-191 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-165 10755645-3 2000 Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 6-FA. 6-fa 160-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 10602707-0 1999 Analogues of neuroactive polyamine wasp toxins that lack inner basic sites exhibit enhanced antagonism toward a muscle-type mammalian nicotinic acetylcholine receptor. Polyamines 25-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 134-166 10563623-10 1999 C755T replaced serine 252 (Ser252) in the second membrane-spanning domain (M2) of CHRNA4 with a leucine. Serine 15-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-88 10572015-5 1999 On the basis of these results, we also describe a simple protocol for identifying disulfide loops in soluble and membrane proteins, exemplified by the alpha subunit of the muscle nicotinic acetylcholine receptor (nAChR). Disulfides 82-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 213-218 10487182-6 1999 RESULTS: ACh-evoked currents at the human alpha4beta2 nAChR were readily and reversibly inhibited by approximately 100 microM CBZ. Acetylcholine 9-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 10509744-3 1999 Nicotine, a neuronal nicotinic acetylcholine receptor (nAChR) agonist, has long been known to have antinociceptive effects in both experimental animals and humans. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 10509744-3 1999 Nicotine, a neuronal nicotinic acetylcholine receptor (nAChR) agonist, has long been known to have antinociceptive effects in both experimental animals and humans. Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 10509744-6 1999 Epibatidine, a potent nAChR agonist, was found to have full efficacy relative to opioids in preclinical pain models. epibatidine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 10509744-8 1999 Moreover, exploration of the molecular biology of nAChRs revealed evidence of receptor diversity, suggesting that nAChR subtype-selective agents less toxic than nicotine might be discovered; and early medicinal chemistry efforts already have resulted in compounds with improved safety profiles. Nicotine 161-169 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 10509744-9 1999 For example, ABT-594 is a nAChR agonist with the antinociceptive efficacy of epibatidine, but with an improved safety profile. 5-(2-azetidinylmethoxy)-2-chloropyridine 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10509744-9 1999 For example, ABT-594 is a nAChR agonist with the antinociceptive efficacy of epibatidine, but with an improved safety profile. epibatidine 77-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10487182-6 1999 RESULTS: ACh-evoked currents at the human alpha4beta2 nAChR were readily and reversibly inhibited by approximately 100 microM CBZ. Carbamazepine 126-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 54-59 10487182-11 1999 The increased sensitivity of these mutant receptors supports the hypothesis that the antiepileptic activity of CBZ can, at least to some extent, be attributed to the nAChR inhibition. Carbamazepine 111-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 10428390-2 1999 Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H-thienylcyclohexyl-piperidine (TCP). tenocyclidine 163-194 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 10441742-1 1999 As a first step in determining whether there are polymorphisms in the nicotinic acetylcholine receptor (nAChR) genes that are associated with nicotine addiction, we isolated genomic clones of the beta2-nAChR genes from human and mouse BAC libraries. Nicotine 142-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-102 10441742-1 1999 As a first step in determining whether there are polymorphisms in the nicotinic acetylcholine receptor (nAChR) genes that are associated with nicotine addiction, we isolated genomic clones of the beta2-nAChR genes from human and mouse BAC libraries. Nicotine 142-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 10450598-0 1999 SER252PHE and 776INS3 mutations in the CHRNA4 gene are rare in the Italian ADNFLE population. ser252phe 0-9 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-45 10366615-1 1999 It is hypothesized that desensitization of neuronal nicotinic acetylcholine receptors (nAChRs) induced by chronic exposure to nicotine initiates upregulation of nAChR number. Nicotine 126-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 10419547-0 1999 Photoaffinity labeling the torpedo nicotinic acetylcholine receptor with [(3)H]tetracaine, a nondesensitizing noncompetitive antagonist. [(3)h]tetracaine 73-89 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 10419547-1 1999 Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). Tetracaine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 246-278 10419547-1 1999 Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). Tetracaine 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 280-285 10419547-1 1999 Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). n,n-dimethylaminoethyl-4-butylaminobenzoate 12-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 246-278 10419547-1 1999 Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). aromatic amine 189-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 246-278 10419547-1 1999 Tetracaine (N,N-dimethylaminoethyl-4-butylaminobenzoate) and related N,N-dialkylaminoethyl substituted benzoic acid esters have been used to characterize the high-affinity binding site for aromatic amine noncompetitive antagonists in the Torpedo nicotinic acetylcholine receptor (nAChR). aromatic amine 189-203 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 280-285 10419547-2 1999 [(3)H]Tetracaine binds at equilibrium to a single site with a K(eq) value of 0.5 microM in the absence of agonist or presence of alpha-bungarotoxin and with a K(eq) value of 30 microM in the presence of agonist (i.e., for nAChR in the desensitized state). [(3)h]tetracaine 0-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 222-227 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). n,n-deae 73-81 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). n,n-diethylaminopropyl esters 86-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). 4-ethoxybenzoic acid ester 219-245 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). 2-diethylaminoethanol 249-273 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). 4-amino benzoate ester 291-313 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-3 1999 Preferential binding to nAChR in the absence of agonist is also seen for N,N-DEAE and N,N-diethylaminopropyl esters, both binding with 10-fold higher affinity in the absence of agonist than in the presence, and for the 4-ethoxybenzoic acid ester of N, N-diethylaminoethanol, but not for the 4-amino benzoate ester (procaine). Procaine 315-323 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 10419547-4 1999 Irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine resulted in covalent incorporation with similar efficiency into nAChR alpha, beta, gamma, and delta subunits. [(3)h]tetracaine 64-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 10419547-4 1999 Irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine resulted in covalent incorporation with similar efficiency into nAChR alpha, beta, gamma, and delta subunits. [(3)h]tetracaine 64-80 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 10419547-5 1999 The pharmacological specificity of nAChR subunit photolabeling as well as its dependence on [(3)H]tetracaine concentration establish that the observed photolabeling is at the high-affinity [(3)H]tetracaine-binding site. [(3)h]tetracaine 92-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 10419547-5 1999 The pharmacological specificity of nAChR subunit photolabeling as well as its dependence on [(3)H]tetracaine concentration establish that the observed photolabeling is at the high-affinity [(3)H]tetracaine-binding site. Tetracaine 98-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 10419547-7 1999 With all four subunits contributing to [(3)H]tetracaine site, the site in the closed channel state of the nAChR is most likely within the central ion channel domain. [(3)h]tetracaine 39-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 106-111 10419548-0 1999 Identification of amino acids of the torpedo nicotinic acetylcholine receptor contributing to the binding site for the noncompetitive antagonist [(3)H]tetracaine. [(3)h]tetracaine 145-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-77 10419548-1 1999 [(3)H]Tetracaine is a noncompetitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds with high affinity in the absence of cholinergic agonist (K(eq) = 0.5 microM) and weakly (K(eq) = 30 microM) in the presence of agonist (i.e., to nAChR in the desensitized state). [(3)h]tetracaine 0-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-95 10419548-1 1999 [(3)H]Tetracaine is a noncompetitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds with high affinity in the absence of cholinergic agonist (K(eq) = 0.5 microM) and weakly (K(eq) = 30 microM) in the presence of agonist (i.e., to nAChR in the desensitized state). [(3)h]tetracaine 0-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 10419548-1 1999 [(3)H]Tetracaine is a noncompetitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds with high affinity in the absence of cholinergic agonist (K(eq) = 0.5 microM) and weakly (K(eq) = 30 microM) in the presence of agonist (i.e., to nAChR in the desensitized state). [(3)h]tetracaine 0-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 261-266 10419548-2 1999 In the absence of agonist, irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine results in specific photoincorporation of [(3)H]tetracaine into each nAChR subunit. [(3)h]tetracaine 91-107 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 10419548-2 1999 In the absence of agonist, irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine results in specific photoincorporation of [(3)H]tetracaine into each nAChR subunit. [(3)h]tetracaine 91-107 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 10419548-2 1999 In the absence of agonist, irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine results in specific photoincorporation of [(3)H]tetracaine into each nAChR subunit. [(3)h]tetracaine 150-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 10419548-2 1999 In the absence of agonist, irradiation at 302 nm of nAChR-rich membranes equilibrated with [(3)H]tetracaine results in specific photoincorporation of [(3)H]tetracaine into each nAChR subunit. [(3)h]tetracaine 150-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 10419548-3 1999 In this report, we identify the amino acids of each nAChR subunit specifically photolabeled by [(3)H]tetracaine that contribute to the high-affinity binding site. [(3)h]tetracaine 95-111 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 10419548-4 1999 Subunits isolated from nAChR-rich membranes photolabeled with [(3)H]tetracaine were subjected to enzymatic digestion, and peptides containing (3)H were purified by SDS-polyacrylamide gel electrophoresis followed by reversed phase HPLC. [(3)h]tetracaine 62-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 10377231-0 1999 Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors. 2-fluoro-3-[2(s)-2-azetidinylmethoxy]pyridine 77-122 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. 3-pyridyl ethers 37-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-218 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. 3-pyridyl ethers 37-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 220-225 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. azetidine 59-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-218 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. azetidine 59-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 220-225 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. 3-[(s)-2-azetidinylmethoxy]pyridine 89-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 186-218 10377231-1 1999 The lead compound of a new series of 3-pyridyl ethers, the azetidine derivative A-85380 (3-[(S)-2-azetidinylmethoxy]pyridine), is a potent and selective ligand for the human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtype. 3-[(s)-2-azetidinylmethoxy]pyridine 89-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 220-225 10428390-2 1999 Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H-thienylcyclohexyl-piperidine (TCP). tenocyclidine 163-194 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 10428390-2 1999 Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H-thienylcyclohexyl-piperidine (TCP). tenocyclidine 196-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 10428390-2 1999 Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range according to an inhibition assay using 3H-thienylcyclohexyl-piperidine (TCP). tenocyclidine 196-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 10213799-6 1999 Discussed are recent advances in the areas of: 1) g-aminobutyric acid subtype A receptor/benzodiazepine (GABAA/BZ) inverse agonists; 2) nicotinic acetylcholine receptor (nAChR) agonists; 3) serotonin subtype 3 receptor (5-HT3R) antagonists; and 4) potassium (K+) M-channel inhibitors. Serotonin 190-199 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 10359088-0 1999 Neuronal nAChR stereoselectivity to non-natural epibatidine derivatives. epibatidine 48-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 10213799-6 1999 Discussed are recent advances in the areas of: 1) g-aminobutyric acid subtype A receptor/benzodiazepine (GABAA/BZ) inverse agonists; 2) nicotinic acetylcholine receptor (nAChR) agonists; 3) serotonin subtype 3 receptor (5-HT3R) antagonists; and 4) potassium (K+) M-channel inhibitors. Potassium 248-257 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-175 10215652-2 1999 The aim of the present study was to characterize the effect of acute ethanol treatment on different combinations of human nAChR (hnAChR) subunits expressed in Xenopus oocytes. Ethanol 69-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 10037483-3 1999 This study also confirms previous findings of nAChR functional block by fluoxetine (Prozac). Fluoxetine 72-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 10216184-1 1999 Tetracycline-regulated expression of recombinant nicotinic acetylcholine receptors (nAChR) composed of human alpha7 subunits is achieved in native nAChR-null SH-EP1 human epithelial cells. Tetracycline 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-82 10216184-1 1999 Tetracycline-regulated expression of recombinant nicotinic acetylcholine receptors (nAChR) composed of human alpha7 subunits is achieved in native nAChR-null SH-EP1 human epithelial cells. Tetracycline 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 84-89 10216184-1 1999 Tetracycline-regulated expression of recombinant nicotinic acetylcholine receptors (nAChR) composed of human alpha7 subunits is achieved in native nAChR-null SH-EP1 human epithelial cells. Tetracycline 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 10216184-5 1999 Chronic exposure to nicotine induces up-regulation of human recombinant alpha7-nAChR (80% up-regulation at 10 microM nicotine) just as it does native alpha7-nAChR in other human cell lines. Nicotine 20-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 10216184-5 1999 Chronic exposure to nicotine induces up-regulation of human recombinant alpha7-nAChR (80% up-regulation at 10 microM nicotine) just as it does native alpha7-nAChR in other human cell lines. Nicotine 20-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 10216184-5 1999 Chronic exposure to nicotine induces up-regulation of human recombinant alpha7-nAChR (80% up-regulation at 10 microM nicotine) just as it does native alpha7-nAChR in other human cell lines. Nicotine 117-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 10191324-7 1999 It is this alpha3-containing nAChR subtype that probably accounts for most of the excess activity elicited by nicotine application. Nicotine 110-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 10037483-3 1999 This study also confirms previous findings of nAChR functional block by fluoxetine (Prozac). Fluoxetine 84-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 10072197-5 1999 Pretreatment with several nAChR ligands (nicotine, cytisine, epibatidine, unlabeled fluoro-A-85380) substantially reduced uptake of the radioligand in the three cerebral areas. Nicotine 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10208315-2 1999 Neuronal nicotinic acetylcholine receptor (nAchR) subunits are expressed in trigeminal primary afferents and could constitute the receptors involved in nicotine perception. Nicotine 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-41 10208315-2 1999 Neuronal nicotinic acetylcholine receptor (nAchR) subunits are expressed in trigeminal primary afferents and could constitute the receptors involved in nicotine perception. Nicotine 152-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 43-48 9927628-2 1999 Several LAs induce subtle changes in the vibrational spectrum of the nAChR over a range of concentrations consistent with their reported nAChR-binding affinities. Lanthanum 8-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 9927628-2 1999 Several LAs induce subtle changes in the vibrational spectrum of the nAChR over a range of concentrations consistent with their reported nAChR-binding affinities. Lanthanum 8-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 9927628-6 1999 Our results suggest that LAs stabilize multiple conformations of the nAChR by binding to at least two conformationally sensitive LA-binding sites. Lanthanum 25-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 10051526-0 1999 Regulation of alpha4beta2 nicotinic receptor desensitization by calcium and protein kinase C. Neuronal nicotinic acetylcholine receptor (nAChR) desensitization is hypothesized to be a trigger for long-term changes in receptor number and function observed after chronic administration of nicotine at levels similar to those found in persons who use tobacco. Nicotine 287-295 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 10072197-5 1999 Pretreatment with several nAChR ligands (nicotine, cytisine, epibatidine, unlabeled fluoro-A-85380) substantially reduced uptake of the radioligand in the three cerebral areas. cytisine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10072197-5 1999 Pretreatment with several nAChR ligands (nicotine, cytisine, epibatidine, unlabeled fluoro-A-85380) substantially reduced uptake of the radioligand in the three cerebral areas. epibatidine 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10072197-5 1999 Pretreatment with several nAChR ligands (nicotine, cytisine, epibatidine, unlabeled fluoro-A-85380) substantially reduced uptake of the radioligand in the three cerebral areas. fluoro-a 84-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 10096514-1 1999 We have previously shown that [18F]norchlorofluoroepibatidine ([18F]NFEP) would be an ideal radiotracer for positron emission tomography (PET) imaging of nicotinic acetylcholine receptors (nAChR); however, its high toxicity is a limiting factor for human studies. [18f]norchlorofluoroepibatidine 30-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-187 9862757-2 1999 The present study establishes the acute functional effects of bupropion, phencyclidine, and ibogaine on two human nAChR subtypes. Bupropion 62-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 9862757-2 1999 The present study establishes the acute functional effects of bupropion, phencyclidine, and ibogaine on two human nAChR subtypes. Phencyclidine 73-86 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 9862757-2 1999 The present study establishes the acute functional effects of bupropion, phencyclidine, and ibogaine on two human nAChR subtypes. Ibogaine 92-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 114-119 10096514-1 1999 We have previously shown that [18F]norchlorofluoroepibatidine ([18F]NFEP) would be an ideal radiotracer for positron emission tomography (PET) imaging of nicotinic acetylcholine receptors (nAChR); however, its high toxicity is a limiting factor for human studies. [18f]norchlorofluoroepibatidine 30-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 9732388-0 1998 Potentiation