PMID-sentid Pub_year Sent_text comp_official_name comp_offset protein_name organism prot_offset 18786552-1 2009 Amongst the family members of Cys-loop LGICs, the atypical ability of the 5-HT3A subunit to form functional homomeric receptors allowed a direct investigation of the role of the C-terminus. Cysteine 30-33 5-hydroxytryptamine receptor 3A Homo sapiens 74-80 18474595-3 2008 Mutation of cytoplasmic arginine residues 432, 436, and 440 to glutamine, aspartate, and alanine (the aligned residues of the human 5-HT3B subunit (yielding 5-HT3A(QDA)) increased PCa/PCs from 1.4 to 3.7. N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine 164-167 5-hydroxytryptamine receptor 3A Homo sapiens 157-163 18622264-0 2008 Association between a polymorphism of the HTR3A gene and therapeutic response to risperidone treatment in drug-naive Chinese schizophrenia patients. Risperidone 81-92 5-hydroxytryptamine receptor 3A Homo sapiens 42-47 18622264-4 2008 METHODS: The study recruited 107 drug-naive Chinese schizophrenia patients who were given 8 weeks of risperidone monotherapy and it explored three of four single nucleotide polymorphisms spanning HTR3A for possible association with therapeutic improvement, using the Positive and Negative Symptom Scale. Risperidone 101-112 5-hydroxytryptamine receptor 3A Homo sapiens 196-201 18622264-9 2008 CONCLUSION: The results of this study are the first to suggest that the polymorphism of HTR3A may be a useful predictor of therapeutic response to risperidone treatment in Chinese schizophrenic patients, although these conclusions should be treated with caution because of the intricacy of the variety of the therapeutic effects to risperidone. Risperidone 147-158 5-hydroxytryptamine receptor 3A Homo sapiens 88-93 19086332-2 2008 Factors predicting treatment responsiveness are not known, although we have demonstrated that symptom improvement with the 5-HT3R antagonist alosetron is correlated with reduced amygdala activity. alosetron 141-150 5-hydroxytryptamine receptor 3A Homo sapiens 123-129 19086332-8 2008 CONCLUSIONS: Irritable bowel disease symptom improvement with 5-HT3R antagonist alosetron is related to pre-treatment reactivity of the left OFC, which may be partially captured by subjective measures of interpersonal sensitivity. alosetron 80-89 5-hydroxytryptamine receptor 3A Homo sapiens 62-68 18622264-9 2008 CONCLUSION: The results of this study are the first to suggest that the polymorphism of HTR3A may be a useful predictor of therapeutic response to risperidone treatment in Chinese schizophrenic patients, although these conclusions should be treated with caution because of the intricacy of the variety of the therapeutic effects to risperidone. Risperidone 332-343 5-hydroxytryptamine receptor 3A Homo sapiens 88-93 18670328-5 2008 Among the currently available 5-hydroxytryptamine receptor 3 antagonists (5-HT3), ondansetron is being most widely used with unsatisfactory results regarding opioid-based IV PCA related PONV. Ondansetron 82-93 5-hydroxytryptamine receptor 3A Homo sapiens 30-60 18474595-2 2008 We examined the influence on Ca2+ permeation of amino acids located at intra- and extracellular ends of the conduction pathway of the human 5-hydroxytryptamine type 3A (5-HT3A) receptor. Serotonin 140-159 5-hydroxytryptamine receptor 3A Homo sapiens 169-175 18474595-6 2008 A conserved aspartate, located toward the extracellular end of the conduction pathway and known to influence ionic selectivity, contributed to the inhibitory effect of Ca2+ on macroscopic currents mediated by 5-HT3A receptors. Aspartic Acid 12-21 5-hydroxytryptamine receptor 3A Homo sapiens 209-215 18635474-0 2008 The effects of fentanyl-like opioids and hydromorphone on human 5-HT3A receptors. Hydromorphone 41-54 5-hydroxytryptamine receptor 3A Homo sapiens 