PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 26428091-9 2016 Autoradiographic analysis of nAChR density revealed higher epibatidine binding in frontal cortical regions in mice exposed to nicotine and ethanol compared to mice exposed to ethanol only. epibatidine 59-70 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 29-34 27166021-1 2016 In this study, we report the synthesis, nAChR in vitro and in vivo pharmacological properties of 2"-fluoro-(carbamoylpyridinyl)deschloroepibatidine analogues (5, 6a,b, and 7a,b), which are analogues of our lead structure epibatidine. epibatidine 136-147 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 40-45 22285742-6 2012 Changes in [(125)I]-epibatidine binding at cytisine-sensitive and cytisine-resistant nAChRs and chronic nicotine-related changes in alpha4, alpha7, and beta2 nAChR subunit mRNA expression were assessed. epibatidine 20-31 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 85-90 26233800-1 2015 Over the last several years we have synthesized and studied the in vitro and in vivo nAChR pharmacological properties of epibatidine (4) analogs. epibatidine 121-132 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 85-90 24800895-0 2014 Discriminative stimulus and hypothermic effects of some derivatives of the nAChR agonist epibatidine in mice. epibatidine 89-100 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 75-80 24800895-8 2014 The nAChR antagonist mecamylamine (3.2 mg/kg) antagonized the discriminative stimulus effects of epibatidine and RTI-7527-102, as well as the hypothermic effects of every drug except cytisine. epibatidine 97-108 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 4-9 25560939-7 2015 In contrast, beta4 gene-dose-dependent decreases in expression 5IA-85380 resistant [(125)I]-epibatidine binding sites (primarily beta4*-nAChR) were observed. epibatidine 92-103 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 136-141 22216213-3 2011 Rapid local delivery (picospritzing) of the nAChR agonist epibatidine was combined with intracellular sharp microelectrode recording to monitor spontaneous and field-stimulation-evoked neurotransmitter release from sympathetic nerve terminals in the mouse isolated vas deferens. epibatidine 58-69 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 44-49 21575611-10 2011 [(125)I]Epibatidine also labels beta4* nAChR, which was readily apparent for incubations conducted in the presence of 100nM cytisine. epibatidine 8-19 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 39-44 21146628-6 2011 Inhibition of alpha7 and alpha9(alpha10) nAChRs with methyllicaconitine resulted in considerable augmentation of CD40-mediated B lymphocyte proliferation in cells of all genotypes; stimulation of alpha4beta2 nAChRs with epibatidine increased the IgM-mediated proliferation of the wild-type and alpha7(-/-), but not beta2(-/-) cells. epibatidine 220-231 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 14-39 21146628-6 2011 Inhibition of alpha7 and alpha9(alpha10) nAChRs with methyllicaconitine resulted in considerable augmentation of CD40-mediated B lymphocyte proliferation in cells of all genotypes; stimulation of alpha4beta2 nAChRs with epibatidine increased the IgM-mediated proliferation of the wild-type and alpha7(-/-), but not beta2(-/-) cells. epibatidine 220-231 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 14-20 22216213-4 2011 Locally applied epibatidine (1 microM) produced "epibatidine-induced depolarisations" (EIDs) that were similar in shape to spontaneous excitatory junction potentials (SEJPs) and were abolished by nonselective nAChR antagonists and the purinergic desensitizing agonist alpha,beta-methylene ATP. epibatidine 16-27 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 209-214 22216213-4 2011 Locally applied epibatidine (1 microM) produced "epibatidine-induced depolarisations" (EIDs) that were similar in shape to spontaneous excitatory junction potentials (SEJPs) and were abolished by nonselective nAChR antagonists and the purinergic desensitizing agonist alpha,beta-methylene ATP. epibatidine 49-60 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 209-214 20702707-8 2010 The effects of nicotine and epibatidine were independent on nicotinic ACh receptor (nAChR) activation because they persisted in the presence of nAChR antagonists. epibatidine 28-39 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 144-149 20599770-4 2010 The studies described here evaluated desensitization elicited by low concentrations of epibatidine, nicotine, cytisine or methylcarbachol of brain alpha4beta2-nAChR function measured with acetylcholine-stimulated (86)Rb(+) efflux from mouse thalamic synaptosomes. epibatidine 87-98 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 159-164 17631923-1 2007 [3H]Epibatidine binds to nAChR subtypes in mouse brain with higher (KD approximately 0.02 nM) and lower affinity (KD approximately 7 nM), which can be further subdivided through inhibition by selected agonists and antagonists. epibatidine 4-15 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 25-30 19672723-1 2010 The diversity of nicotinic acetylcholine receptor (nAChR) subtypes was explored by measuring the effects of gene deletion and pharmacological diversity of epibatidine binding sites