and inhibition of nicotinic acetylcholine receptors by spermine in the TE671 human muscle cell line. Spermine 68-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 31-64 10022256-2 1998 The use of the alpha7-nAChR-selective agonist choline and of nAChR-subtype-selective antagonists led to the conclusion that these responses can be mediated by alpha7 or alpha4beta2 nAChRs. Choline 46-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 22-27 9863767-8 1998 Human nAChR in SH-SY5Y cells appeared more sensitive to block by physostigmine, PSP and paraoxon, while these AChE inhibitors similarly inhibited nicotinic currents in insect cells and in mouse neuroblastoma cells. Physostigmine 65-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 9863767-8 1998 Human nAChR in SH-SY5Y cells appeared more sensitive to block by physostigmine, PSP and paraoxon, while these AChE inhibitors similarly inhibited nicotinic currents in insect cells and in mouse neuroblastoma cells. phenylsaligenin cyclic phosphate 80-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 9863767-8 1998 Human nAChR in SH-SY5Y cells appeared more sensitive to block by physostigmine, PSP and paraoxon, while these AChE inhibitors similarly inhibited nicotinic currents in insect cells and in mouse neuroblastoma cells. Paraoxon 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 10049129-4 1998 (2) The present experiments investigate the effects of L-NMMA, L-Name, and L-arginine on the nicotinic acetylcholine receptor channel (nAChR) using patch clamp techniques and a piezo-driven application system. omega-N-Methylarginine 55-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 10049129-4 1998 (2) The present experiments investigate the effects of L-NMMA, L-Name, and L-arginine on the nicotinic acetylcholine receptor channel (nAChR) using patch clamp techniques and a piezo-driven application system. NG-Nitroarginine Methyl Ester 63-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 10049129-4 1998 (2) The present experiments investigate the effects of L-NMMA, L-Name, and L-arginine on the nicotinic acetylcholine receptor channel (nAChR) using patch clamp techniques and a piezo-driven application system. Arginine 75-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 140-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-79 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 140-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 157-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-79 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 157-161 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 252-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-79 10049140-1 1998 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded in the absence and presence of the agonist carbamylcholine (Carb) reveals a complex pattern of positive and negative bands that provides a spectral map of Carb-induced structural change. Carbachol 252-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 10049140-4 1998 Spectral variations are also observed that are indicative of both the displacement of the anesthetics from the nAChR upon the addition of Carb and physical interactions that occur between the anesthetics and binding site residues. Carbachol 138-142 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 9784183-2 1998 A nAChR subtype composed of alpha3 and beta4 subunits (alpha3/beta4 subtype), prepared from a stably transfected KXalpha3beta4R2 cell line, has been immobilized in the phospholipid monolayer of an immobilized artificial membrane (IAM) liquid chromatography (LC) stationary phase. Phospholipids 168-180 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 2-7 9778355-0 1998 Secondary structure of the exchange-resistant core from the nicotinic acetylcholine receptor probed directly by infrared spectroscopy and hydrogen/deuterium exchange. Hydrogen 138-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 9778355-0 1998 Secondary structure of the exchange-resistant core from the nicotinic acetylcholine receptor probed directly by infrared spectroscopy and hydrogen/deuterium exchange. Deuterium 147-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 60-92 9778355-1 1998 The spectral changes that occur in infrared spectra recorded as a function of time after exposure of the nicotinic acetylcholine receptor (nAChR) to 2H2O buffer were examined in order to investigate the secondary structure of the transmembrane domain. 2h2o 149-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-137 9778355-1 1998 The spectral changes that occur in infrared spectra recorded as a function of time after exposure of the nicotinic acetylcholine receptor (nAChR) to 2H2O buffer were examined in order to investigate the secondary structure of the transmembrane domain. 2h2o 149-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 9778355-4 1998 Further exposure of the nAChR to 2H2O under conditions of both increasing pH and membrane "fluidity" led to additional exchange of peptide hydrogens for deuterium. 2h2o 33-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 9778355-4 1998 Further exposure of the nAChR to 2H2O under conditions of both increasing pH and membrane "fluidity" led to additional exchange of peptide hydrogens for deuterium. Hydrogen 139-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 9778355-4 1998 Further exposure of the nAChR to 2H2O under conditions of both increasing pH and membrane "fluidity" led to additional exchange of peptide hydrogens for deuterium. Deuterium 153-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 24-29 9778355-5 1998 The greatest degree of peptide 1H/2H exchange (95%) under nondenaturing conditions was found for the nAChR reconstituted into the highly fluid egg phosphatidylcholine membranes lacking cholesterol and anionic lipids at pH 9.0. Hydrogen 31-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 9778355-5 1998 The greatest degree of peptide 1H/2H exchange (95%) under nondenaturing conditions was found for the nAChR reconstituted into the highly fluid egg phosphatidylcholine membranes lacking cholesterol and anionic lipids at pH 9.0. Deuterium 34-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 9778355-5 1998 The greatest degree of peptide 1H/2H exchange (95%) under nondenaturing conditions was found for the nAChR reconstituted into the highly fluid egg phosphatidylcholine membranes lacking cholesterol and anionic lipids at pH 9.0. Phosphatidylcholines 147-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 9778355-5 1998 The greatest degree of peptide 1H/2H exchange (95%) under nondenaturing conditions was found for the nAChR reconstituted into the highly fluid egg phosphatidylcholine membranes lacking cholesterol and anionic lipids at pH 9.0. Cholesterol 185-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 9765366-1 1998 ACh receptors sensitive to nicotine (nAChR) are present in human skin keratinocytes and in bronchial epithelial cells. Nicotine 27-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 9804040-2 1998 Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. 2-fluoro-a 160-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 9736631-6 1998 The synaptic enhancement lasting minutes suggests that nAChR activity can initiate calcium-dependent mechanisms that are known to induce glutamatergic synaptic plasticity. Calcium 83-90 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 9726923-1 1998 The nicotinic acetylcholine receptor (nAChR) is a cation-selective ion channel that opens in response to acetylcholine binding. Acetylcholine 14-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 9726923-6 1998 In particular, for the nAChR the ring of glutamate side chains at the extracellular mouth of the pore is predicted to be largely protonated at neutral pH, whereas those glutamate side chains in the intracellular and intermediate rings (at the opposite mouth of the pore) are predicted to be fully ionized. Glutamic Acid 41-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 9572289-6 1998 The nicotine-induced up-regulation of nAChR binding sites in SH-SY5Y cells was shifted to the right by two orders of magnitude as compared with that in M10 cells. Nicotine 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 9694939-4 1998 nAChRs also are targets of nicotine, which acts acutely like acetylcholine to stimulate nAChR function. Nicotine 27-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 9694939-4 1998 nAChRs also are targets of nicotine, which acts acutely like acetylcholine to stimulate nAChR function. Acetylcholine 61-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 9694939-6 1998 Chronic nicotine treatment induces increases in numbers of human muscle-type nAChRs containing alpha-1, beta-1, gamma and delta subunits, a human ganglionic nAChR subtype containing alpha-3 and beta-4 subunits and a human ganglionic nAChR containing alpha-7 subunits in intracellular and (except for alpha-7 nAChRs) in cell surface pools. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 9694939-6 1998 Chronic nicotine treatment induces increases in numbers of human muscle-type nAChRs containing alpha-1, beta-1, gamma and delta subunits, a human ganglionic nAChR subtype containing alpha-3 and beta-4 subunits and a human ganglionic nAChR containing alpha-7 subunits in intracellular and (except for alpha-7 nAChRs) in cell surface pools. Nicotine 8-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 157-162 9694939-7 1998 However, the half-maximal potency with which nicotine has these effects differs across these nAChR subtypes, as do rates and magnitudes of the "nicotine-induced nAChR up-regulation." Nicotine 45-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 9694939-7 1998 However, the half-maximal potency with which nicotine has these effects differs across these nAChR subtypes, as do rates and magnitudes of the "nicotine-induced nAChR up-regulation." Nicotine 45-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 9694939-7 1998 However, the half-maximal potency with which nicotine has these effects differs across these nAChR subtypes, as do rates and magnitudes of the "nicotine-induced nAChR up-regulation." Nicotine 144-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 9694939-7 1998 However, the half-maximal potency with which nicotine has these effects differs across these nAChR subtypes, as do rates and magnitudes of the "nicotine-induced nAChR up-regulation." Nicotine 144-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 161-166 9694939-9 1998 Nicotine exposure more potently, more rapidly, and with nAChR-subtype specificity, induces two phases of losses in functional responsiveness of muscle-type nAChRs and alpha-3 beta-4 nAChRs, including a "persistent inactivation" that is distinct from classicly defined "desensitization." Nicotine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 9694939-10 1998 Based on these results, we hypothesize that chronic nicotine treatment induces persistent functional inactivation and numerical up-regulation of all nAChR subtypes via distinct post-transcriptional mechanisms and with potencies, at rates and with magnitudes that are nAChR-subtype specific. Nicotine 52-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 9694939-10 1998 Based on these results, we hypothesize that chronic nicotine treatment induces persistent functional inactivation and numerical up-regulation of all nAChR subtypes via distinct post-transcriptional mechanisms and with potencies, at rates and with magnitudes that are nAChR-subtype specific. Nicotine 52-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 267-272 9649579-2 1998 Myasthenia gravis (MG) is a neuromuscular disorder mediated by antibodies directed against the acetylcholine receptor (nAChR) resulting in a functional nAChR loss. Acetylcholine 95-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 119-124 9649579-2 1998 Myasthenia gravis (MG) is a neuromuscular disorder mediated by antibodies directed against the acetylcholine receptor (nAChR) resulting in a functional nAChR loss. Acetylcholine 95-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 152-157 10076528-10 1998 Our findings suggest that NNK may contribute to the genesis of SCLC in smokers via chronic stimulation of the alpha BTX-sensitive nAChR-subtype expressed in these cells. BATRACHOTOXIN 116-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 9580626-2 1998 The discovery of (+/-)-epibatidine, a naturally occurring neuronal nicotinic acetylcholine receptor (nAChR) agonist with antinociceptive activity 200-fold more potent than that of morphine, has renewed interest in the potential role of nAChRs in pain processing. epibatidine 17-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 9703439-1 1998 The effects of carbamate anticholinesterases, pyridostigmine and physostigmine, on the function of the nicotinic receptor (nAChR) in TE671 cells was studied, precluding their inhibition of acetylcholine hydrolysis by carbachol usage. Carbamates 15-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 9571060-10 1998 These structural data are used to interpret the varying nAChR binding of the non-native forms.A model for the binding of native GI(2-7;3-13) to the mammalian nAChR is proposed, with an alpha-subunit binding face made up of Cys2, Asn4, Pro5, Ala6 and Cys7 and a selectivity face, comprised of Arg9 and His10. CYS7 250-254 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 9572289-7 1998 The epibatidine-induced up-regulation of nAChR binding sites in SH-SY5Y cells was one-fourth that in M10 cells. epibatidine 4-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 9580626-3 1998 However, (+/-)-epibatidine has significant side-effect liabilities associated with potent activity at the ganglionic and neuromuscular junction nAChR subtypes which limit its potential as a clinical entity. epibatidine 9-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 144-149 9580626-4 1998 ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine] is a novel, potent cholinergic nAChR ligand with analgesic properties (see accompanying paper by Bannon et al., 1998b) that shows preferential selectivity for neuronal nAChRs and a consequently improved in vivo side-effect profile compared with (+/-)-epibatidine. 5-(2-azetidinylmethoxy)-2-chloropyridine 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 9584223-2 1998 Here, we studied up-regulation of the nAChR composed of alpha4 and beta2 subunits in the M10 cell line by using [3H]epibatidine to measure nAChR in cells in situ and in membrane preparations. Tritium 113-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 9580626-4 1998 ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine] is a novel, potent cholinergic nAChR ligand with analgesic properties (see accompanying paper by Bannon et al., 1998b) that shows preferential selectivity for neuronal nAChRs and a consequently improved in vivo side-effect profile compared with (+/-)-epibatidine. (r)-5-(2-azetidinylmethoxy)-2-chloropyridine 9-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 9580626-8 1998 The S-enantiomer of ABT-594, A-98593 has activity at the neuronal alpha 4 beta 2 nAChR identical with ABT-594 (Ki = 34-39 pM), which demonstrates a lack of stereospecific binding similar to that reported previously for (+/-)-epibatidine. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 9584223-2 1998 Here, we studied up-regulation of the nAChR composed of alpha4 and beta2 subunits in the M10 cell line by using [3H]epibatidine to measure nAChR in cells in situ and in membrane preparations. epibatidine 116-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 9489734-0 1998 Chronic ethanol treatment decreases [3H]epibatidine and [3H]nicotine binding and differentially regulates mRNA levels of nicotinic acetylcholine receptor subunits expressed in M10 and SH-SY5Y neuroblastoma cells. Ethanol 8-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-153 9508836-13 1998 Our findings indicate that the adult-type muscle nAChR (alphabetaepsilondelta) is more permeable to Ca2+ than the fetal-type (alphabetagammadelta), while ganglionic-like alpha3beta4 nAChR is more permeable to Ca2+ than the examined alpha4-containing nAChRs. nachrs 250-256 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 49-54 9676742-2 1998 MPA showed an affinity (Ki = 1.21 nM) which was higher than anatoxin-a > (-)-nicotine > (+)-[R]nornicotine > (-)-[S]nornicotine > and (+)-nicotine, but lower than cytisine (Ki = 0.46 nM) in competing for (-)-[3H]nicotine binding in M10 cells, which stably express the recombinant alpha4beta2 nAChR subtype. Nicotine 80-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 304-309 9489734-5 1998 Chronic treatment for 4 days with 100 mM ethanol significantly decreased the mRNA level for the alpha3 nAChR subunit (-39%), while the mRNA levels for the alpha7 (+30%) and alpha4 (+22%) subunits were significantly increased. Ethanol 41-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 9489734-7 1998 Changes in the levels of nAChR protein and mRNA may have adaptive significance and be involved in the development of dependence, tolerance, and addiction to chronic ethanol and nicotine exposure. Ethanol 165-172 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 9495846-1 1998 The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (+/-)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR) (EC50 = 59 +/- 17 nM; Emax = 110 +/- 09% vs. nicotine). pyridine 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 218-239 9489734-7 1998 Changes in the levels of nAChR protein and mRNA may have adaptive significance and be involved in the development of dependence, tolerance, and addiction to chronic ethanol and nicotine exposure. Nicotine 177-185 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 9495846-1 1998 The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (+/-)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR) (EC50 = 59 +/- 17 nM; Emax = 110 +/- 09% vs. nicotine). pyridine 94-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 9512361-0 1998 Identification of tryptophan 55 as the primary site of [3H]nicotine photoincorporation in the gamma-subunit of the Torpedo nicotinic acetylcholine receptor. Tryptophan 18-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 9495846-1 1998 The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (+/-)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR) (EC50 = 59 +/- 17 nM; Emax = 110 +/- 09% vs. nicotine). 2-(3-pyridinyl)-1-azabicyclo(2.2.2)octane 112-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 218-239 9495846-1 1998 The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (+/-)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR) (EC50 = 59 +/- 17 nM; Emax = 110 +/- 09% vs. nicotine). 2-(3-pyridinyl)-1-azabicyclo(2.2.2)octane 112-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 9537682-2 1998 The present study examined the effects of (-)-nicotine and the novel central nicotinic receptor (nAChR) agonists ABT-418 [(S)-3-methyl-2-pyrrolidinyl)isoxazole] and ABT-089 [2-methyl-3-(2-(S)-pyrrolindinylmethoxy)pyridine dihydrochloride] on the delayed recall accuracy of adult monkeys exposed to distracting stimuli. 