64-70 17161536-1 2007 Despite its beneficial effect in IBS patients, the mechanism of action of the 5-HT3 receptor (5-HT3R) antagonist alosetron is still incompletely understood. alosetron 113-122 5-hydroxytryptamine receptor 3A Homo sapiens 78-92 18379051-6 2008 In oocytes expressing glycine or 5-HT3A receptors, quercetin- or its glycosides-induced inhibitions on glycine- (IGly) and 5-HT-induced current (I5-HT) were dose-dependent and reversible. Glycine 103-110 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 18379051-10 2008 These results also indicate that quercetin glycosides might regulate the human glycine alpha1 and mouse 5-HT3A receptors with differential manners. Rutin 33-53 5-hydroxytryptamine receptor 3A Homo sapiens 104-110 18311193-4 2008 KEY RESULTS: 5-HT(3A) receptor responses were inhibited by mefloquine, quinine and chloroquine with IC(50) values of 0.66, 1.06 and 24.3 microM. Mefloquine 59-69 5-hydroxytryptamine receptor 3A Homo sapiens 13-20 18311193-4 2008 KEY RESULTS: 5-HT(3A) receptor responses were inhibited by mefloquine, quinine and chloroquine with IC(50) values of 0.66, 1.06 and 24.3 microM. Chloroquine 83-94 5-hydroxytryptamine receptor 3A Homo sapiens 13-20 18311193-11 2008 CONCLUSIONS AND IMPLICATIONS: The effects of mefloquine, quinine and chloroquine are distinct at GABA(A) and GABA(C) receptors, whereas their effects on 5-HT(3AB) receptors are broadly similar to those at 5-HT(3A) receptors. Mefloquine 45-55 5-hydroxytryptamine receptor 3A Homo sapiens 153-160 18311193-11 2008 CONCLUSIONS AND IMPLICATIONS: The effects of mefloquine, quinine and chloroquine are distinct at GABA(A) and GABA(C) receptors, whereas their effects on 5-HT(3AB) receptors are broadly similar to those at 5-HT(3A) receptors. Chloroquine 69-80 5-hydroxytryptamine receptor 3A Homo sapiens 153-160 18292429-12 2008 CONCLUSIONS: At least two separate inhibitory actions on 5-HT3A receptors could be identified for propofol, whereas the enhancing action seen for the two related smaller phenol derivatives could no longer be detected. Propofol 98-106 5-hydroxytryptamine receptor 3A Homo sapiens 57-63 17993512-0 2008 Anandamide inhibition of 5-HT3A receptors varies with receptor density and desensitization. anandamide 0-10 5-hydroxytryptamine receptor 3A Homo sapiens 25-31 18045909-0 2007 Differential effects of serotonin and dopamine on human 5-HT3A receptor kinetics: interpretation within an allosteric kinetic model. Serotonin 24-33 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 18045909-0 2007 Differential effects of serotonin and dopamine on human 5-HT3A receptor kinetics: interpretation within an allosteric kinetic model. Dopamine 38-46 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 18045909-3 2007 In this study, we report the results of electrophysiological studies using rapid solution exchange designed to characterize and compare the actions of the high-efficacy agonist serotonin and the low-efficacy agonist dopamine on human 5-HT3A receptors expressed in human embryonic kidney HEK293 cells. Serotonin 177-186 5-hydroxytryptamine receptor 3A Homo sapiens 234-240 18045909-3 2007 In this study, we report the results of electrophysiological studies using rapid solution exchange designed to characterize and compare the actions of the high-efficacy agonist serotonin and the low-efficacy agonist dopamine on human 5-HT3A receptors expressed in human embryonic kidney HEK293 cells. Dopamine 216-224 5-hydroxytryptamine receptor 3A Homo sapiens 234-240 17669396-0 2007 Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital. Etomidate 56-65 5-hydroxytryptamine receptor 3A Homo sapiens 20-27 17669396-0 2007 Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital. Propofol 67-75 5-hydroxytryptamine receptor 3A Homo sapiens 20-27 17669396-0 2007 Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital. Pentobarbital 80-93 5-hydroxytryptamine receptor 3A Homo sapiens 20-27 17669396-2 2007 Using oocyte electrophysiology, the effects of etomidate, propofol, and pentobarbital on human 5-HT(3A) and 5-HT(3AB) receptors were studied and compared. Pentobarbital 72-85 5-hydroxytryptamine receptor 3A Homo sapiens 95-102 17669396-4 2007 Because the half-maximal inhibitory concentrations for etomidate, propofol and pentobarbital in 5-HT(3A) and 5-HT(3AB) receptors were all above their respective anaesthetic concentrations, the results of our study suggest that neither 5-HT(3) receptor subtype contributes to the anaesthetic actions of etomidate, propofol or pentobarbital. Etomidate 55-64 5-hydroxytryptamine receptor 3A Homo sapiens 96-103 17669396-4 2007 Because the half-maximal inhibitory concentrations for etomidate, propofol and pentobarbital in 5-HT(3A) and 5-HT(3AB) receptors were all above their respective anaesthetic concentrations, the results of our study suggest that neither 5-HT(3) receptor subtype contributes to the anaesthetic actions of etomidate, propofol or pentobarbital. Propofol 66-74 5-hydroxytryptamine receptor 3A Homo sapiens 96-103 17669396-4 2007 Because the half-maximal inhibitory concentrations for etomidate, propofol and pentobarbital in 5-HT(3A) and 5-HT(3AB) receptors were all above their respective anaesthetic concentrations, the results of our study suggest that neither 5-HT(3) receptor subtype contributes to the anaesthetic actions of etomidate, propofol or pentobarbital. Pentobarbital 79-92 5-hydroxytryptamine receptor 3A Homo sapiens 96-103 17637025-0 2007 1-Oxo-5-hydroxytryptamine: a surprisingly potent agonist of the 5-HT3 (serotonin) receptor. 1-oxo-5-hydroxytryptamine 0-25 5-hydroxytryptamine receptor 3A Homo sapiens 64-90 18379051-3 2008 In the previous studies, we demonstrated that quercetin inhibits both glycine and 5-hydroxytryptamine type 3, (5-HT3A) receptor channel activities expressed in Xenopus oocytes. Quercetin 46-55 5-hydroxytryptamine receptor 3A Homo sapiens 111-117 18379051-4 2008 However, the effects of quercetin glycosides on glycine and 5-HT3A receptor channel activities are not well known. Rutin 24-44 5-hydroxytryptamine receptor 3A Homo sapiens 60-66 18379051-6 2008 In oocytes expressing glycine or 5-HT3A receptors, quercetin- or its glycosides-induced inhibitions on glycine- (IGly) and 5-HT-induced current (I5-HT) were dose-dependent and reversible. Quercetin 51-60 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 18379051-6 2008 In oocytes expressing glycine or 5-HT3A receptors, quercetin- or its glycosides-induced inhibitions on glycine- (IGly) and 5-HT-induced current (I5-HT) were dose-dependent and reversible. Glycosides 69-79 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 18292429-0 2008 Molecular actions of propofol on human 5-HT3A receptors: enhancement as well as inhibition by closely related phenol derivatives. Propofol 21-29 5-hydroxytryptamine receptor 3A Homo sapiens 39-45 18292429-0 2008 Molecular actions of propofol on human 5-HT3A receptors: enhancement as well as inhibition by closely related phenol derivatives. Phenol 110-116 5-hydroxytryptamine receptor 3A Homo sapiens 39-45 18292429-3 2008 To investigate the molecular mechanisms responsible for these contrasting actions, we examined the kinetics of the action of propofol and its lesser hydrophobic derivatives 2-isopropylphenol and phenol on human 5-HT3A receptors. Propofol 125-133 5-hydroxytryptamine receptor 3A Homo sapiens 211-217 18292429-3 2008 To investigate the molecular mechanisms responsible for these contrasting actions, we examined the kinetics of the action of propofol and its lesser hydrophobic derivatives 2-isopropylphenol and phenol on human 5-HT3A receptors. 