in mouse brain. epibatidine 155-166 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 17-49 19672723-1 2010 The diversity of nicotinic acetylcholine receptor (nAChR) subtypes was explored by measuring the effects of gene deletion and pharmacological diversity of epibatidine binding sites in mouse brain. epibatidine 155-166 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 51-56 19672723-3 2010 In agreement with general belief, the alpha4beta2*-nAChR and alpha7-nAChR subtypes are major components of the epibatidine binding sites. epibatidine 111-122 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 51-56 19672723-3 2010 In agreement with general belief, the alpha4beta2*-nAChR and alpha7-nAChR subtypes are major components of the epibatidine binding sites. epibatidine 111-122 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 61-73 19672723-4 2010 alpha4beta2*-nAChR sites account for approximately 70% of total high- and low-affinity epibatidine binding sites, while alpha7-nAChR accounts for 16% of the total sites all of which have lower affinity for epibatidine. epibatidine 87-98 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 13-18 19672723-4 2010 alpha4beta2*-nAChR sites account for approximately 70% of total high- and low-affinity epibatidine binding sites, while alpha7-nAChR accounts for 16% of the total sites all of which have lower affinity for epibatidine. epibatidine 206-217 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 120-132 17631923-9 2007 Deletion of alpha4 virtually eliminated cytisine-sensitive, higher-affinity [3H]epibatidine binding as did beta2 deletion, confirming that these sites are alpha4beta2*-nAChR. epibatidine 80-91 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 168-173 17631923-4 2007 Deletion of the alpha7, beta2 or beta4 nicotinic receptor subunit genes identifies highly expressed subtypes with relatively low affinity for [3H]epibatidine. epibatidine 146-157 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 16-22 20641870-9 2004 FPhEP is an analogue of epibatidine, which was showed to be a functional antagonist of alpha4beta2 nAChR in mice. epibatidine 24-35 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 99-104 17325648-3 2007 EXPERIMENTAL APPROACH: The effect of the nicotinic acetylcholine receptor (nAChR) agonist epibatidine on neurotransmitter release in mouse and guinea pig isolated vas deferens was investigated using contraction studies and conventional intracellular recording techniques. epibatidine 90-101 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 75-80 17203487-6 2007 The density of [(3)H]epibatidine binding sites and the mRNA and protein level of the alpha3 and beta2 nAChR subunits were also increased by RA-induced differentiation. epibatidine 21-32 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 102-107 15383622-4 2004 In contrast, epibatidine (EB) binding sites, which correspond to heteromeric nAChR subtypes, were detected in WBCs of smokers but not in WBCs of nonsmokers. epibatidine 13-24 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 77-82 16545497-3 2006 The alkaloid epibatidine is a highly potent non-opioid analgesic and nAChR agonist, but too toxic to be a useful ligand. epibatidine 13-24 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 69-74 16728647-15 2006 These studies establish that the lower-affinity sites represent a structurally diverse set of sites that require expression of either alpha7, beta2, or beta4 subunits and extend and confirm previous classifications of the higher-affinity [3H]epibatidine binding sites. epibatidine 242-253 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 134-140 15383622-4 2004 In contrast, epibatidine (EB) binding sites, which correspond to heteromeric nAChR subtypes, were detected in WBCs of smokers but not in WBCs of nonsmokers. epibatidine 26-28 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 77-82 15111021-6 2004 As anticipated, likely alpha4beta2-nAChR [125I]-epibatidine binding sites increased with treatment (estimated dosage for one-half maximal increase was 0.44 mg/kg/h, plasma nicotine approximately 20 ng/ml). epibatidine 48-59 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 35-40 15111021-7 2004 86Rb+ efflux with higher sensitivity to acetylcholine and cytisine-sensitive [125I]-epibatidine binding are predominantly alpha4beta2-nAChR. epibatidine 84-95 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 134-139 32585787-6 2004 As anticipated, likely alpha4beta2-nAChR [125I]-epibatidine binding sites increased with treatment (estimated dosage for one-half maximal increase was 0.44 mg/kg/h, plasma nicotine 20 ng/ml). epibatidine 48-59 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 35-40 32585787-7 2004 86Rb+ efflux with higher sensitivity to acetylcholine and cytisine-sensitive [125I]-epibatidine binding are predominantly alpha4beta2-nAChR. epibatidine 84-95 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 134-139 28585241-7 2018 KEY RESULTS: Immunochemical studies confirmed that most of the [3 H]-epibatidine binding corresponds to alpha4beta2*-nAChR and that increases in binding correspond to increases in alpha4 and beta2 proteins. epibatidine 69-80 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 117-122 12079404-2 2002 The