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 9495824-1 1998 To extend our knowledge of the pharmacological profile of human alpha4beta2 neuronal nicotinic receptors, we investigated the action of hexamethonium on the major brain human nicotinic acetylcholine receptor (nAChR) stably expressed in human embryonic kidney 293 cells. Hexamethonium 136-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 175-207 9495824-1 1998 To extend our knowledge of the pharmacological profile of human alpha4beta2 neuronal nicotinic receptors, we investigated the action of hexamethonium on the major brain human nicotinic acetylcholine receptor (nAChR) stably expressed in human embryonic kidney 293 cells. Hexamethonium 136-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 209-214 9512361-0 1998 Identification of tryptophan 55 as the primary site of [3H]nicotine photoincorporation in the gamma-subunit of the Torpedo nicotinic acetylcholine receptor. Tritium 56-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 9512361-0 1998 Identification of tryptophan 55 as the primary site of [3H]nicotine photoincorporation in the gamma-subunit of the Torpedo nicotinic acetylcholine receptor. Nicotine 59-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-155 9512361-1 1998 [3H]nicotine has been used as a photoaffinity agonist to identify amino acids within the Torpedo nicotinic acetylcholine receptor (nAChR) gamma-subunit that contributes to the structure of the agonist binding site. Tritium 1-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-129 9512361-1 1998 [3H]nicotine has been used as a photoaffinity agonist to identify amino acids within the Torpedo nicotinic acetylcholine receptor (nAChR) gamma-subunit that contributes to the structure of the agonist binding site. Tritium 1-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 9512361-1 1998 [3H]nicotine has been used as a photoaffinity agonist to identify amino acids within the Torpedo nicotinic acetylcholine receptor (nAChR) gamma-subunit that contributes to the structure of the agonist binding site. Nicotine 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-129 9512361-1 1998 [3H]nicotine has been used as a photoaffinity agonist to identify amino acids within the Torpedo nicotinic acetylcholine receptor (nAChR) gamma-subunit that contributes to the structure of the agonist binding site. Nicotine 4-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 9512361-2 1998 UV irradiation (254 nm) of nAChR-rich membranes equilibrated with [3H]nicotine results in covalent incorporation into alpha- and gamma-subunits that is inhibitable by agonists and competitive antagonists, but not by non-competitive antagonists (Middleton, R.E. Tritium 67-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 9417028-2 1998 A potent (inhibition constant = 37 picomolar) neuronal nicotinic acetylcholine receptor (nAChR) ligand called ABT-594 was developed that has antinociceptive properties equal in efficacy to those of morphine across a series of diverse animal models of acute thermal, persistent chemical, and neuropathic pain states. 5-(2-azetidinylmethoxy)-2-chloropyridine 110-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 9512361-2 1998 UV irradiation (254 nm) of nAChR-rich membranes equilibrated with [3H]nicotine results in covalent incorporation into alpha- and gamma-subunits that is inhibitable by agonists and competitive antagonists, but not by non-competitive antagonists (Middleton, R.E. Nicotine 70-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 9621392-9 1998 The differential sensitivity of these receptors to the nicotinic agonists, cytisine and nicotine, reflects the heterogeneity of the NAchR subtypes involved. cytisine 75-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 9621392-9 1998 The differential sensitivity of these receptors to the nicotinic agonists, cytisine and nicotine, reflects the heterogeneity of the NAchR subtypes involved. Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 9417028-2 1998 A potent (inhibition constant = 37 picomolar) neuronal nicotinic acetylcholine receptor (nAChR) ligand called ABT-594 was developed that has antinociceptive properties equal in efficacy to those of morphine across a series of diverse animal models of acute thermal, persistent chemical, and neuropathic pain states. 5-(2-azetidinylmethoxy)-2-chloropyridine 110-117 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 9486473-6 1998 These data indicate that mecamylamine reduced irritation elicited by nicotine but not capsaicin, and provide further evidence that nicotine oral irritation is mediated via a neuronal nAchR while capsaicin activates trigeminal fibers via a separate molecular receptor. Nicotine 131-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 183-188 9417028-3 1998 These effects were blocked by the nAChR antagonist mecamylamine. Mecamylamine 51-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 9336329-4 1997 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 32-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-156 9585143-3 1998 Examples of NAChR agonists studied are nicotine, SIB-1508Y, SIB-1553A and epibatidine. Nicotine 39-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 9585143-3 1998 Examples of NAChR agonists studied are nicotine, SIB-1508Y, SIB-1553A and epibatidine. epibatidine 74-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 12-17 9585143-9 1998 The discovery of subtype-selective NAChR agonists such as SIB-1508Y and SIB-1553A provides a new class of neuropsychopharmacological agents with better therapeutic ratios than nonspecific agents such as nicotine. Nicotine 203-211 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 9374343-4 1997 In this study, the distribution and kinetics of [(+/-)-exo-2-(2-[18F] fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane (18F-FPH), a high-affinity nAChR agonist, was evaluated in a baboon using PET. [(+/-)-exo-2-(2-[18f] fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane 48-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 9374343-4 1997 In this study, the distribution and kinetics of [(+/-)-exo-2-(2-[18F] fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane (18F-FPH), a high-affinity nAChR agonist, was evaluated in a baboon using PET. 18f-fph 116-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 142-147 9407073-0 1997 Identification of amino acids contributing to high and low affinity d-tubocurarine sites in the Torpedo nicotinic acetylcholine receptor. Tubocurarine 68-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-136 9407073-1 1997 d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM). Tubocurarine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-103 9407073-1 1997 d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM). Tubocurarine 0-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9407073-1 1997 d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM). Tubocurarine 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-103 9407073-1 1997 d-Tubocurarine (dTC) is a potent competitive antagonist of the Torpedo nicotinic acetylcholine receptor (nAChR) that binds non-equivalently to the two agonist sites (Kd values of 30 nM and 8 microM). Tubocurarine 16-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9407073-2 1997 When nAChR-rich membranes equilibrated with [3H]dTC are irradiated with 254 nm UV light, [3H]dTC is covalently incorporated into the alpha-, gamma-, and delta-subunits in a concentration-dependent and agonist-inhibitable manner, consistent with the localization of the high and low affinity dTC binding sites at the alpha-gamma- and alpha-delta-subunit interfaces, respectively (Pedersen, S. E. and Cohen, J. Tritium 45-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 9407073-2 1997 When nAChR-rich membranes equilibrated with [3H]dTC are irradiated with 254 nm UV light, [3H]dTC is covalently incorporated into the alpha-, gamma-, and delta-subunits in a concentration-dependent and agonist-inhibitable manner, consistent with the localization of the high and low affinity dTC binding sites at the alpha-gamma- and alpha-delta-subunit interfaces, respectively (Pedersen, S. E. and Cohen, J. Tubocurarine 48-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 9407073-2 1997 When nAChR-rich membranes equilibrated with [3H]dTC are irradiated with 254 nm UV light, [3H]dTC is covalently incorporated into the alpha-, gamma-, and delta-subunits in a concentration-dependent and agonist-inhibitable manner, consistent with the localization of the high and low affinity dTC binding sites at the alpha-gamma- and alpha-delta-subunit interfaces, respectively (Pedersen, S. E. and Cohen, J. Tritium 90-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 9407073-2 1997 When nAChR-rich membranes equilibrated with [3H]dTC are irradiated with 254 nm UV light, [3H]dTC is covalently incorporated into the alpha-, gamma-, and delta-subunits in a concentration-dependent and agonist-inhibitable manner, consistent with the localization of the high and low affinity dTC binding sites at the alpha-gamma- and alpha-delta-subunit interfaces, respectively (Pedersen, S. E. and Cohen, J. Tubocurarine 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 9407073-2 1997 When nAChR-rich membranes equilibrated with [3H]dTC are irradiated with 254 nm UV light, [3H]dTC is covalently incorporated into the alpha-, gamma-, and delta-subunits in a concentration-dependent and agonist-inhibitable manner, consistent with the localization of the high and low affinity dTC binding sites at the alpha-gamma- and alpha-delta-subunit interfaces, respectively (Pedersen, S. E. and Cohen, J. Tubocurarine 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 9407073-11 1997 Subunits isolated from nAChR-rich membranes photolabeled with [3H]dTC were subjected to enzymatic digestion, and peptides containing 3H were isolated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and/or reversed-phase high performance liquid chromatography. [3h]dtc 62-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 9407073-11 1997 Subunits isolated from nAChR-rich membranes photolabeled with [3H]dTC were subjected to enzymatic digestion, and peptides containing 3H were isolated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and/or reversed-phase high performance liquid chromatography. Tritium 63-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 9407073-18 1997 This pattern of conservation may indicate a functional significance for tryptophan at that location in all nAChR agonist sites. Tryptophan 72-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 9353587-5 1997 Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively. Vincristine 37-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9353587-5 1997 Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively. tubulazole 50-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9353587-5 1997 Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively. Podophyllotoxin 62-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9353587-5 1997 Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively. Demecolcine 83-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9353587-5 1997 Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively. Catecholamines 122-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 9336329-4 1997 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 32-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 323-328 9336329-4 1997 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. cytisine 98-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-156 9336329-4 1997 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. cytisine 98-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 323-328 9336329-5 1997 In cation flux and channel current studies, ABT-089 displayed a more complex profile than (-)-nicotine having agonist, partial agonist and inhibitory activities depending on the nAChR subtype with which it interacts. pozanicline 44-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 9336329-5 1997 In cation flux and channel current studies, ABT-089 displayed a more complex profile than (-)-nicotine having agonist, partial agonist and inhibitory activities depending on the nAChR subtype with which it interacts. Nicotine 90-102 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 9336329-9 1997 The differential full agonist/partial agonist profile of ABT-089, as compared with (-)-nicotine and ABT-418, illustrates the complexity of nAChR activation and the potential to target responses at subclasses of the neuronal and peripheral receptors. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 57-60 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 139-144 20654340-6 1997 The nature of the effect of the heavy metal Pb(2+) depends on the combination of mammalian neuronal a and beta nAChR subunits. metal pb 38-46 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 111-116 9344890-8 1997 The data suggest that in addition to inhibition of acetylcholinesterase, these OPs bind to a site on the nAChR that is different from the sites that bind ACh or TCP and that this binding induces nAChR desensitization. Acetylcholine 106-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 9344890-8 1997 The data suggest that in addition to inhibition of acetylcholinesterase, these OPs bind to a site on the nAChR that is different from the sites that bind ACh or TCP and that this binding induces nAChR desensitization. N-(3,4,5-trichlorophenyl)succinimide 161-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 20654340-7 1997 Ion currents mediated by alpha4beta2 and alpha3beta4 nAChR are inhibited and those mediated by alpha3beta2 nAChR are potentiated by Pb(2+). Lead 132-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 9284304-0 1997 Molecular dynamics study of water and Na+ ions in models of the pore region of the nicotinic acetylcholine receptor. Water 28-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-115 9387186-7 1997 The function of the nAChR channels expressed by BEC was demonstrated by biphasic increase in the concentrations of intracellular calcium ([Ca++]i) in response to activation of the channel by Nic and fluctuations of [Ca++]i due to channel blockade by mecamylamine (Mec). Calcium 129-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 9282914-2 1997 The cellular events underlying the antinociceptive effects of (+/-)-epibatidine, a nicotinic acetylcholine receptor (nAChR) ligand that is 200-fold more potent than morphine, is unknown. epibatidine 62-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 83-115 9282914-2 1997 The cellular events underlying the antinociceptive effects of (+/-)-epibatidine, a nicotinic acetylcholine receptor (nAChR) ligand that is 200-fold more potent than morphine, is unknown. epibatidine 62-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 117-122 9282914-5 1997 The noncompetitive nAChR antagonist mecamylamine potently antagonized (-)-nicotine-evoked ion flux, whereas the competitive antagonist dihydro-beta-erythroidine was a weak antagonist, giving support to an alpha3beta4 nAChR subtype. Mecamylamine 36-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 9282914-5 1997 The noncompetitive nAChR antagonist mecamylamine potently antagonized (-)-nicotine-evoked ion flux, whereas the competitive antagonist dihydro-beta-erythroidine was a weak antagonist, giving support to an alpha3beta4 nAChR subtype. Nicotine 70-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 19-24 9282914-5 1997 The noncompetitive nAChR antagonist mecamylamine potently antagonized (-)-nicotine-evoked ion flux, whereas the competitive antagonist dihydro-beta-erythroidine was a weak antagonist, giving support to an alpha3beta4 nAChR subtype. Nicotine 70-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 217-222 9282914-7 1997 Furthermore, prolonged exposure to (+/-)-epibatidine desensitized the functional response of the nAChR in this cell line (IC50 = 12 +/- 9 nM). epibatidine 35-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-102 9281615-2 1997 In this study, the regulation of recombinant human alpha4beta2 nAChR subtype by (-)-nicotine and other cholinergic channel modulators was studied using human embryonic kidney 293 cells stably expressing this subunit combination. Nicotine 80-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 9281615-10 1997 Both 6-beta-[beta"(piperidino)propionyl]forskolin and phorbol-12-myristate-13-acetate increased [3H]cytisine binding sites and nAChR function and enhanced the effects of chronic (-)-nicotine treatment in a synergistic manner. 6-beta-[beta"(piperidino)propionyl]forskolin 5-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 9281615-10 1997 Both 6-beta-[beta"(piperidino)propionyl]forskolin and phorbol-12-myristate-13-acetate increased [3H]cytisine binding sites and nAChR function and enhanced the effects of chronic (-)-nicotine treatment in a synergistic manner. Tetradecanoylphorbol Acetate 54-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 9387186-7 1997 The function of the nAChR channels expressed by BEC was demonstrated by biphasic increase in the concentrations of intracellular calcium ([Ca++]i) in response to activation of the channel by Nic and fluctuations of [Ca++]i due to channel blockade by mecamylamine (Mec). Mecamylamine 250-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 9387186-7 1997 The function of the nAChR channels expressed by BEC was demonstrated by biphasic increase in the concentrations of intracellular calcium ([Ca++]i) in response to activation of the channel by Nic and fluctuations of [Ca++]i due to channel blockade by mecamylamine (Mec). Mecamylamine 264-267 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 9387186-10 1997 An over exposure of BEC to Nic, however, produced an antagonist-like effect, suggesting that the pathobiological effects of Nic toxicity might result from both activation of nAChR channels and nAChR desensitization. Nicotine 27-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-179 9387186-10 1997 An over exposure of BEC to Nic, however, produced an antagonist-like effect, suggesting that the pathobiological effects of Nic toxicity might result from both activation of nAChR channels and nAChR desensitization. Nicotine 27-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 193-198 9387186-12 1997 We believe that outside the neural system Nic interferes with functioning of non-neuronal cholinergic networks by displacing from nAChR its natural ligand acetylcholine which acts as a local hormone or cytokine in a variety of non-neuronal locations. Acetylcholine 155-168 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 9189657-12 1997 The expression of multiple nAChR subtypes may allow for precise control of neurotransmission mediated by acetylcholine in diverse populations of neurons. Acetylcholine 105-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-32 9221782-1 1997 We show that three of the eleven genes of the nematode Caenorhabditis elegans that mediate resistance to the nematocide levamisole and to other cholinergic agonists encode nicotinic acetylcholine receptor (nAChR) subunits. Levamisole 120-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 206-211 9221782-4 1997 Expression in Xenopus oocytes of combinations of these subunits that include the unc-38 alpha subunit results in levamisole-induced currents that are suppressed by the nAChR antagonists mecamylamine, neosurugatoxin, and d-tubocurarine but not alpha-bungarotoxin. Levamisole 113-123 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 9221782-4 1997 Expression in Xenopus oocytes of combinations of these subunits that include the unc-38 alpha subunit results in levamisole-induced currents that are suppressed by the nAChR antagonists mecamylamine, neosurugatoxin, and d-tubocurarine but not alpha-bungarotoxin. Mecamylamine 186-198 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 9221782-4 1997 Expression in Xenopus oocytes of combinations of these subunits that include the unc-38 alpha subunit results in levamisole-induced currents that are suppressed by the nAChR antagonists mecamylamine, neosurugatoxin, and d-tubocurarine but not alpha-bungarotoxin. Tubocurarine 220-234 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 168-173 9223339-3 1997 Here we show that 3,3"-dimethyl suberimidate (DMS) is an agonistic bifunctional cross-linking reagent, which irreversibly "freezes" the nAChR in a high agonist affinity/closed-channel state. 