2-isopropylphenol 173-190 5-hydroxytryptamine receptor 3A Homo sapiens 211-217 18292429-6 2008 RESULTS: When applied in equilibrium (60 s before and during the 5-HT pulse), propofol inhibited human 5-HT3A receptors (IC50 = 18 +/- 1.0 microM). Propofol 78-86 5-hydroxytryptamine receptor 3A Homo sapiens 103-109 18292429-7 2008 In equilibrium, the less hydrophobic 2-isopropylphenol was surprisingly a similarly potent inhibitor of human 5-HT3A receptors (IC50 = 17 +/- 3.2 microM), whereas phenol was considerably less potent (IC50 = 1.6 +/- 0.2 mM). 2-isopropylphenol 37-54 5-hydroxytryptamine receptor 3A Homo sapiens 110-116 18292429-7 2008 In equilibrium, the less hydrophobic 2-isopropylphenol was surprisingly a similarly potent inhibitor of human 5-HT3A receptors (IC50 = 17 +/- 3.2 microM), whereas phenol was considerably less potent (IC50 = 1.6 +/- 0.2 mM). Phenol 48-54 5-hydroxytryptamine receptor 3A Homo sapiens 110-116 18082160-2 2008 Here we show that 5-fluorotryptamine (5-FT) is a partial agonist at both 5-HT3A and 5-HT3AB receptors with an Rmax (Imax/Imax 5-HT) of 0.64 and 0.45 respectively. 5-fluorotryptamine 18-36 5-hydroxytryptamine receptor 3A Homo sapiens 73-85 18082160-2 2008 Here we show that 5-fluorotryptamine (5-FT) is a partial agonist at both 5-HT3A and 5-HT3AB receptors with an Rmax (Imax/Imax 5-HT) of 0.64 and 0.45 respectively. 5-fluorotryptamine 38-42 5-hydroxytryptamine receptor 3A Homo sapiens 73-85 17656445-3 2007 The aims of this study were to evaluate the effects of the 5-HT3 antagonist granisetron on the BP, heart rate (HR), and antropyloroduodenal (APD) motility responses to intraduodenal glucose in healthy older subjects. Glucose 182-189 5-hydroxytryptamine receptor 3A Homo sapiens 59-64 17161536-1 2007 Despite its beneficial effect in IBS patients, the mechanism of action of the 5-HT3 receptor (5-HT3R) antagonist alosetron is still incompletely understood. alosetron 113-122 5-hydroxytryptamine receptor 3A Homo sapiens 94-100 17360702-7 2007 Potentiation by smaller alcohols was consistently significantly greater in 5-HT(3A) than in 5-HT(3AB) receptors, whereas inhibition by larger alcohols was not. Alcohols 24-32 5-hydroxytryptamine receptor 3A Homo sapiens 75-82 16534507-1 2006 We investigated the effect of 5-hydroxytryptamine 3A and 3B receptor (HTR3A and HTR3B) gene polymorphisms on nausea induced by paroxetine in Japanese psychiatric patients. Paroxetine 127-137 5-hydroxytryptamine receptor 3A Homo sapiens 70-75 17562330-4 2007 Ondansetron, a 5-HT-3 serotonin receptor antagonist augmented significantly ADCC. Ondansetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 15-40 16873768-6 2007 Further experiments with isotype-selective receptor agonists allowed us to demonstrate that 5-HT induced calcium transients via activation of 5-HTR1, 5-HTR2, and 5-HTR3 in A549 and BEAS-2B cells. Calcium 105-112 5-hydroxytryptamine receptor 3A Homo sapiens 164-168 17692006-9 2007 Of all GlyR potentiating substances identified to date, we conclude that 5HT(3)R antagonists such as tropisetron offer the most promise as therapeutic lead compounds. Tropisetron 101-112 5-hydroxytryptamine receptor 3A Homo sapiens 73-80 16931691-0 2006 The effects of morphine on human 5-HT3A receptors. Morphine 15-23 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 16427041-5 2006 A similar low potent inhibition of human 5-HT(3A) receptors was found for (+) and (-) O-demethyl-tramadol (IC50=158 and 63 microM, respectively). O-demethyltramadol 86-105 5-hydroxytryptamine receptor 3A Homo sapiens 41-48 16551836-0 2006 N-terminal domains in mouse and human 5-hydroxytryptamine3A receptors confer partial agonist and antagonist properties to benzylidene analogs of anabaseine. benzylidene 122-133 5-hydroxytryptamine receptor 3A Homo sapiens 38-59 16551836-0 2006 N-terminal