binding of Epibatidine and alphaBungarotoxin, ligands for alpha3- and alpha7-containing receptors, respectively, revealed, for each ligand, a single class of high-affinity binding sites, with similar affinity in both wild-type and mdx mice. epibatidine 15-26 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 74-80 11923417-3 2002 Heterologously expressed alpha3beta2 and alpha3beta4 nAChRs are pharmacologically similar to native [125I]alpha-conotoxin MII (alpha-CtxMII)-binding and 3-(2(S)-azetidinylmethoxy)pyridine dihydrochloride (A85380)-resistant [125I]epibatidine-binding nAChR subtypes, respectively. epibatidine 229-240 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 53-58 11923417-8 2002 In contrast, most -resistant [125I]epibatidine-binding nAChRs were dependent on alpha3 gene expression, suggesting that they do indeed correspond to an alpha3 nAChR subtype. epibatidine 35-46 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 55-60 9667769-6 1998 The nAChR agonists (-)nicotine, cytisine, and (+) epibatidine reduced the radioactivity due to [11C]A-84543 in the superior colliculus by 41%, 38%, and 27%, respectively, while lobeline, which also interacts with central nAChRs, produced a 24% inhibition. epibatidine 50-61 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 4-9 9255161-2 1997 This paper describes in vivo binding, kinetics and pharmacology of a highly potent 18F-labeled analog of epibatidine, (+/-)-exo-2-(2-[18F]fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane ([18F]FPH), in the mouse brain with the view towards application of this tracer for PET imaging of nAChR in human brain. epibatidine 105-116 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 282-287 9255161-11 1997 Preinjection of blocking doses of unlabeled epibatidine, (-)-nicotine, lobeline and cytisine significantly inhibited [18F]FPH binding in thalamus and superior colliculus, but not in cerebellum, whereas drugs that interact with binding sites other than acetylcholine recognition sites of nAChR (e.g., mecamylamine, scopolamine, N-methylspiperone and ketanserin) had no effect on [18F]FPH accumulation in any of the brain regions examined. epibatidine 44-55 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 287-292 33326305-9 2021 DC-shifts were produced via nAChRs on primary afferents: they were also seen with nAChR agonists (epibatidine and nicotine), blocked with D-TC but not GABAA receptor blockers, and retained after block of voltage-gated Na+ channels. epibatidine 98-109 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 28-33 33074245-5 2020 This nAChR is a candidate for the analgesic effects of nicotine as well as the frog toxin epibatidine. epibatidine 90-101 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 5-10 32209809-2 2020 Here, we established that the alpha4beta2* nAChR agonist epibatidine can function as a discriminative stimulus in mice. epibatidine 57-68 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 43-48 32209809-6 2020 The partial alpha4beta2* nAChR agonists varenicline and 2"-fluoro-3"-(4-nitro-phenyl)deschloroepibatidine produced 61 and 69% epibatidine-appropriate responding, respectively. epibatidine 94-105 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 25-30 32209809-8 2020 These results show that epibatidine may be trained as a discriminative stimulus in mice and has utility in elucidating the in-vivo pharmacology of alpha4beta2* nAChR ligands. epibatidine 24-35 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 160-165 11030722-1 2000 [(125)I]-Epibatidine binds to multiple nicotinic acetylcholine receptor (nAChR) subtypes with high affinity. epibatidine 9-20 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 39-71 11030722-1 2000 [(125)I]-Epibatidine binds to multiple nicotinic acetylcholine receptor (nAChR) subtypes with high affinity. epibatidine 9-20 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 73-78 11030722-2 2000 In this study, [(125)I]-epibatidine was used to label and characterize a novel nAChR subtype found in mouse brain inferior colliculus, interpeduncular nucleus, and olfactory bulb homogenates. epibatidine 24-35 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 79-84 7542542-1 1995 The purpose of this investigation was to determine if analogous to (-)-nicotine"s analgesic effect, the analgesic effect of the recently characterized potent nicotinic acetylcholine receptor (nAChR) agonist (+/-)-epibatidine was altered in response to treatment with the calcium channel agonist (+/-)-Bay K 8644. epibatidine 207-224 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 158-190 7542542-1 1995 The purpose of this investigation was to determine if analogous to (-)-nicotine"s analgesic effect, the analgesic effect of the recently characterized potent nicotinic acetylcholine receptor (nAChR) agonist (+/-)-epibatidine was altered in response to treatment with the calcium channel agonist (+/-)-Bay K 8644. epibatidine 207-224 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 192-197 28781257-2 2017 Quantitative determination of nAChR in the striatum and substantia nigra (SN) was performed using the radioactive derivatives of epibatidine, -conotoxin MII, and -bungarotoxin as ligands. epibatidine 129-140 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 30-35