3,3"-dimethyl suberimidate 18-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 9223339-3 1997 Here we show that 3,3"-dimethyl suberimidate (DMS) is an agonistic bifunctional cross-linking reagent, which irreversibly "freezes" the nAChR in a high agonist affinity/closed-channel state. dms 46-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 136-141 9132013-1 1997 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded using the attenuated total reflectance technique in the presence and absence of carbamylcholine exhibits a complex pattern of positive and negative bands that provides a spectral map of the structural changes that occur in the nAChR upon agonist binding and subsequent desensitization. Carbachol 177-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 9132013-1 1997 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded using the attenuated total reflectance technique in the presence and absence of carbamylcholine exhibits a complex pattern of positive and negative bands that provides a spectral map of the structural changes that occur in the nAChR upon agonist binding and subsequent desensitization. Carbachol 177-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 324-329 9132013-1 1997 The difference between infrared spectra of the nicotinic acetylcholine receptor (nAChR) recorded using the attenuated total reflectance technique in the presence and absence of carbamylcholine exhibits a complex pattern of positive and negative bands that provides a spectral map of the structural changes that occur in the nAChR upon agonist binding and subsequent desensitization. Carbachol 177-192 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-79 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 31-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 245-250 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 108-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 108-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 245-250 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. Amides 130-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. Amides 130-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 245-250 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 108-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 9132013-5 1997 Difference spectra recorded in 2H2O buffer within either minutes or hours of prior exposure of the nAChR to 2H2O exhibit the same amide I difference band shifts that are observed in difference spectra recorded after 3 days prior exposure of the nAChR to 2H2O. 2h2o 108-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 245-250 9104590-2 1997 For all nAChRs examined (chick and rat alpha 3 beta 4, chick alpha 3 beta 2, alpha 4 beta 2, alpha 7 and alpha 8), expression levels were high enough to allow measurements of acetylcholine-evoked whole-cell currents and nicotine-elicited Ca2+ transients as well as the functional characterization of nAChR channels. Acetylcholine 175-188 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 8-13 9104590-2 1997 For all nAChRs examined (chick and rat alpha 3 beta 4, chick alpha 3 beta 2, alpha 4 beta 2, alpha 7 and alpha 8), expression levels were high enough to allow measurements of acetylcholine-evoked whole-cell currents and nicotine-elicited Ca2+ transients as well as the functional characterization of nAChR channels. Nicotine 220-228 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 8-13 9104590-3 1997 Unitary acetylcholine-evoked events of alpha 8 nAChR had a slope conductance of 23 pS, whereas two conductance classes (19-23 and 32-45 pS) were identified for all other nAChR channels. Acetylcholine 8-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 8987816-4 1996 The rank order of potency of four nAChR ligands to activate human alpha4beta2 receptors is (-)-nicotine > ACh > (-)-cytisine > ABT-418. Nicotine 91-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 9022806-0 1997 Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties. pozanicline 30-76 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 9022806-0 1997 Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties. pozanicline 78-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 9022806-0 1997 Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties. 3-Pyridyl ether 111-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-159 9022806-1 1997 2-Methyl-3-(2(S)-pyrrolidinylmethoxy)pyridine, ABT-089 (S-4), a member of the 3-pyridyl ether class of nicotinic acetylcholine receptor (nAChR) ligands, shows positive effects in rodent and primate models of cognitive enhancement and a rodent model of anxiolytic activity and possesses a reduced propensity to activate peripheral ganglionic type receptors. pozanicline 0-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 9022806-1 1997 2-Methyl-3-(2(S)-pyrrolidinylmethoxy)pyridine, ABT-089 (S-4), a member of the 3-pyridyl ether class of nicotinic acetylcholine receptor (nAChR) ligands, shows positive effects in rodent and primate models of cognitive enhancement and a rodent model of anxiolytic activity and possesses a reduced propensity to activate peripheral ganglionic type receptors. pozanicline 0-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 9022806-1 1997 2-Methyl-3-(2(S)-pyrrolidinylmethoxy)pyridine, ABT-089 (S-4), a member of the 3-pyridyl ether class of nicotinic acetylcholine receptor (nAChR) ligands, shows positive effects in rodent and primate models of cognitive enhancement and a rodent model of anxiolytic activity and possesses a reduced propensity to activate peripheral ganglionic type receptors. 3-Pyridyl ether 78-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-135 9022806-1 1997 2-Methyl-3-(2(S)-pyrrolidinylmethoxy)pyridine, ABT-089 (S-4), a member of the 3-pyridyl ether class of nicotinic acetylcholine receptor (nAChR) ligands, shows positive effects in rodent and primate models of cognitive enhancement and a rodent model of anxiolytic activity and possesses a reduced propensity to activate peripheral ganglionic type receptors. 3-Pyridyl ether 78-93 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 137-142 8987816-4 1996 The rank order of potency of four nAChR ligands to activate human alpha4beta2 receptors is (-)-nicotine > ACh > (-)-cytisine > ABT-418. cytisine 118-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 8987816-4 1996 The rank order of potency of four nAChR ligands to activate human alpha4beta2 receptors is (-)-nicotine > ACh > (-)-cytisine > ABT-418. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 136-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 8987816-6 1996 Coapplication of 1 microM ACh with known nAChR inhibitors such as dihydro-beta-erythroidine and methyllycaconitine reversibly reduces the current evoked by the agonist with respective IC50 values of 80 nM and 1.5 microM. Acetylcholine 26-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 8987816-6 1996 Coapplication of 1 microM ACh with known nAChR inhibitors such as dihydro-beta-erythroidine and methyllycaconitine reversibly reduces the current evoked by the agonist with respective IC50 values of 80 nM and 1.5 microM. Dihydro-beta-Erythroidine 66-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 8987816-6 1996 Coapplication of 1 microM ACh with known nAChR inhibitors such as dihydro-beta-erythroidine and methyllycaconitine reversibly reduces the current evoked by the agonist with respective IC50 values of 80 nM and 1.5 microM. methyllycaconitine 96-114 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 9007339-0 1996 Dinucleotide polymorphism in the first intron of the human neuronal nicotinic acetylcholine receptor alpha 4 subunit gene (CHRNA4). Dinucleoside Phosphates 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-129 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-111 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 257-262 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-111 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 113-118 8941400-1 1996 Methyllycaconitine (MLA, 1) is a novel, potent probe for mammalian and insect nicotinic acetylcholine receptors (nAChR) and displays remarkable selectivity toward neuronal [125I]-alpha-bungarotoxin (alpha BgTX) binding sites that correspond to alpha 7-type nAChR in mammalian brain. methyllycaconitine 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 257-262 8941400-5 1996 This study therefore extends the range of norditerpenoids, other than MLA, which can be used to probe this important class of nAChR. Diterpenes 42-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 126-131 8941400-6 1996 All 12 alkaloids were assessed for activity at [3H]nicotine binding sites which are considered to represent alpha 4 beta 2 nAChR. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 8831330-1 1996 Single channel recordings have shown that ketamine (Ket) decreases the open time of the nicotinic acetylcholine receptor channel (nAChR). Ketamine 42-50 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 8831330-1 1996 Single channel recordings have shown that ketamine (Ket) decreases the open time of the nicotinic acetylcholine receptor channel (nAChR). Ketamine 52-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 8923487-3 1996 Acute exposure to SP inhibits carbamylcholine- or nicotine-stimulated function measured using 86Rb+ efflux assays of human ganglionic (alpha 3 beta 4) nAChR expressed in SH-SY5Y neuroblastoma cells (IC50 approximately 2.3 microM) or of human muscle-type (alpha 1 beta 1 gamma delta) nAChR expressed in TE671/RD clonal cells (IC50 approximately 21 microM). Carbachol 30-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-156 8923487-3 1996 Acute exposure to SP inhibits carbamylcholine- or nicotine-stimulated function measured using 86Rb+ efflux assays of human ganglionic (alpha 3 beta 4) nAChR expressed in SH-SY5Y neuroblastoma cells (IC50 approximately 2.3 microM) or of human muscle-type (alpha 1 beta 1 gamma delta) nAChR expressed in TE671/RD clonal cells (IC50 approximately 21 microM). Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-156 8923487-3 1996 Acute exposure to SP inhibits carbamylcholine- or nicotine-stimulated function measured using 86Rb+ efflux assays of human ganglionic (alpha 3 beta 4) nAChR expressed in SH-SY5Y neuroblastoma cells (IC50 approximately 2.3 microM) or of human muscle-type (alpha 1 beta 1 gamma delta) nAChR expressed in TE671/RD clonal cells (IC50 approximately 21 microM). Nicotine 50-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 283-288 8738758-3 1996 In this study we use Northern blot analysis, double-label immunocytochemistry, and single cell RNA analysis using polymerase chain reaction to show that RA-treated P19 cells with neuronal-like morphology also express neuronal nicotinic acetylcholine receptor (nAChR) subunits alpha 3, alpha 4, and beta 2. Tretinoin 153-155 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 260-265 8752117-2 1996 The present study tests whether nAChR are potential targets for steroids. Steroids 64-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 8752117-3 1996 Acute or short-term (5 min) preexposure to steroids such as progesterone (which acts most potently), estradiol, corticosterone, or dexamethasone inhibits function of human muscle-type (alpha 1 beta 1 gamma delta) or ganglionic (alpha 3 beta 4) nAChR measured using 86Rb+ efflux assays in TE671/RD clonal or SH-SY5Y neuroblastoma cells. Steroids 43-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 244-249 8752117-3 1996 Acute or short-term (5 min) preexposure to steroids such as progesterone (which acts most potently), estradiol, corticosterone, or dexamethasone inhibits function of human muscle-type (alpha 1 beta 1 gamma delta) or ganglionic (alpha 3 beta 4) nAChR measured using 86Rb+ efflux assays in TE671/RD clonal or SH-SY5Y neuroblastoma cells. Progesterone 60-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 244-249 8752117-3 1996 Acute or short-term (5 min) preexposure to steroids such as progesterone (which acts most potently), estradiol, corticosterone, or dexamethasone inhibits function of human muscle-type (alpha 1 beta 1 gamma delta) or ganglionic (alpha 3 beta 4) nAChR measured using 86Rb+ efflux assays in TE671/RD clonal or SH-SY5Y neuroblastoma cells. Estradiol 101-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 244-249 8752117-3 1996 Acute or short-term (5 min) preexposure to steroids such as progesterone (which acts most potently), estradiol, corticosterone, or dexamethasone inhibits function of human muscle-type (alpha 1 beta 1 gamma delta) or ganglionic (alpha 3 beta 4) nAChR measured using 86Rb+ efflux assays in TE671/RD clonal or SH-SY5Y neuroblastoma cells. Dexamethasone 131-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 244-249 8752117-4 1996 Absolute (high nanomolar to intermediate micromolar range) and rank-order potencies for steroid-mediated functional inhibition are similar across nAChR subtypes but differ for some steroid derivatives. Steroids 88-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 146-151 8752117-6 1996 Steroid-mediated blockade of nAChR function is insurmountable by increasing agonist concentrations, and cell-impermeant progesterone:bovine serum albumin conjugates have full potency as inhibitors of ganglionic or muscle-type nAChR function. Steroids 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 29-34 8752117-6 1996 Steroid-mediated blockade of nAChR function is insurmountable by increasing agonist concentrations, and cell-impermeant progesterone:bovine serum albumin conjugates have full potency as inhibitors of ganglionic or muscle-type nAChR function. Steroids 0-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 226-231 8752117-6 1996 Steroid-mediated blockade of nAChR function is insurmountable by increasing agonist concentrations, and cell-impermeant progesterone:bovine serum albumin conjugates have full potency as inhibitors of ganglionic or muscle-type nAChR function. Progesterone 120-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 226-231 8752117-7 1996 Chronic (48 h) exposure to progesterone or estradiol, but not the other steroids, also produces blockade of nAChR function, without significant effects on numbers of nAChR radioligand-binding sites. Progesterone 27-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 8752117-7 1996 Chronic (48 h) exposure to progesterone or estradiol, but not the other steroids, also produces blockade of nAChR function, without significant effects on numbers of nAChR radioligand-binding sites. Estradiol 43-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 8752117-8 1996 Collectively, these results suggest that steroids act noncompetitively at extracellular sites to inhibit nAChR function with unique potencies for different steroid-nAChR subtype combinations. Steroids 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 8752117-8 1996 Collectively, these results suggest that steroids act noncompetitively at extracellular sites to inhibit nAChR function with unique potencies for different steroid-nAChR subtype combinations. Steroids 41-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 8752117-8 1996 Collectively, these results suggest that steroids act noncompetitively at extracellular sites to inhibit nAChR function with unique potencies for different steroid-nAChR subtype combinations. Steroids 41-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 8752117-8 1996 Collectively, these results suggest that steroids act noncompetitively at extracellular sites to inhibit nAChR function with unique potencies for different steroid-nAChR subtype combinations. Steroids 41-48 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 8752117-9 1996 Thus, nAChR could be among the targets mediating physiologically relevant effects of steroid action in the nervous system. Steroids 85-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-11 8738758-4 1996 Greater than 80% of RA-treated P19 cells with a neuronal-like phenotype express nAChR alpha 4 subunit transcripts and both alpha 4 and beta 2 protein. Tretinoin 20-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 8738758-7 1996 The appearance of nAChR subunits also coincides with RA-induced expression of high affinity [3H]-nicotine binding receptors. Tretinoin 53-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 8738758-7 1996 The appearance of nAChR subunits also coincides with RA-induced expression of high affinity [3H]-nicotine binding receptors. Tritium 93-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 8887981-9 1996 Thus, A-85380 displays a profile of robust activation of a number of nAChR subtypes with substantially less affinity for [125I] alpha-BgT sites than [3H](-)-cytisine sites, suggesting that it may serve as a more selective pharmacologic probe for the alpha 4 beta 2 subtype relative to the alpha 7 and alpha 1 beta 1 delta g nAChRs than (+/-)-epibatidine. Tritium 150-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 8789148-1 1996 We report here the preparative scale isolation of the four subunits of the nicotinic acetylcholine receptor (nAChR) applying short inverse pore gradient SDS gels on an elution-PAGE apparatus. Sodium Dodecyl Sulfate 153-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-107 8610122-1 1996 To determine inhalational anesthetic binding domains on a ligand-gated ion channel, I used halothane direct photoaffinity labeling of the nicotinic acetylcholine receptor (nAChR) in native Torpedo membranes. Halothane 91-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-170 8610122-1 1996 To determine inhalational anesthetic binding domains on a ligand-gated ion channel, I used halothane direct photoaffinity labeling of the nicotinic acetylcholine receptor (nAChR) in native Torpedo membranes. Halothane 91-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 8610122-2 1996 [14C]Halothane photoaffinity labeling of both the native Torpedo membranes and the isolated nAChR was saturable, with Kd values within the clinically relevant range. Carbon-14 1-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 8610122-2 1996 [14C]Halothane photoaffinity labeling of both the native Torpedo membranes and the isolated nAChR was saturable, with Kd values within the clinically relevant range. Halothane 5-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 92-97 8610122-5 1996 Within the alpha-subunit, greater than 90% of label was found in the endoprotease Glu-C digestion fragments which contain the four transmembrane regions, and the pattern was different from that reported for photoactivatable phospholipid binding to the nAChR. Phospholipids 224-236 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 252-257 8610122-6 1996 Unlabeled halothane reduced labeling more than did isoflurane, suggesting differences in the binding domains for inhalational anesthetics in the nAChR. Halothane 10-19 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 8610122-6 1996 Unlabeled halothane reduced labeling more than did isoflurane, suggesting differences in the binding domains for inhalational anesthetics in the nAChR. Isoflurane 51-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 8610122-7 1996 These data suggest multiple similar binding domains for halothane in the transmembrane region of the nAChR. Halothane 56-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 101-106 8789148-1 1996 We report here the preparative scale isolation of the four subunits of the nicotinic acetylcholine receptor (nAChR) applying short inverse pore gradient SDS gels on an elution-PAGE apparatus. Sodium Dodecyl Sulfate 153-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 8558445-1 1996 (-)-Nicotine, the prototypical agonist for neuronal nicotinic acetylcholine receptors (nAChR) has been shown to bind with high affinity to the rodent and avian alpha 4 beta 2 nAChR subtype. Nicotine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-85 8558445-12 1996 These results demonstrate that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 beta 2 nAChR. Tritium 155-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 8558445-1 1996 (-)-Nicotine, the prototypical agonist for neuronal nicotinic acetylcholine receptors (nAChR) has been shown to bind with high affinity to the rodent and avian alpha 4 beta 2 nAChR subtype. Nicotine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 87-92 8558445-12 1996 These results demonstrate that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 beta 2 nAChR. Tritium 155-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 338-343 8558445-1 1996 (-)-Nicotine, the prototypical agonist for neuronal nicotinic acetylcholine receptors (nAChR) has been shown to bind with high affinity to the rodent and avian alpha 4 beta 2 nAChR subtype. Nicotine 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 175-180 8558445-12 1996 These results demonstrate that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 beta 2 nAChR. cytisine 158-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 77-82 7578128-1 1995 FTIR spectra have been recorded both as a function of time and after prolonged exposure to 2H2O buffer in order to study the structural changes that lead to both the ligand- and lipid-dependent channel-inactive states of the nicotinic acetylcholine receptor (nAChR). 