domains in mouse and human 5-hydroxytryptamine3A receptors confer partial agonist and antagonist properties to benzylidene analogs of anabaseine. anabaseine 145-155 5-hydroxytryptamine receptor 3A Homo sapiens 38-59 16551836-1 2006 The present study tested the hypothesis that mouse and human 5-hydroxytryptamine3A (5-HT3A) receptors may be differentially modulated by benzylidene analogs of anabaseine (BA) and that these analogs may be useful in assessing residues involved in receptor gating. benzylidene 137-148 5-hydroxytryptamine receptor 3A Homo sapiens 61-82 16551836-1 2006 The present study tested the hypothesis that mouse and human 5-hydroxytryptamine3A (5-HT3A) receptors may be differentially modulated by benzylidene analogs of anabaseine (BA) and that these analogs may be useful in assessing residues involved in receptor gating. anabaseine 160-170 5-hydroxytryptamine receptor 3A Homo sapiens 61-82 16551836-1 2006 The present study tested the hypothesis that mouse and human 5-hydroxytryptamine3A (5-HT3A) receptors may be differentially modulated by benzylidene analogs of anabaseine (BA) and that these analogs may be useful in assessing residues involved in receptor gating. Barium 172-174 5-hydroxytryptamine receptor 3A Homo sapiens 61-82 16551836-5 2006 BA compounds antagonized 1.5 microM 5-HT-mediated (EC50) responses in the HWT 5-HT3A receptor with a rank order of potency (IC50 in muM) of 2-OHMBA (1.5 +/- 0.1) > DMXBA (3.1 +/- 0.2) > 4-OHMBA (7.4 +/- 0.5) > 2,4-DiOHBA (12.8 +/- 0.7). Barium 0-2 5-hydroxytryptamine receptor 3A Homo sapiens 78-84 16551836-5 2006 BA compounds antagonized 1.5 microM 5-HT-mediated (EC50) responses in the HWT 5-HT3A receptor with a rank order of potency (IC50 in muM) of 2-OHMBA (1.5 +/- 0.1) > DMXBA (3.1 +/- 0.2) > 4-OHMBA (7.4 +/- 0.5) > 2,4-DiOHBA (12.8 +/- 0.7). 2-ohmba 140-147 5-hydroxytryptamine receptor 3A Homo sapiens 78-84 16551836-5 2006 BA compounds antagonized 1.5 microM 5-HT-mediated (EC50) responses in the HWT 5-HT3A receptor with a rank order of potency (IC50 in muM) of 2-OHMBA (1.5 +/- 0.1) > DMXBA (3.1 +/- 0.2) > 4-OHMBA (7.4 +/- 0.5) > 2,4-DiOHBA (12.8 +/- 0.7). 3-(2,4-dimethoxybenzylidene)anabaseine 167-172 5-hydroxytryptamine receptor 3A Homo sapiens 78-84 16551836-5 2006 BA compounds antagonized 1.5 microM 5-HT-mediated (EC50) responses in the HWT 5-HT3A receptor with a rank order of potency (IC50 in muM) of 2-OHMBA (1.5 +/- 0.1) > DMXBA (3.1 +/- 0.2) > 4-OHMBA (7.4 +/- 0.5) > 2,4-DiOHBA (12.8 +/- 0.7). 4-ohmba 192-199 5-hydroxytryptamine receptor 3A Homo sapiens 78-84 16551836-5 2006 BA compounds antagonized 1.5 microM 5-HT-mediated (EC50) responses in the HWT 5-HT3A receptor with a rank order of potency (IC50 in muM) of 2-OHMBA (1.5 +/- 0.1) > DMXBA (3.1 +/- 0.2) > 4-OHMBA (7.4 +/- 0.5) > 2,4-DiOHBA (12.8 +/- 0.7). 2,4-diohba 219-229 5-hydroxytryptamine receptor 3A Homo sapiens 78-84 16551836-8 2006 Thus, amino acids present in the distal one-third of the N terminus of mouse and human 5-HT3A receptors are necessary and sufficient to confer partial agonist or antagonist properties of 2-OHMBA. 2-ohmba 187-194 5-hydroxytryptamine receptor 3A Homo sapiens 87-93 16874005-6 2006 The 178C/C genotype of the HTR3A was associated with an antidepressant response (p = 0.022-0.042), and more significantly in paroxetine-treated patients (p = 0.002-0.042). Paroxetine 125-135 5-hydroxytryptamine receptor 3A Homo sapiens 27-32 15920198-2 2005 Studies have shown that modulation of 5-HT3A receptor currents by n-alcohols depends on molecular volume, suggesting that steric interactions between n-alcohols and their binding sites define their action on this receptor. n-alcohols 66-76 5-hydroxytryptamine receptor 3A Homo sapiens 38-44 16221844-9 2005 Disulfide bonds formed in 5-HT3A/K81C/A304C and 5-HT3A/K81C/I305C when coexpressed with 5-HT3B. Disulfides 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 26-32 16221844-9 2005 Disulfide bonds formed in 5-HT3A/K81C/A304C and 5-HT3A/K81C/I305C when coexpressed with 5-HT3B. Disulfides 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 48-54 16314763-0 2005 Serotonin receptor genes HTR3A and HTR3B are not involved in Gilles de la Tourette syndrome. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 25-30 15914697-1 2005 The serotonin type 3 receptor (5-HT(3)R) is a member of the cys-loop ligand-gated ion channel (LGIC) superfamily. Cysteine 60-63 5-hydroxytryptamine receptor 3A Homo sapiens 31-39 15814570-7 2005 Mutation of the 7" leucine to threonine in 5-HT3A receptors increased PTX sensitivity roughly 10-fold, comparable with that observed in GABA(A) receptors, and also conferred distinct gating kinetics. Picrotoxin 70-73 5-hydroxytryptamine receptor 3A Homo sapiens 43-49 15920198-2 2005 Studies have shown that modulation of 5-HT3A receptor currents by n-alcohols depends on molecular volume, suggesting that steric interactions between n-alcohols and their binding sites define their action on this receptor. n-alcohols 150-160 5-hydroxytryptamine receptor 3A Homo sapiens 38-44 15920198-9 2005 However, only agents smaller than 0.120 nm3 shifted the 5-HT3A receptor"s serotonin concentration-response curve to the left, whereas larger anesthetics shifted them to the right. Serotonin 74-83 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 15920198-10 2005 Modulation of human 5-HT3A-mediated currents by volatile anesthetics exhibits a dependence on molecular volume consistent with the n-alcohols, suggesting that both classes of agents may enhance 5-HT3A receptor function via the same mechanism. n-alcohols 131-141 5-hydroxytryptamine receptor 3A Homo sapiens 20-26 15830306-11 2005 Palonosetron is a new drug in the class of 5-HT (3) (serotonin) receptor antagonists. Palonosetron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 43-72 15554432-4 2004 Administration of the 5-HT3 serotonin receptor subtype antagonist, ondansetron, has been associated with substantial sustained clinical ameliorations of profound fatigue in at least some patients with chronic liver disease. Ondansetron 67-78 5-hydroxytryptamine receptor 3A Homo sapiens 22-46 15683818-4 2005 Palonoestron (a 5-HT3R antagonist) and aprepitant (an antagonist for the protachykinin 1 receptor) have been introduced for the prevention of emesis. palonoestron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 16-22 15157181-9 2004 Replacement of three arginine residues (R432, R436 and R440) unique to the HA stretch of the 5-HT3A subunit with the aligned residues (Q395, D399 and A403) of the 5-HT3B subunit increased the single-channel conductance 28-fold. Arginine 21-29 5-hydroxytryptamine receptor 3A Homo sapiens 93-99 15318223-3 2004 Here we identify structural requirements for functionally coupling the two domains by combining acetylcholine (ACh)-binding protein, whose structure was determined at atomic resolution, with the pore domain from the serotonin type-3A (5-HT3A) receptor. Acetylcholine 96-109 5-hydroxytryptamine receptor 3A Homo sapiens 235-241 15318223-4 2004 Only when amino-acid sequences of three loops in ACh-binding protein are changed to their 5-HT3A counterparts does ACh bind with low affinity characteristic of activatable receptors, and trigger opening of the ion pore. Acetylcholine 49-52 5-hydroxytryptamine receptor 3A Homo sapiens 90-96 15515405-1 2004 There is evidence from both human and animal research that 5-hydroxytryptamine3 (5-HT3) receptor antagonists, particularly tropisetron, exert analgesic and antiinflammatory effects. Tropisetron 123-134 5-hydroxytryptamine receptor 3A Homo sapiens 81-86 15541891-6 2004 In both preparations, the 5-HT effect was shown to be mediated by 5HT3Rs, as it was mimicked by the selective 5HT3R agonist m-chlorophenyl biguanide and blocked by the selective 5HT3R antagonist 3-tropanylindole-3-carboxylate hydrochloride. 