2h2o 91-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 225-257 8558445-12 1996 These results demonstrate that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 beta 2 nAChR. cytisine 158-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 338-343 8788942-15 1995 The rate of myoblast fusion was increased by carbachol, an effect antagonized by alpha-bungarotoxin, curare and decamethonium, but not by atropine, indicating that nAChR were involved. Carbachol 45-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 164-169 8747166-1 1995 Subtypes of nicotinic acetylcholine receptors (nAChRs) were characterized in human temporal cortex and in a alpha 4 beta 2 nAChR-transfected M10 cell line using the nicotinic agonists epibatidine, ABT 418 and (-)nicotine in competition studies with [3H]nicotine and [3H]cytisine. Acetylcholine 22-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 47-52 7493938-0 1995 Fourier transform infrared and hydrogen/deuterium exchange reveal an exchange-resistant core of alpha-helical peptide hydrogens in the nicotinic acetylcholine receptor. Hydrogen 31-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-167 7493938-0 1995 Fourier transform infrared and hydrogen/deuterium exchange reveal an exchange-resistant core of alpha-helical peptide hydrogens in the nicotinic acetylcholine receptor. Deuterium 40-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-167 7493938-0 1995 Fourier transform infrared and hydrogen/deuterium exchange reveal an exchange-resistant core of alpha-helical peptide hydrogens in the nicotinic acetylcholine receptor. Hydrogen 118-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-167 7493938-1 1995 The structure of the nicotinic acetylcholine receptor (nAChR) has been studied using a novel combination of hydrogen/deuterium exchange and attenuated total reflectance Fourier transform infrared spectroscopy. Hydrogen 108-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 7493938-1 1995 The structure of the nicotinic acetylcholine receptor (nAChR) has been studied using a novel combination of hydrogen/deuterium exchange and attenuated total reflectance Fourier transform infrared spectroscopy. Hydrogen 108-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 7493938-1 1995 The structure of the nicotinic acetylcholine receptor (nAChR) has been studied using a novel combination of hydrogen/deuterium exchange and attenuated total reflectance Fourier transform infrared spectroscopy. Deuterium 117-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-53 7493938-1 1995 The structure of the nicotinic acetylcholine receptor (nAChR) has been studied using a novel combination of hydrogen/deuterium exchange and attenuated total reflectance Fourier transform infrared spectroscopy. Deuterium 117-126 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 7493938-2 1995 Fourier transform infrared spectra show marked changes in both the amide I and amide II bands upon exposure of the nAChR to 2H2O. Amides 67-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 7493938-2 1995 Fourier transform infrared spectra show marked changes in both the amide I and amide II bands upon exposure of the nAChR to 2H2O. Amides 79-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 7493938-2 1995 Fourier transform infrared spectra show marked changes in both the amide I and amide II bands upon exposure of the nAChR to 2H2O. 2h2o 124-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 115-120 7493938-4 1995 The 30% of peptide hydrogens that exchange within seconds is highly exposed to solvent and likely involved in random and turn conformations, whereas the 25% of exchange-resistant peptide hydrogens is relatively inaccessible to solvent and likely located in the transmembrane domains of the nAChR. Hydrogen 187-196 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 290-295 7493938-5 1995 Marked changes occur in the amide I contour within seconds of exposure of the nAChR to 2H2O as a result of relatively large downshifts in the frequencies of amide I component bands assigned to turns and random structures. Amides 28-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 7493938-5 1995 Marked changes occur in the amide I contour within seconds of exposure of the nAChR to 2H2O as a result of relatively large downshifts in the frequencies of amide I component bands assigned to turns and random structures. 2h2o 87-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 7493938-5 1995 Marked changes occur in the amide I contour within seconds of exposure of the nAChR to 2H2O as a result of relatively large downshifts in the frequencies of amide I component bands assigned to turns and random structures. Amides 157-162 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 7493938-7 1995 It is demonstrated that the time courses and relative magnitudes of the amide I component band shifts can be used both as an aid in the assignment of component bands to specific secondary structures and as a probe of the exchange rates of different types of secondary structures in the nAChR. Amides 72-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 286-291 8531111-0 1995 The "calcium antagonist" TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester] is a potent, non-competitive, functional antagonist at diverse nicotinic acetylcholine receptor subtypes. Calcium 5-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-185 8531111-0 1995 The "calcium antagonist" TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester] is a potent, non-competitive, functional antagonist at diverse nicotinic acetylcholine receptor subtypes. tmb-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester 25-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 153-185 8531111-2 1995 However, this study shows that TMB-8 acts as a noncompetitive, functional antagonist at diverse nicotinic acetylcholine receptor (nAChR) subtypes with potencies that exceed those for other reported effects of TMB-8, including inhibition of intracellular Ca2+ mobilization. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 31-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-128 8531111-2 1995 However, this study shows that TMB-8 acts as a noncompetitive, functional antagonist at diverse nicotinic acetylcholine receptor (nAChR) subtypes with potencies that exceed those for other reported effects of TMB-8, including inhibition of intracellular Ca2+ mobilization. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 31-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 130-135 8531111-3 1995 TMB-8 is a potent inhibitor (IC50 approximately 400 nM) of agonist-stimulated ion flux mediated by functional human muscle nAChR or ganglionic alpha 3 beta 4-nAChR subtypes expressed by TE671/RD or SH-SY5Y cells. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 8531111-3 1995 TMB-8 is a potent inhibitor (IC50 approximately 400 nM) of agonist-stimulated ion flux mediated by functional human muscle nAChR or ganglionic alpha 3 beta 4-nAChR subtypes expressed by TE671/RD or SH-SY5Y cells. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 158-163 8531111-5 1995 TMB-8 is much less potent (IC50 approximately 30-200 microM) as an inhibitor of high-affinity 3H-labeled acetylcholine or 125I-labeled alpha-bungarotoxin binding to human muscle nAChR, ganglionic alpha 3 beta 4-nAChR, or ganglionic alpha 7-nAChR subtypes. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 178-183 8531111-5 1995 TMB-8 is much less potent (IC50 approximately 30-200 microM) as an inhibitor of high-affinity 3H-labeled acetylcholine or 125I-labeled alpha-bungarotoxin binding to human muscle nAChR, ganglionic alpha 3 beta 4-nAChR, or ganglionic alpha 7-nAChR subtypes. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 211-216 8531111-5 1995 TMB-8 is much less potent (IC50 approximately 30-200 microM) as an inhibitor of high-affinity 3H-labeled acetylcholine or 125I-labeled alpha-bungarotoxin binding to human muscle nAChR, ganglionic alpha 3 beta 4-nAChR, or ganglionic alpha 7-nAChR subtypes. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 211-216 8531111-6 1995 Moreover, functional inhibition by TMB-8 of muscle-type nAChR is due to a reduction in agonist efficacy, but not potency, and is proportionately stronger with increasing agonist concentration, thereby suggesting that TMB-8 acts as a noncompetitive inhibitor. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 35-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 8531111-6 1995 Moreover, functional inhibition by TMB-8 of muscle-type nAChR is due to a reduction in agonist efficacy, but not potency, and is proportionately stronger with increasing agonist concentration, thereby suggesting that TMB-8 acts as a noncompetitive inhibitor. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 217-222 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 8531111-8 1995 Studies with TMB-8 or BAPTA [1,2-bis(2-aminophenoxy)ethane N,N,N",N"-tetraacetic acid] analogues indicate that the amino group of TMB-8 is essential and that Ca2+ chelation is not required for inhibition of nAChR function. 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate 130-135 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 207-212 7578128-0 1995 Structure of both the ligand- and lipid-dependent channel-inactive states of the nicotinic acetylcholine receptor probed by FTIR spectroscopy and hydrogen exchange. Hydrogen 146-154 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-113 7578128-6 1995 However, in the absence of both cholesterol and anionic lipids, there is a slightly enhanced rate of exchange of alpha-helical peptide hydrogens for deuterium that occurs as a result of either an increase in nAChR dynamics or an increase in the accessibility of transmembrane peptide hydrogens to 2H2O. Hydrogen 135-144 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 7578128-6 1995 However, in the absence of both cholesterol and anionic lipids, there is a slightly enhanced rate of exchange of alpha-helical peptide hydrogens for deuterium that occurs as a result of either an increase in nAChR dynamics or an increase in the accessibility of transmembrane peptide hydrogens to 2H2O. Deuterium 149-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Aspartyl-Glutamine 133-140 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-2 1995 A 17-residue sequence that includes a cystine disulfide and an N-linked glycosylation site is conserved in the extracellular domain of each of the nAChR subunits, and is involved in intersubunit interactions that are critical for assembly of intact, pentameric complexes. cystine disulfide 38-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 9383482-2 1995 A 17-residue sequence that includes a cystine disulfide and an N-linked glycosylation site is conserved in the extracellular domain of each of the nAChR subunits, and is involved in intersubunit interactions that are critical for assembly of intact, pentameric complexes. Nitrogen 63-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Glutamine 137-140 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. ac-tyr-cys 86-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Glutamic Acid 97-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Asparagine 145-148 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Isoleucine 101-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Cysteine 93-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Isoleucine 105-108 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Threonine 153-156 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Valine 109-112 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Amido radical 157-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Threonine 113-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Histidine 117-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Tritium 41-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-202 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Phenylalanine 121-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Proline 125-128 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 9383482-3 1995 A polypeptide representing the relevant sequence from the alpha-subunit of the nAChR (Ac-Tyr-Cys-Glu-Ile-Ile-Val-Thr-His-Phe-Pro-Phe-Asp-Gln-Gln Asn-Cys-Thr-NH2) is small enough to allow detailed structural analysis, which may provide insight into the role of glycosylation in the maturation process that leads to ion-channel assembly. Phenylalanine 129-132 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Tritium 41-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Nicotine 45-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-202 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Nicotine 45-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Nicotine 47-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-202 7473192-1 1995 There is a consensus that high-affinity [3H]-L-nicotine binding sites in the mammalian brain, which are thought to represent a predominant form of central nervous system nicotinic acetylcholine receptor (nAChR) composed of alpha 4 and beta 2 subunits, are increased in number after chronic nicotine exposure. Nicotine 47-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 204-209 7637783-1 1995 In nicotinic acetylcholine receptors (nAChR), as well as glycine, GABAA (gamma-aminobutyric acid), serotonin (5-HT3), and GluCl glutamate receptors, a leucine residue at the approximate midpoint of the M2 transmembrane domain (the 9" position) is conserved across most known subunits. Leucine 151-158 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 3-36 7756343-1 1995 Previous studies have shown that the pattern and degree of 3-(trifluoromethyl)-3-(m-[125I]iodophenyl)diazirine ([125I]TID) photoincorporation into the nicotinic acetylcholine receptor (nAChR) can be used as a sensitive measure of nAChR conformation. 3-(trifluoromethyl)-3-(m-[125i]iodophenyl)diazirine 59-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 151-183 7566493-1 1995 Responses of the human alpha 7 nicotinic acetylcholine receptor (nAChR) in Xenopus laevis oocytes were quantified using two-electrode voltage clamp in the presence of barium (10 mM) to block secondary activation of Ca(2+)-dependent chloride currents. Barium 167-173 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 65-70 7566493-6 1995 Reversible blockade by methyllycaconitine (10 nM) corroborated the responses as due to activation of alpha 7 nAChR. methyllycaconitine 23-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 8567173-6 1995 Moreover, modification of the Glu-21 carboxyl group of cobrotoxin further reduced the nAChR binding activity, while the antigenicity remained unchange. Glutamic Acid 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-91 8567173-7 1995 Thus, our results conclude that the Glu-21 residue and the common interaction of the terminal Leu-1 alpha-amino group and the Asp-58 carboxyl group are related to the nAChR-binding activity of cobrotoxin, and the free carboxyl groups in cobrotoxin are conformation-essential. Glutamic Acid 36-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 8567173-7 1995 Thus, our results conclude that the Glu-21 residue and the common interaction of the terminal Leu-1 alpha-amino group and the Asp-58 carboxyl group are related to the nAChR-binding activity of cobrotoxin, and the free carboxyl groups in cobrotoxin are conformation-essential. Aspartic Acid 126-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 167-172 7490259-0 1995 Determination of soluble nAChR-binding activity of alpha-neurotoxins by an innovative precipitation with DEAE-Sephacel. deae-sephacel 105-118 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 25-30 7756343-1 1995 Previous studies have shown that the pattern and degree of 3-(trifluoromethyl)-3-(m-[125I]iodophenyl)diazirine ([125I]TID) photoincorporation into the nicotinic acetylcholine receptor (nAChR) can be used as a sensitive measure of nAChR conformation. 3-(trifluoromethyl)-3-(m-[125i]iodophenyl)diazirine 59-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 7756343-1 1995 Previous studies have shown that the pattern and degree of 3-(trifluoromethyl)-3-(m-[125I]iodophenyl)diazirine ([125I]TID) photoincorporation into the nicotinic acetylcholine receptor (nAChR) can be used as a sensitive measure of nAChR conformation. 3-(trifluoromethyl)-3-(m-[125i]iodophenyl)diazirine 59-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 230-235 7756343-4 1995 Unlike all other compounds previously tested, alpha-bungarotoxin and alpha-cobrotoxin reproducibly increased the level of [125I]TID incorporation into all four subunits of nAChR reconstituted into dioleoylphosphatidylcholine, dioleoylphosphatidic acid and cholesterol. alpha-cobrotoxin 69-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 7756343-4 1995 Unlike all other compounds previously tested, alpha-bungarotoxin and alpha-cobrotoxin reproducibly increased the level of [125I]TID incorporation into all four subunits of nAChR reconstituted into dioleoylphosphatidylcholine, dioleoylphosphatidic acid and cholesterol. 1,2-oleoylphosphatidylcholine 197-224 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 7541791-4 1995 These findings suggest that Lys-27, Lys-47, and Arg-28 residues may be related to the direct binding to nAChR, and that there is no involvement of Lys-27 in the antigenic determinants of cobrotoxin. Lysine 28-31 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 7541791-4 1995 These findings suggest that Lys-27, Lys-47, and Arg-28 residues may be related to the direct binding to nAChR, and that there is no involvement of Lys-27 in the antigenic determinants of cobrotoxin. Arginine 48-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 7541791-5 1995 Extending the modification to Arg-30, Arg-33, and Arg-36 caused progressive conformational changes of cobrotoxin and resulted in decreased binding activity to antibody and nAChR. Arginine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 7541791-5 1995 Extending the modification to Arg-30, Arg-33, and Arg-36 caused progressive conformational changes of cobrotoxin and resulted in decreased binding activity to antibody and nAChR. Arginine 38-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 7541791-5 1995 Extending the modification to Arg-30, Arg-33, and Arg-36 caused progressive conformational changes of cobrotoxin and resulted in decreased binding activity to antibody and nAChR. Arginine 38-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 172-177 7961707-4 1994 We have shown previously that ionophore-induced calcium influx across the plasma membrane preferentially decreases expression from the adult-type specific nAChR epsilon-subunit gene (Walke, W., Staple, J., Adams, L., Gnegy, M., Chahine, K., and Goldman, D. (1994) J. Biol. Calcium 48-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 155-160 9383400-6 1995 RESULTS: A radiolabeled PhTX analog, containing a photolabile group substituted on one of its aromatic rings, photocrosslinked to all five subunits (alpha, alpha 1, beta, gamma, delta) of purified nAChR in the absence of the 43 kDa protein. phtx 24-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 7480004-3 1995 (+/-)-Epibatidine, GTS-21 and ABT-418 differentially interact with nAChR subtypes to elicit a diversity of behavioral effects including analgesia, neuroprotection and cognitive enhancement. epibatidine 0-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 7480004-3 1995 (+/-)-Epibatidine, GTS-21 and ABT-418 differentially interact with nAChR subtypes to elicit a diversity of behavioral effects including analgesia, neuroprotection and cognitive enhancement. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 7696505-6 1995 Changing the [Ca2+]0 from 1 to 10 mM, the VRs of the nAChR and NMDA currents were shifted by +5.6 +/- 0.4 and +8.3 +/- 0.4 mV, respectively, and the nAChR current decay was accelerated. N-Methylaspartate 63-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 7696505-6 1995 Changing the [Ca2+]0 from 1 to 10 mM, the VRs of the nAChR and NMDA currents were shifted by +5.6 +/- 0.4 and +8.3 +/- 0.4 mV, respectively, and the nAChR current decay was accelerated. N-Methylaspartate 63-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 7957916-3 1994 Electrophysiological studies reveal that these alpha 7-nAChR function as alpha-bungarotoxin (Bgt)-sensitive, quickly activating/inactivating ion channels with a unique pharmacological profile and an unusually high permeability to calcium ions. Calcium 230-237 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 9216991-3 1994 Here we report a single point mutation converting a serine codon to a stop codon in the exon 5 of CHRNA4, in one BFNC family. Serine 52-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-104 7984036-5 1994 Using autopsy samples of the human precentral cortex (Area 4) as a paradigm we have applied digoxigenin-labeled cRNA probes to localize transcripts for the alpha 3- and alpha 4-1-subunits of the nAChR. Digoxigenin 92-103 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 195-200 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 0-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 7963258-13 1994 We suggest that inhibition of ACh-current by long-chain MACs is accounted for by (i) a long-lasting, apparently irreversible, binding of the drug near the channel of nAChR via its long aliphatic chain and (ii) a slow reversible block of the nAChR channel with the MAC"s ammonium head. Acetylcholine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 7963258-13 1994 We suggest that inhibition of ACh-current by long-chain MACs is accounted for by (i) a long-lasting, apparently irreversible, binding of the drug near the channel of nAChR via its long aliphatic chain and (ii) a slow reversible block of the nAChR channel with the MAC"s ammonium head. Acetylcholine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 241-246 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 0-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole 51-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Isoxazoles 40-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Isoxazoles 40-49 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 160-192 7913497-2 1994 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Nicotine 88-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 7913497-3 1994 Compared to (-)-nicotine, ABT 418 has reduced potency to interact with the subunit isoforms of nAChR found in sympathetic ganglia, and it does not compete for alpha-bungarotoxin binding sites in brain or at the neuromuscular junction. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid 26-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 7516704-1 1994 The secondary structure and effects of two ligands, carbamylcholine and tetracaine, on the secondary structure of affinity-purified nicotinic acetylcholine receptor (nAChR) from Torpedo has been studied using Fourier transform infrared spectroscopy (FTIR). Carbachol 52-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 8011898-3 1994 Therefore, given the dimensions of the extracellular domain of the receptor, the ACh binding sites are located significantly below (approximately 25 A) the extracellular apex of the nAChR. Acetylcholine 81-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 7516704-1 1994 The secondary structure and effects of two ligands, carbamylcholine and tetracaine, on the secondary structure of affinity-purified nicotinic acetylcholine receptor (nAChR) from Torpedo has been studied using Fourier transform infrared spectroscopy (FTIR). Carbachol 52-67 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 7516704-1 1994 The secondary structure and effects of two ligands, carbamylcholine and tetracaine, on the secondary structure of affinity-purified nicotinic acetylcholine receptor (nAChR) from Torpedo has been studied using Fourier transform infrared spectroscopy (FTIR). Tetracaine 72-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-164 7516704-1 1994 The secondary structure and effects of two ligands, carbamylcholine and tetracaine, on the secondary structure of affinity-purified nicotinic acetylcholine receptor (nAChR) from Torpedo has been studied using Fourier transform infrared spectroscopy (FTIR). Tetracaine 72-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 166-171 7516704-2 1994 FTIR spectra of the nAChR were acquired in both 1H2O and 2H2O buffer and exhibit spectral features indicative of a substantial alpha-helical content with lesser amounts of beta-sheet and random coil structures. 1h2o 48-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 7516704-2 1994 FTIR spectra of the nAChR were acquired in both 1H2O and 2H2O buffer and exhibit spectral features indicative of a substantial alpha-helical content with lesser amounts of beta-sheet and random coil structures. 2h2o 57-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 20-25 8038129-2 1994 The beta 4 nAChR subunit was detected in both transverse and horizontal sections of the retina using a subunit-specific antiserum and the avidin-biotin complex technique. avidin-biotin 138-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 8038129-9 1994 In situ hybridization with a 35S-labeled cRNA probe revealed the expression of mRNA coding for the nAChR beta 4 subunit in the ganglion cell layer and the inner third of the inner nuclear layer. Sulfur-35 29-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 99-104 7950973-3 1994 We have studied the distribution of nAchR in human brain, particularly in the hippocampus and thalamus, by binding of 3H-nicotine and 3H-cytisine and by in situ hybridization with human alpha 3 and beta 2 nAchR subunits of mRNA. 3h-nicotine 118-129 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 7950973-3 1994 We have studied the distribution of nAchR in human brain, particularly in the hippocampus and thalamus, by binding of 3H-nicotine and 3H-cytisine and by in situ hybridization with human alpha 3 and beta 2 nAchR subunits of mRNA. 3h-cytisine 134-145 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 36-41 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 248-281 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). Nicotine 30-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 283-288 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). Nitrosamines 68-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 248-281 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). Nitrosamines 68-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 283-288 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone 81-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 248-281 7715858-3 1994 We have previously shown that nicotine and the structurally related nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), stimulate the proliferation of neuroendocrine cell lines derived from lung carcinoid tumors via interaction with nicotinic acetylcholine receptors (nAChR). 4-(N-methyl-N-nitrosamino)-1-(3-pyridyl)-1-butanone 81-127 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 283-288 8360687-2 1993 Here we show that cytochalasin treatment, which causes disruption of actin networks, induces marked changes in the numbers and distribution of nAChR, but not mAChR. Cytochalasins 18-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 143-148 8241115-4 1993 Previous studies involving covalent modification of the native nAChR from Torpedo membranes with a variety of affinity reagents indicate that several residues contained within the dodecapeptide sequence (namely, Tyr-190, Cys-192, and Cys-193) apparently contribute directly to the formation of the cholinergic ligand binding site. Tyrosine 212-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 8241115-4 1993 Previous studies involving covalent modification of the native nAChR from Torpedo membranes with a variety of affinity reagents indicate that several residues contained within the dodecapeptide sequence (namely, Tyr-190, Cys-192, and Cys-193) apparently contribute directly to the formation of the cholinergic ligand binding site. Cysteine 234-237 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 8360687-4 1993 Treatment of TE671/RD cells with different cytochalasin analogues (rank order efficacy at 5 micrograms/ml is H > J = B = C = D > A = E) produces a two- to fourfold increase in numbers of membrane-bound nAChR (Bmax in units of specific 125I-labeled alpha-bungarotoxin binding per milligram of membrane protein). Cytochalasins 43-55 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 8360687-5 1993 nAChR up-regulation is evident after 1-2 days of cytochalasin B exposure, is maximal after 3-6 days of drug treatment, and is dominated by an approximately 10-fold increase (per cell) in an intracellular nAChR pool. Cytochalasin B 49-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-5 8360687-6 1993 Cytochalasin-induced nAChR up-regulation is similar in magnitude to, but not additive with, up-regulation of nAChR following chronic exposure to nicotine or phorbol ester. Cytochalasins 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 8360687-6 1993 Cytochalasin-induced nAChR up-regulation is similar in magnitude to, but not additive with, up-regulation of nAChR following chronic exposure to nicotine or phorbol ester. Cytochalasins 0-12 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 109-114 8360687-6 1993 Cytochalasin-induced nAChR up-regulation is similar in magnitude to, but not additive with, up-regulation of nAChR following chronic exposure to nicotine or phorbol ester. Nicotine 145-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 8360687-6 1993 Cytochalasin-induced nAChR up-regulation is similar in magnitude to, but not additive with, up-regulation of nAChR following chronic exposure to nicotine or phorbol ester. Phorbol Esters 157-170 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 8360687-10 1993 These studies suggest that presumed modulation by cytochalasin treatment of cytoskeletal microfilament integrity can differentially influence expression and function of mAChR (a prototype of the metabotropic receptor superfamily) and nAChR (a prototype of the ligand-gated ion-channel superfamily). Cytochalasins 50-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 234-239 8516349-1 1993 Vinblastine has been demonstrated to inhibit nicotinic acetylcholine receptor (nAChR) activity in adrenal chromaffin cells and superior cervical ganglia and to alter agonist binding affinity to nAChR of the electric organ of Torpedo californica. Vinblastine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 194-199 7693004-5 1993 This is consistent with studies of the blocking properties of alcohols at the nAChR channel. Alcohols 62-70 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 8516349-1 1993 Vinblastine has been demonstrated to inhibit nicotinic acetylcholine receptor (nAChR) activity in adrenal chromaffin cells and superior cervical ganglia and to alter agonist binding affinity to nAChR of the electric organ of Torpedo californica. chromaffin 106-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 8516349-1 1993 Vinblastine has been demonstrated to inhibit nicotinic acetylcholine receptor (nAChR) activity in adrenal chromaffin cells and superior cervical ganglia and to alter agonist binding affinity to nAChR of the electric organ of Torpedo californica. Vinblastine 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 8516349-2 1993 In cultured chromaffin cells, vinblastine (IC50, 8.9 microM) is significantly more potent than hexamethonium (IC50, 16 microM) and decamethonium (IC50, 18 microM) and significantly less potent than d-tubocurarine (IC50, 2 microM), pentolinium (IC50, 0.6 microM), and mecamylamine (IC50, 0.1 microM) in inhibiting nAChR-stimulated catecholamine release. Vinblastine 30-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 313-318 8516349-3 1993 These results demonstrate that vinblastine has moderately potent anti-nAChR activity on adrenal nAChR. Vinblastine 31-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 70-75 8516349-3 1993 These results demonstrate that vinblastine has moderately potent anti-nAChR activity on adrenal nAChR. Vinblastine 31-42 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 96-101 8516349-8 1993 The results suggest that vinblastine"s antinicotinic actions are selective for neuronal-type nAChR and do not extend to nAChR of mammalian skeletal muscle. Vinblastine 25-36 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 8474012-7 1993 These results are consistent with expression by IMR-32 cells of functional ganglia-type nAChR that correlate with high affinity [3H]ACh binding sites as well as expression of a distinct class of neuronal/nicotinic alpha-bungarotoxin binding sites that have a ganglia-type pharmacology. Tritium 129-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 20732210-2 1993 Neuronal nAChR are highly sensitive to inorganic lead (Pb(2+)). Lead 55-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 9-14 20732210-5 1993 Surprisingly, between 10 mum and 100 mum Pb(2+) the blocking effect on the nAChR is reversed, and the kinetics of the ACh-induced inward current are delayed. Lead 41-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 20732210-6 1993 Nitromethylene heterocyclic (NMH) compound constitute a new class of selective insecticides, that presumably affect insect nAChR. nitromethylene heterocyclic 0-27 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 20732210-6 1993 Nitromethylene heterocyclic (NMH) compound constitute a new class of selective insecticides, that presumably affect insect nAChR. Methylnitrosourea 29-32 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 123-128 20732210-7 1993 The effect of the NMH compound 1-(pyridin-3-yl-methyl)-2-nitromethylene-imidazolidine (PMNI) on the different subtypes of nAChR has been analysed. Methylnitrosourea 18-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 20732210-7 1993 The effect of the NMH compound 1-(pyridin-3-yl-methyl)-2-nitromethylene-imidazolidine (PMNI) on the different subtypes of nAChR has been analysed. 1-(5-pyridylmethyl)-2-(nitromethylene)imidazolidine 31-85 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 20732210-7 1993 The effect of the NMH compound 1-(pyridin-3-yl-methyl)-2-nitromethylene-imidazolidine (PMNI) on the different subtypes of nAChR has been analysed. Benanomicinone AGL 87-91 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 8474012-6 1993 Functional nAChR ion channels of the ganglia-type are expressed by IMR-32 cells, as assessed by the abilities of nicotinic agonists to stimulate 86Rb+ efflux, the relatively higher sensitivity of those responses to blockade by mecamylamine than by d-tubocurarine, and the inability of alpha-bungarotoxin to antagonize nAChR function. Rubidium-86 145-150 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 8474012-6 1993 Functional nAChR ion channels of the ganglia-type are expressed by IMR-32 cells, as assessed by the abilities of nicotinic agonists to stimulate 86Rb+ efflux, the relatively higher sensitivity of those responses to blockade by mecamylamine than by d-tubocurarine, and the inability of alpha-bungarotoxin to antagonize nAChR function. Mecamylamine 227-239 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 8474012-6 1993 Functional nAChR ion channels of the ganglia-type are expressed by IMR-32 cells, as assessed by the abilities of nicotinic agonists to stimulate 86Rb+ efflux, the relatively higher sensitivity of those responses to blockade by mecamylamine than by d-tubocurarine, and the inability of alpha-bungarotoxin to antagonize nAChR function. Tubocurarine 248-262 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 1397309-4 1992 The cyclic nucleotide-gated channels may be activated by a similar mechanism, but the opening of nicotinic acetylcholine receptor (nAChR) channels is likely to be initiated by the formation of tyrosine radicals. tyrosine radical 193-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-129 8510190-9 1993 The duration of nAChR desensitization may also be useful in explaining individual variability to nicotine"s behavioral effects and may be related to the induction of acute and/or chronic tolerance in both animals and man. Nicotine 97-105 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 1397309-4 1992 The cyclic nucleotide-gated channels may be activated by a similar mechanism, but the opening of nicotinic acetylcholine receptor (nAChR) channels is likely to be initiated by the formation of tyrosine radicals. tyrosine radical 193-210 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 1384491-2 1992 Although the binding activity of cobrotoxin to the nicotinic acetylcholine receptor (nAChR) was decreased after modification of Trp-29, the antigenicity remained essentially unchanged as measured by a competitive RIA. Tryptophan 128-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-83 1505686-2 1992 The binding and interaction of carbamoylcholine with the nicotinic acetylcholine receptor was investigated using photolytically released carbamoylcholine ("caged" carbamoylcholine). Carbachol 31-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-89 1505686-2 1992 The binding and interaction of carbamoylcholine with the nicotinic acetylcholine receptor was investigated using photolytically released carbamoylcholine ("caged" carbamoylcholine). Carbachol 137-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-89 1505686-2 1992 The binding and interaction of carbamoylcholine with the nicotinic acetylcholine receptor was investigated using photolytically released carbamoylcholine ("caged" carbamoylcholine). Carbachol 137-153 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-89 1465217-2 1992 Acetylcholine, nicotine and the neuronal nAChR agonist dimethylphenylpiperazinium iodide (DMPP), but not muscarine, all evoked inward currents in the cells (voltage-clamped at -60 mV). Dimethylphenylpiperazinium Iodide 55-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 1465217-2 1992 Acetylcholine, nicotine and the neuronal nAChR agonist dimethylphenylpiperazinium iodide (DMPP), but not muscarine, all evoked inward currents in the cells (voltage-clamped at -60 mV). Dimethylphenylpiperazinium Iodide 90-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 1465217-3 1992 DMPP"s actions were concentration- and voltage-dependent, and were antagonised by the neuronal nAChR antagonist mecamylamine (1-3 microM). Dimethylphenylpiperazinium Iodide 0-4 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 1465217-3 1992 DMPP"s actions were concentration- and voltage-dependent, and were antagonised by the neuronal nAChR antagonist mecamylamine (1-3 microM). Mecamylamine 112-124 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-100 1465217-7 1992 These findings clearly identify nAChRs in SH-SY5Y cells, and provide two possible mechanisms by which receptor activation may lead to noradrenaline release, namely by triggering Ca2+ influx through the nAChR itself or by opening voltage-gated Ca2+ channels. Norepinephrine 134-147 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 1384491-2 1992 Although the binding activity of cobrotoxin to the nicotinic acetylcholine receptor (nAChR) was decreased after modification of Trp-29, the antigenicity remained essentially unchanged as measured by a competitive RIA. Tryptophan 128-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 1384491-3 1992 Tyr-35-nitrated cobrotoxin still retained relatively high antigenicity and potent binding activity to nAChR. Tyrosine 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 102-107 1592722-8 1992 The plasma dTC concentration required for steady-state twitch inhibition was significantly (P less than 0.05) higher in the experimental group (0.83 +/- 0.04 vs. 0.50 +/- 0.15 micrograms/ml) as were the extrajunctional nAChR (19.76 +/- 1.77 vs. 13.37 +/- 1.82 fmol/mg protein). Tubocurarine 11-14 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 219-224 1517779-1 1992 Anatoxin-a (AnTX) is a highly potent agonist acting at the nicotinic acetylcholine receptor (nAChR) and represents a valuable tool in the study of this receptor. anatoxin a 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-91 1517779-1 1992 Anatoxin-a (AnTX) is a highly potent agonist acting at the nicotinic acetylcholine receptor (nAChR) and represents a valuable tool in the study of this receptor. anatoxin a 0-10 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 1517779-1 1992 Anatoxin-a (AnTX) is a highly potent agonist acting at the nicotinic acetylcholine receptor (nAChR) and represents a valuable tool in the study of this receptor. anatoxin a 12-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-91 1517779-1 1992 Anatoxin-a (AnTX) is a highly potent agonist acting at the nicotinic acetylcholine receptor (nAChR) and represents a valuable tool in the study of this receptor. anatoxin a 12-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 93-98 1581507-7 1992 Fourier transform infrared difference spectra calculated from spectra recorded in the presence and absence of carbamylcholine show small, reproducible bands which reflect changes in nAChR structure upon desensitization. Carbachol 110-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 1592722-10 1992 This study confirms that chronic doses of dTC cause tolerance to its effects and proliferation of nAChR even in the absence of immobilization. Tubocurarine 42-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 2002334-2 1991 Chronic (3-72-h) agonist (nicotine or carbamylcholine) treatment of cells led to a complete (TE671) or nearly complete (PC12) loss of functional nAChR responses, which is referred to as "functional inactivation." Nicotine 26-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 1740234-1 1992 Acetylcholine signals through two types of unrelated membrane receptors referred to as nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. Acetylcholine 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 98-103 1385107-2 1992 A "4-8-12" sequence motif, comprising serine (S) or threonine (T) residues at positions 4, 8 and 12 of M2, is conserved between different members, anion and cation selective, of the nAChR superfamily. Serine 38-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 1385107-2 1992 A "4-8-12" sequence motif, comprising serine (S) or threonine (T) residues at positions 4, 8 and 12 of M2, is conserved between different members, anion and cation selective, of the nAChR superfamily. Threonine 52-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 182-187 1651933-1 1991 The nicotinic acetylcholine receptor (nAChR) is phosphorylated to a high stoichiometry on tyrosine residues both in vitro and in vivo. Tyrosine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 1651933-1 1991 The nicotinic acetylcholine receptor (nAChR) is phosphorylated to a high stoichiometry on tyrosine residues both in vitro and in vivo. Tyrosine 90-98 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 1651933-3 1991 We report here the purification and characterization of a protein tyrosine phosphatase that dephosphorylates tyrosine-phosphorylated nAChR from Torpedo electroplax, a tissue highly enriched in the nAChR. Tyrosine 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 1651933-3 1991 We report here the purification and characterization of a protein tyrosine phosphatase that dephosphorylates tyrosine-phosphorylated nAChR from Torpedo electroplax, a tissue highly enriched in the nAChR. Tyrosine 66-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 197-202 1651933-4 1991 The 32P-labeled tyrosine phosphorylated nAChR was used as a substrate to monitor the enzyme activity during purification. Phosphorus-32 4-7 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 1651933-4 1991 The 32P-labeled tyrosine phosphorylated nAChR was used as a substrate to monitor the enzyme activity during purification. Tyrosine 16-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 1651933-8 1991 It had a neutral pH optimum and a specific activity of 18 mumol/mg of protein/min, with a Km of 4.7 microM for tyrosine-phosphorylated nAChR. Tyrosine 111-119 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 135-140 1651933-9 1991 The phosphatase was specific for tyrosine phosphorylated nAChR; it showed no activity towards the nAChR phosphorylated on serine residues by cAMP-dependent protein kinase. Tyrosine 33-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 2002334-2 1991 Chronic (3-72-h) agonist (nicotine or carbamylcholine) treatment of cells led to a complete (TE671) or nearly complete (PC12) loss of functional nAChR responses, which is referred to as "functional inactivation." Carbachol 38-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 145-150 2002334-3 1991 Some inactivation of nAChR function was also observed for the nicotinic ligands d-tubocurarine (d-TC), mecamylamine, and decamethonium. Tubocurarine 80-94 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 2002334-3 1991 Some inactivation of nAChR function was also observed for the nicotinic ligands d-tubocurarine (d-TC), mecamylamine, and decamethonium. Tubocurarine 96-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 2002334-3 1991 Some inactivation of nAChR function was also observed for the nicotinic ligands d-tubocurarine (d-TC), mecamylamine, and decamethonium. Mecamylamine 103-115 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 2002334-3 1991 Some inactivation of nAChR function was also observed for the nicotinic ligands d-tubocurarine (d-TC), mecamylamine, and decamethonium. decamethonium 121-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 21-26 2002334-8 1991 Recovery of TE671 cell nAChR function following treatment with carbamylcholine, nicotine, or d-TC occurred with half-times of 1-3 days whether cells were maintained in situ or harvested and replated after removal of ligand. Carbachol 63-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 2002334-8 1991 Recovery of TE671 cell nAChR function following treatment with carbamylcholine, nicotine, or d-TC occurred with half-times of 1-3 days whether cells were maintained in situ or harvested and replated after removal of ligand. Nicotine 80-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 2002334-8 1991 Recovery of TE671 cell nAChR function following treatment with carbamylcholine, nicotine, or d-TC occurred with half-times of 1-3 days whether cells were maintained in situ or harvested and replated after removal of ligand. Tubocurarine 93-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 23-28 1910671-1 1991 The pharmacological specificity of a nicotinic acetylcholine receptor (nAChR) optical biosensor was investigated using three fluorescein isothiocyanate (FITC)-tagged neurotoxic peptides that vary in the reversibility of their receptor inhibition: alpha-bungarotoxin (alpha-BGT), alpha-Naja toxin (alpha-NT), and alpha-conotoxin (GI) (alpha-CNTX). Fluorescein-5-isothiocyanate 125-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 1715611-4 1991 Although there is a slight inhibition of the closed nAChR, the main action of MK-801 is to enter and block the open channel. Dizocilpine Maleate 78-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 2049167-5 1991 Stored in phosphate buffered saline (PBS) or in a dry nitrogen atmosphere, the nAChR optical sensor showed no loss of activity over the first 3 days, then showed a slow but gradual loss in activity (45% over the next 30 days). Phosphate-Buffered Saline 10-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 19912783-0 1991 Differential regulation of nicotinic acetylcholine receptor expression by human TE671/RD cells following second messenger modulation and sodium butyrate treatments. Butyric Acid 137-152 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 27-59 19912783-1 1991 Effects of second messenger system modulation and sodium butyrate (NaBu) treatment on nicotinic acetylcholine receptor (nAChR) expression by cells of the TE671/RD human clone were established. Butyric Acid 50-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-118 19912783-1 1991 Effects of second messenger system modulation and sodium butyrate (NaBu) treatment on nicotinic acetylcholine receptor (nAChR) expression by cells of the TE671/RD human clone were established. sethoxydim 67-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 86-118 19912783-2 1991 Treatment with dibutyryl cyclic adenosine 3":5"-monophosphate (dbcAMP) or other substances that increase cellular cAMP content induces a 70% loss of nAChR per unit of membrane protein as assessed by binding studies using (125)I-labeled alpha-bungarotoxin (I-Bgt). Bucladesine 15-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 19912783-2 1991 Treatment with dibutyryl cyclic adenosine 3":5"-monophosphate (dbcAMP) or other substances that increase cellular cAMP content induces a 70% loss of nAChR per unit of membrane protein as assessed by binding studies using (125)I-labeled alpha-bungarotoxin (I-Bgt). Bucladesine 63-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 19912783-2 1991 Treatment with dibutyryl cyclic adenosine 3":5"-monophosphate (dbcAMP) or other substances that increase cellular cAMP content induces a 70% loss of nAChR per unit of membrane protein as assessed by binding studies using (125)I-labeled alpha-bungarotoxin (I-Bgt). Cyclic AMP 65-69 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 19912783-5 1991 Treatment with both PMA and dbcAMP induces a threefold increase in nAChR expression, whereas treatment with NaBu alone or with PMA induces an 80% decrease in I-Bgt binding site expression. Tetradecanoylphorbol Acetate 20-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 19912783-5 1991 Treatment with both PMA and dbcAMP induces a threefold increase in nAChR expression, whereas treatment with NaBu alone or with PMA induces an 80% decrease in I-Bgt binding site expression. Bucladesine 28-34 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 67-72 19912783-7 1991 These data indicate involvement of both cAMP and C-kinase pathways in the regulation of nAChR expression in ways that are not simply additive, possibly due to cross-talk between second messenger pathways. Cyclic AMP 40-44 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 88-93 1910671-1 1991 The pharmacological specificity of a nicotinic acetylcholine receptor (nAChR) optical biosensor was investigated using three fluorescein isothiocyanate (FITC)-tagged neurotoxic peptides that vary in the reversibility of their receptor inhibition: alpha-bungarotoxin (alpha-BGT), alpha-Naja toxin (alpha-NT), and alpha-conotoxin (GI) (alpha-CNTX). Fluorescein-5-isothiocyanate 125-151 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-69 2049167-5 1991 Stored in phosphate buffered saline (PBS) or in a dry nitrogen atmosphere, the nAChR optical sensor showed no loss of activity over the first 3 days, then showed a slow but gradual loss in activity (45% over the next 30 days). Nitrogen 54-62 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 1910671-1 1991 The pharmacological specificity of a nicotinic acetylcholine receptor (nAChR) optical biosensor was investigated using three fluorescein isothiocyanate (FITC)-tagged neurotoxic peptides that vary in the reversibility of their receptor inhibition: alpha-bungarotoxin (alpha-BGT), alpha-Naja toxin (alpha-NT), and alpha-conotoxin (GI) (alpha-CNTX). Fluorescein-5-isothiocyanate 153-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-69 1910671-1 1991 The pharmacological specificity of a nicotinic acetylcholine receptor (nAChR) optical biosensor was investigated using three fluorescein isothiocyanate (FITC)-tagged neurotoxic peptides that vary in the reversibility of their receptor inhibition: alpha-bungarotoxin (alpha-BGT), alpha-Naja toxin (alpha-NT), and alpha-conotoxin (GI) (alpha-CNTX). Fluorescein-5-isothiocyanate 153-157 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 1910671-2 1991 Kinetic analysis of the time course of binding of FITC-neurotoxins to the nAChR-coated fiber gave association rate constants (k+1) of 8.4 x 10(6) M-1 min-1 for FITC-alpha-BGT, 6.0 x 10(6) M-1 min-1 for FITC-alpha-NT and 1.4 x 10(6) M-1 min-1 for FITC-alpha-CNTX. Fluorescein-5-isothiocyanate 50-54 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 1910671-2 1991 Kinetic analysis of the time course of binding of FITC-neurotoxins to the nAChR-coated fiber gave association rate constants (k+1) of 8.4 x 10(6) M-1 min-1 for FITC-alpha-BGT, 6.0 x 10(6) M-1 min-1 for FITC-alpha-NT and 1.4 x 10(6) M-1 min-1 for FITC-alpha-CNTX. Fluorescein-5-isothiocyanate 160-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 1910671-2 1991 Kinetic analysis of the time course of binding of FITC-neurotoxins to the nAChR-coated fiber gave association rate constants (k+1) of 8.4 x 10(6) M-1 min-1 for FITC-alpha-BGT, 6.0 x 10(6) M-1 min-1 for FITC-alpha-NT and 1.4 x 10(6) M-1 min-1 for FITC-alpha-CNTX. fitc-alpha-nt 202-215 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 1910671-2 1991 Kinetic analysis of the time course of binding of FITC-neurotoxins to the nAChR-coated fiber gave association rate constants (k+1) of 8.4 x 10(6) M-1 min-1 for FITC-alpha-BGT, 6.0 x 10(6) M-1 min-1 for FITC-alpha-NT and 1.4 x 10(6) M-1 min-1 for FITC-alpha-CNTX. fitc-alpha-cntx 246-261 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 1910671-8 1991 The optical signal generated by FITC-alpha-NT binding to the nAChR-coated fiber was effectively quenched by agonists and antagonists of the nAChR but not by most of the tested agonists and antagonists of muscarinic cholinergic, adrenergic, glutamatergic, serotonergic, dopaminergic or GABAergic receptors. fitc-alpha-nt 32-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 1910671-8 1991 The optical signal generated by FITC-alpha-NT binding to the nAChR-coated fiber was effectively quenched by agonists and antagonists of the nAChR but not by most of the tested agonists and antagonists of muscarinic cholinergic, adrenergic, glutamatergic, serotonergic, dopaminergic or GABAergic receptors. fitc-alpha-nt 32-45 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 2099742-1 1990 Models for the acetylcholine (ACh)-binding site of the nicotinic acetylcholine receptor (nAChR) are proposed. Acetylcholine 15-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 1979446-0 1990 The role of tyrosine at the ligand-binding site of the nicotinic acetylcholine receptor. Tyrosine 12-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 1979446-5 1990 We have used intrinsic fluorescence spectroscopic analyses together with binding studies of selectively modified peptide fragments of the nAChR to suggest that one or two invariant tyrosine residues at positions 190 and 198 on the alpha-subunit provide the critical negative subsite required for ligand binding. Tyrosine 181-189 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 2209600-8 1990 We have also shown that when the chick nAChR alpha-subunit is expressed in the absence of other receptor subunits, unexpectedly high concentrations of nicotine (10 mM) were required to displace bound alpha-bungarotoxin. Nicotine 151-159 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 39-44 2099742-1 1990 Models for the acetylcholine (ACh)-binding site of the nicotinic acetylcholine receptor (nAChR) are proposed. Acetylcholine 15-28 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 2099742-1 1990 Models for the acetylcholine (ACh)-binding site of the nicotinic acetylcholine receptor (nAChR) are proposed. Acetylcholine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-87 2099742-1 1990 Models for the acetylcholine (ACh)-binding site of the nicotinic acetylcholine receptor (nAChR) are proposed. Acetylcholine 30-33 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 33778899-10 2021 To provide a third line of evidence for neonicotinoid signaling via nAChR, we studied cross-desensitization: pretreatment of LUHMES and SH-SY5Y cells with active neonicotinoids (at 1-10 microM) blunted the signaling response of nicotine. Neonicotinoids 40-53 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 34756924-2 2022 MG624 is a 4-oxystilbene derivative that is active on alpha7- and alpha9-containing neuronal nicotinic acetylcholine receptor (nAChR) subtypes. triethyl-(beta-4-stilbenoxyethyl)ammonium 0-5 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 33809417-1 2021 Garcinol, a nicotinic acetylcholine receptor (nAChR) antagonist, has recently been established as an anti-inflammation agent. garcinol 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 33809417-1 2021 Garcinol, a nicotinic acetylcholine receptor (nAChR) antagonist, has recently been established as an anti-inflammation agent. Acetylcholine 22-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 46-51 28600847-2 2018 Here, we have examined the role of the fifth subunit in the ACh responses of the (alpha4beta2)2 beta2 nAChR type. Acetylcholine 60-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 102-107 34916082-2 2022 The alpha7 nicotinic ACh receptor (nAChR) subtype is highly expressed throughout the hippocampus, has the highest calcium permeability compared with other subtypes of nAChRs, and is of high therapeutic interest due to its association with a variety of neurological disorders and neurodegenerative diseases. Calcium 114-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-40 34756924-2 2022 MG624 is a 4-oxystilbene derivative that is active on alpha7- and alpha9-containing neuronal nicotinic acetylcholine receptor (nAChR) subtypes. 4-oxystilbene 11-24 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 34756924-2 2022 MG624 is a 4-oxystilbene derivative that is active on alpha7- and alpha9-containing neuronal nicotinic acetylcholine receptor (nAChR) subtypes. Acetylcholine 103-116 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 34946630-2 2021 Due to its well-known toxicity for humans, there is considerable interest in the development of synthetic analogues; in particular, conformationally restricted analogues of nicotine have emerged as promising drug molecules for selective nAChR-targeting ligands. Nicotine 173-181 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 237-242 34969831-6 2022 To explore if the different analogs could affect the nAChR conformational state, the nAChR conformational-sensitive probe crystal violet (CrV) was used. Gentian Violet 122-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 34969831-6 2022 To explore if the different analogs could affect the nAChR conformational state, the nAChR conformational-sensitive probe crystal violet (CrV) was used. Gentian Violet 122-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 34969831-6 2022 To explore if the different analogs could affect the nAChR conformational state, the nAChR conformational-sensitive probe crystal violet (CrV) was used. Gentian Violet 138-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 53-58 34969831-6 2022 To explore if the different analogs could affect the nAChR conformational state, the nAChR conformational-sensitive probe crystal violet (CrV) was used. Gentian Violet 138-141 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 34939632-0 2022 Gas phase protonated nicotine is a mixture of pyridine- and pyrrolidine-protonated conformers: implications for its native structure in the nicotinic acetylcholine receptor. Nicotine 21-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-172 34939632-0 2022 Gas phase protonated nicotine is a mixture of pyridine- and pyrrolidine-protonated conformers: implications for its native structure in the nicotinic acetylcholine receptor. pyrrolidine 60-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-172 34939632-8 2022 One of the gas phase nicotine pyrrolidine protomers has the closest conformational resemblance among all low-lying energy isomers with the X-ray structure of nicotine in the nicotinic acetylcholine receptor (nAChR). Nicotine 21-29 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 34939632-8 2022 One of the gas phase nicotine pyrrolidine protomers has the closest conformational resemblance among all low-lying energy isomers with the X-ray structure of nicotine in the nicotinic acetylcholine receptor (nAChR). pyrrolidine 30-41 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 34939632-8 2022 One of the gas phase nicotine pyrrolidine protomers has the closest conformational resemblance among all low-lying energy isomers with the X-ray structure of nicotine in the nicotinic acetylcholine receptor (nAChR). Nicotine 158-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 174-206 34939632-8 2022 One of the gas phase nicotine pyrrolidine protomers has the closest conformational resemblance among all low-lying energy isomers with the X-ray structure of nicotine in the nicotinic acetylcholine receptor (nAChR). Nicotine 158-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 208-213 34577114-4 2021 In this work, we have surveyed a disparate group of sulfonium compounds for their functional activity with alpha7 as well as other nAChR subtypes. Sulfonium 52-61 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 34628512-9 2021 IMI and IMI-olefin were confirmed as nAChR agonists, although with 2-3 orders of magnitude lower potency. imidacloprid 0-3 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 34628512-9 2021 IMI and IMI-olefin were confirmed as nAChR agonists, although with 2-3 orders of magnitude lower potency. imi-olefin 8-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 37-42 34618202-3 2021 OBJECTIVE: The present study tested whether the prototypical nAChR agonist nicotine enhances the ability of humans and rodents to maintain a broad attentional window. Nicotine 75-83 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 61-66 34523332-2 2021 The alpha3beta2 nAChR subtype participates in pain, addiction to nicotine, and other neurophysiological and pathological activities. Nicotine 65-73 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-21 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Cocaine 71-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Cocaine 71-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Cocaine 71-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 264-269 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Dizocilpine Maleate 317-323 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Dizocilpine Maleate 317-323 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 189-194 34546414-5 2022 By transient kinetic measurements, these DNA aptamers, which displaced cocaine from its binding site on the muscle-type nAChR, were classified into two groups based on their effects on the nAChR: Class I aptamers inhibit agonist-induced current in the muscle-type nAChR and Class II molecules alleviate inhibition by MK-801 ((+)-dizocilpine) without affecting the receptor function. Dizocilpine Maleate 329-340 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 34546414-6 2022 The most potent Class I DNA aptamer, which inhibits the muscle-type nAChR, has an apparent dissociation constant (KIapt) of 5 muM, while the most efficient Class II DNA aptamer, which alleviates MK-801-induced inhibition, has an apparent dissociation constant (KApt) of 1.8 muM. Dizocilpine Maleate 195-201 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 34292752-1 2021 The first synthesis of aristoquinoline (1), a naturally occurring nicotinic acetylcholine receptor (nAChR) antagonist, was accomplished using two different approaches. aristoquinoline 23-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 66-98 34292752-1 2021 The first synthesis of aristoquinoline (1), a naturally occurring nicotinic acetylcholine receptor (nAChR) antagonist, was accomplished using two different approaches. aristoquinoline 23-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 100-105 34446200-1 2021 The sulfoximines, as exemplified by sulfoxaflor (Isoclast active), are a relatively new class of nicotinic acetylcholine receptor (nAChR) competitive modulator (Insecticide Resistance Action Committee (IRAC) Group 4C) insecticides that provide control of a wide range of sap-feeding insect pests. sulfoximines 4-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-129 34446200-1 2021 The sulfoximines, as exemplified by sulfoxaflor (Isoclast active), are a relatively new class of nicotinic acetylcholine receptor (nAChR) competitive modulator (Insecticide Resistance Action Committee (IRAC) Group 4C) insecticides that provide control of a wide range of sap-feeding insect pests. sulfoximines 4-16 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 34446200-1 2021 The sulfoximines, as exemplified by sulfoxaflor (Isoclast active), are a relatively new class of nicotinic acetylcholine receptor (nAChR) competitive modulator (Insecticide Resistance Action Committee (IRAC) Group 4C) insecticides that provide control of a wide range of sap-feeding insect pests. sulfoxaflor 36-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 97-129 34446200-1 2021 The sulfoximines, as exemplified by sulfoxaflor (Isoclast active), are a relatively new class of nicotinic acetylcholine receptor (nAChR) competitive modulator (Insecticide Resistance Action Committee (IRAC) Group 4C) insecticides that provide control of a wide range of sap-feeding insect pests. sulfoxaflor 36-47 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 131-136 34577114-6 2021 The smallest sulfonium compound, trimethylsulfonium, was a partial agonist for alpha7 and other neuronal nAChR. Sulfonium 13-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 34577114-6 2021 The smallest sulfonium compound, trimethylsulfonium, was a partial agonist for alpha7 and other neuronal nAChR. trimethylsulfonium 33-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 105-110 34471351-4 2021 Rabies virus glycoprotein (RVG) is a derivative peptide that can specifically bind to nicotinic acetylcholine receptor (nAChR) widely overexpressed on BBB and glioma cells for the invasion of rabies virus into the brain. Acetylcholine 96-109 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 120-125 34938964-9 2021 Revealing the differential affinities of lynx proteins for nAChR subtypes will help elucidate how lynx regulates nAChR-dependent functions in the brain, including nicotine addiction and other critical pathways. Nicotine 163-171 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 34216863-6 2021 ), which is used to treat tobacco addiction and attenuates nicotine withdrawal in both humans and rodents, blocked elevations in ICSS thresholds induced by a single injection of nicotine (0.5 mg/kg, s.c.) followed 2 h later by the non-selective, non-competitive nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine (3.0 mg/kg, s.c.). Mecamylamine 316-328 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 264-296 34216863-6 2021 ), which is used to treat tobacco addiction and attenuates nicotine withdrawal in both humans and rodents, blocked elevations in ICSS thresholds induced by a single injection of nicotine (0.5 mg/kg, s.c.) followed 2 h later by the non-selective, non-competitive nicotinic acetylcholine receptor (nAChR) antagonist mecamylamine (3.0 mg/kg, s.c.). Mecamylamine 316-328 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 298-303 34216863-7 2021 In Experiment 3a, s.c. administration of the competitive, relatively selective alpha4ss2 nAChR antagonist dihydro-beta-erythroidine (DHssE) (5.6 mg/kg, but not 3.0 mg/kg) following each of 5 daily injections of nicotine (0.5 mg/kg, s.c.) elevated ICSS thresholds. Dihydro-beta-Erythroidine 106-131 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 34216863-7 2021 In Experiment 3a, s.c. administration of the competitive, relatively selective alpha4ss2 nAChR antagonist dihydro-beta-erythroidine (DHssE) (5.6 mg/kg, but not 3.0 mg/kg) following each of 5 daily injections of nicotine (0.5 mg/kg, s.c.) elevated ICSS thresholds. dhsse 133-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 89-94 34360698-2 2021 New drugs that bind only those receptors, such as alpha6beta2* nAChR, implicated in nicotine addiction would avoid the off-target binding. Nicotine 84-92 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 63-68 34437426-7 2021 The experiments with the wild-type alpha7 nAChR supported an allosteric mode of action, which was confirmed by the significantly increased MrIC + PNU-120596 responses of three alpha7 nAChR AA site mutants that were designed in silico to improve MrIC binding. N-neopentyl-N-nitrosourea 146-149 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 42-47 34445117-10 2021 Neonicotinoid-induced changes in nAChR function could be responsible for most of the effects observed in the different studies. Neonicotinoids 0-13 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 33-38 34197807-2 2021 We tested their ability either to directly form plasma membrane ion channels or to change functions of two mammalian plasma membrane ion channels, the epithelial sodium channel (ENaC) and the alpha3beta4 nicotinic acetylcholine receptor (nAChR). Acetylcholine 214-227 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 238-243 34253876-14 2022 Interestingly, two putative alpha4beta2-nAChR isoforms, namely sazetidine A-activated, high-sensitive one (alpha42beta23-nAChR) and cytisine-activated, low-sensitive one (alpha43beta22-nAChR) were pharmacologically separated, and the low-sensitive one was more susceptible to l-THP inhibition than the high-sensitive one. sazetidine-A 63-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 34273166-11 2021 Using nicotinic acetylcholine receptor (nAChR) blockers alpha-bungarotoxin and hexamethonium bromide we found that the effects of nicotine on intracellular Ca2+ and oxidative stress were mediated by alpha7 and alpha3 nAChR. Hexamethonium 79-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-38 34273166-11 2021 Using nicotinic acetylcholine receptor (nAChR) blockers alpha-bungarotoxin and hexamethonium bromide we found that the effects of nicotine on intracellular Ca2+ and oxidative stress were mediated by alpha7 and alpha3 nAChR. Hexamethonium 79-100 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 34273166-11 2021 Using nicotinic acetylcholine receptor (nAChR) blockers alpha-bungarotoxin and hexamethonium bromide we found that the effects of nicotine on intracellular Ca2+ and oxidative stress were mediated by alpha7 and alpha3 nAChR. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 6-38 34273166-11 2021 Using nicotinic acetylcholine receptor (nAChR) blockers alpha-bungarotoxin and hexamethonium bromide we found that the effects of nicotine on intracellular Ca2+ and oxidative stress were mediated by alpha7 and alpha3 nAChR. Nicotine 130-138 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 34253876-15 2022 In conclusion, we demonstrate that l-THP blocks neuronal alpha4beta2-nAChR function, which may underlie its inhibition on nicotine addiction. l-thp 35-40 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 34253876-15 2022 In conclusion, we demonstrate that l-THP blocks neuronal alpha4beta2-nAChR function, which may underlie its inhibition on nicotine addiction. Nicotine 122-130 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 34253876-14 2022 Interestingly, two putative alpha4beta2-nAChR isoforms, namely sazetidine A-activated, high-sensitive one (alpha42beta23-nAChR) and cytisine-activated, low-sensitive one (alpha43beta22-nAChR) were pharmacologically separated, and the low-sensitive one was more susceptible to l-THP inhibition than the high-sensitive one. sazetidine-A 63-75 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 121-126 34253876-14 2022 Interestingly, two putative alpha4beta2-nAChR isoforms, namely sazetidine A-activated, high-sensitive one (alpha42beta23-nAChR) and cytisine-activated, low-sensitive one (alpha43beta22-nAChR) were pharmacologically separated, and the low-sensitive one was more susceptible to l-THP inhibition than the high-sensitive one. l-thp 276-281 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 40-45 34301823-9 2021 SIGNIFICANCE STATEMENT: The alpha7-type nicotinic acetylcholine receptor (nAChR) is acknowledged as a potentially important therapeutic target with functional properties associated with both ionotropic and metabotropic signaling. Acetylcholine 50-63 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-79 34061521-0 2021 Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery. erythrina alkaloid 0-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 32-37 34202022-6 2021 We then use AChBP as a template for alpha3beta2 and alpha3beta4 nAChR homology models bound to the alpha-CTX LvIA and re-predict the potencies of eleven point mutations at both subtypes, with an overall RMSE of 0.85 +- 0.08 kcal/mol and an R2 of 0.49. achbp 12-17 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 35044626-1 2022 We have previously shown that the heteromer composed by the dopamine D3 receptor (D3R) and the nicotinic acetylcholine receptor (nAChR) (D3R-nAChR heteromer) is expressed in dopaminergic neurons, activated by nicotine and represents the molecular unit that, in these neurons, contributes to the modulation of critical events such as structural plasticity and neuroprotection. Dopamine 60-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 34241006-12 2021 When combined, these insights may reconcile several apparently contradictory experiments on the role of anionic phospholipids in modulating nAChR. Phospholipids 112-125 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 140-145 35534578-7 2022 Special attention is devoted to the anionic phospholipid phosphatidic acid (PA), which stabilizes the functional resting form of the nAChR. phospholipid phosphatidic acid 44-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 35534578-7 2022 Special attention is devoted to the anionic phospholipid phosphatidic acid (PA), which stabilizes the functional resting form of the nAChR. Phosphatidic Acids 76-78 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 133-138 35534578-9 2022 PA and cholesterol appear to compete for the same binding sites on the nAChR protein. Phosphatidic Acids 0-2 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 35534578-9 2022 PA and cholesterol appear to compete for the same binding sites on the nAChR protein. Cholesterol 7-18 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 71-76 35346843-2 2022 As previously reported for the benzodioxane based analogues, hydroxylation at proper position of benzene ring results in high alpha4beta2 nAChR affinity and alpha4beta2 vs. alpha3beta4 nAChR selectivity. benzodioxane 31-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 35346843-2 2022 As previously reported for the benzodioxane based analogues, hydroxylation at proper position of benzene ring results in high alpha4beta2 nAChR affinity and alpha4beta2 vs. alpha3beta4 nAChR selectivity. benzodioxane 31-43 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 35346843-2 2022 As previously reported for the benzodioxane based analogues, hydroxylation at proper position of benzene ring results in high alpha4beta2 nAChR affinity and alpha4beta2 vs. alpha3beta4 nAChR selectivity. Benzene 97-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 138-143 35346843-2 2022 As previously reported for the benzodioxane based analogues, hydroxylation at proper position of benzene ring results in high alpha4beta2 nAChR affinity and alpha4beta2 vs. alpha3beta4 nAChR selectivity. Benzene 97-104 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 185-190 35565402-0 2022 Reducing Chemotherapy-Induced DNA Damage via nAChR-Mediated Redox Reprograming-A New Mechanism for SCLC Chemoresistance Boosted by Nicotine. Nicotine 131-139 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 45-50 35044626-1 2022 We have previously shown that the heteromer composed by the dopamine D3 receptor (D3R) and the nicotinic acetylcholine receptor (nAChR) (D3R-nAChR heteromer) is expressed in dopaminergic neurons, activated by nicotine and represents the molecular unit that, in these neurons, contributes to the modulation of critical events such as structural plasticity and neuroprotection. Dopamine 60-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 35044626-1 2022 We have previously shown that the heteromer composed by the dopamine D3 receptor (D3R) and the nicotinic acetylcholine receptor (nAChR) (D3R-nAChR heteromer) is expressed in dopaminergic neurons, activated by nicotine and represents the molecular unit that, in these neurons, contributes to the modulation of critical events such as structural plasticity and neuroprotection. Nicotine 209-217 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 95-127 35044626-1 2022 We have previously shown that the heteromer composed by the dopamine D3 receptor (D3R) and the nicotinic acetylcholine receptor (nAChR) (D3R-nAChR heteromer) is expressed in dopaminergic neurons, activated by nicotine and represents the molecular unit that, in these neurons, contributes to the modulation of critical events such as structural plasticity and neuroprotection. Nicotine 209-217 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 129-134 35044626-1 2022 We have previously shown that the heteromer composed by the dopamine D3 receptor (D3R) and the nicotinic acetylcholine receptor (nAChR) (D3R-nAChR heteromer) is expressed in dopaminergic neurons, activated by nicotine and represents the molecular unit that, in these neurons, contributes to the modulation of critical events such as structural plasticity and neuroprotection. Nicotine 209-217 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 141-146 35222535-1 2022 Objective: To investigate the effects of genetic polymorphisms of human nicotinic acetylcholine receptor subunits alpha3, alpha4 and alpha5, which are encoded by CHRNA3, CHRNA4 CHRNA5 genes, respectively, on nicotine addiction and outcomes of pharmacological treatments for smoking cessation. Acetylcholine 82-95 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 170-176 35392565-9 2022 Cotinine was the least potent nAChR compound, only being able to activate alpha4beta2 and alpha6/3beta2beta3 subtypes at high doses and no detectable activities against alpha3beta4 and alpha7 subtypes at the concentrations tested. Cotinine 0-8 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 30-35 35225139-3 2022 There is the possibility of targeting the alpha9alpha10 nicotinic acetylcholine receptor (nAChR) in the prevention of noise-induced, hidden hearing loss and presbycusis. Acetylcholine 66-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 90-95 35225139-6 2022 AREAS COVERED: The work examines the alpha9alpha10 nicotinic acetylcholine receptor (nAChR), its role in noise-induced, hidden hearing loss and presbycusis and the possibility of targeting. Acetylcholine 61-74 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 85-90 35431807-3 2022 Here, we compare two silent nAChR agonists, phosphocholine, which is known to interact with nAChR subunits alpha7, alpha9, and alpha10, and pCF3-N,N-diethyl-N"-phenyl-piperazine (pCF3-diEPP), a previously identified alpha7 nAChR silent agonist, regarding their anti-inflammatory properties and their effects on ionotropic nAChR functions. Phosphorylcholine 44-58 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 35351814-3 2022 Our objective was to develop a method for the selective detection of the potentially pathogenic alpha3-nAChR antibodies, seemingly present only in patients with AAG. aag 161-164 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 103-108 35351814-13 2022 This study provides Class II evidence that alpha3-nAChR CBA is a specific assay for AAG. aag 84-87 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 50-55 35351814-14 2022 CLASSIFICATION OF EVIDENCE: This study provides Class II evidence that an alpha3-nAChR cell-based assay is a more specific assay for AAG than the standard RIPA. aag 133-136 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 35234149-4 2022 The ligands interact with the same residues as the archetypal nAChR agonist nicotine yet display greater affinity, thereby rationalizing their in vivo activity as potent antagonists of nicotine-induced antinociception. Nicotine 76-84 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 35177988-2 2022 Previous studies have shown a link between nicotinic acetylcholine receptors (nAChR) and alcohol addiction. Acetylcholine 53-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 35177988-2 2022 Previous studies have shown a link between nicotinic acetylcholine receptors (nAChR) and alcohol addiction. Alcohols 89-96 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 35177988-4 2022 Methods: Zebrafish (Danio rerio) were exposed to 0.2% alcohol for 14 days followed by 7 days of repeated withdrawal and then retro-orbitally injected with alpha-conotoxin TxIB (a selective alpha6beta2* nAChR antagonist). 2,2,4-trimethyl-1,3-pentanediol diisobutyrate 171-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 202-207 35111269-0 2022 The Natural Compound Dehydrocrenatidine Attenuates Nicotine-Induced Stemness and Epithelial-Mesenchymal Transition in Hepatocellular Carcinoma by Regulating a7nAChR-Jak2 Signaling Pathways. Nicotine 51-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164 35054856-6 2022 The SARS-CoV-2 spike protein has a sequence similar to neurotoxins, capable of binding nicotinic acetylcholine receptors (nAChR). Acetylcholine 97-110 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 122-127 35111269-0 2022 The Natural Compound Dehydrocrenatidine Attenuates Nicotine-Induced Stemness and Epithelial-Mesenchymal Transition in Hepatocellular Carcinoma by Regulating a7nAChR-Jak2 Signaling Pathways. dehydrocrenatidine 21-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 159-164