1-(3-chlorophenyl)biguanide 124-148 5-hydroxytryptamine receptor 3A Homo sapiens 66-71 15541891-6 2004 In both preparations, the 5-HT effect was shown to be mediated by 5HT3Rs, as it was mimicked by the selective 5HT3R agonist m-chlorophenyl biguanide and blocked by the selective 5HT3R antagonist 3-tropanylindole-3-carboxylate hydrochloride. 1-(3-chlorophenyl)biguanide 124-148 5-hydroxytryptamine receptor 3A Homo sapiens 110-115 15541891-6 2004 In both preparations, the 5-HT effect was shown to be mediated by 5HT3Rs, as it was mimicked by the selective 5HT3R agonist m-chlorophenyl biguanide and blocked by the selective 5HT3R antagonist 3-tropanylindole-3-carboxylate hydrochloride. Tropisetron hydrochloride 195-239 5-hydroxytryptamine receptor 3A Homo sapiens 66-71 15541891-7 2004 The 5HT3R-mediated increase in GABA release was blocked by 100 microM cadmium or by omitting Ca2+ in external solutions, indicating the Ca2+-dependence of the effect. gamma-Aminobutyric Acid 31-35 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 15541891-7 2004 The 5HT3R-mediated increase in GABA release was blocked by 100 microM cadmium or by omitting Ca2+ in external solutions, indicating the Ca2+-dependence of the effect. Cadmium 70-77 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 15102340-7 2004 CONCLUSIONS: The present results suggest that the HTR3A and DBH genes may participate in the regulation of dopamine and serotonin turnover rates in the central nervous system. Dopamine 107-115 5-hydroxytryptamine receptor 3A Homo sapiens 50-55 15102340-7 2004 CONCLUSIONS: The present results suggest that the HTR3A and DBH genes may participate in the regulation of dopamine and serotonin turnover rates in the central nervous system. Serotonin 120-129 5-hydroxytryptamine receptor 3A Homo sapiens 50-55 15055527-0 2004 Differential effect of ginsenoside metabolites on the 5-HT3A receptor-mediated ion current in Xenopus oocytes. Ginsenosides 23-34 5-hydroxytryptamine receptor 3A Homo sapiens 54-60 15055527-5 2004 In previous work we demonstrated that the ginsenoside Rg2 regulates human 5-hydroxytryptamine3A (5-HT3A) receptor channel activity [Choi et al. Ginsenosides 42-53 5-hydroxytryptamine receptor 3A Homo sapiens 97-103 15055527-13 2004 These results indicate that M4, a metabolite of PT ginsenosides, acts primarily on 5-HT3A receptors and further, that ginsenosides as well as ginsenoside metabolites can influence 5-HT3A receptor channel activity in Xenopus oocytes. Ginsenosides 118-130 5-hydroxytryptamine receptor 3A Homo sapiens 180-186 14760130-2 2004 Palonosetron, a potent and highly selective 5-HT3 antagonist with a strong affinity for 5-HT3 and a prolonged plasma elimination half-life, may provide a longer duration of action than other approved agents. Palonosetron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 44-49 14760130-2 2004 Palonosetron, a potent and highly selective 5-HT3 antagonist with a strong affinity for 5-HT3 and a prolonged plasma elimination half-life, may provide a longer duration of action than other approved agents. Palonosetron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 88-93 15123883-3 2004 A high proportion of tsA-201 cells cotransfected with the cDNAs of 5-HT(3)R and CD8 produced large amplitude responses (0.57.0 nA) to serotonin. Serotonin 134-143 5-hydroxytryptamine receptor 3A Homo sapiens 67-75 15123883-5 2004 Lysine at position 281, a basic residue, is more susceptible to acidification-induced blockade of the 5-HT(3)R channel. Lysine 0-6 5-hydroxytryptamine receptor 3A Homo sapiens 102-110 12970351-0 2003 Arginine 222 in the pre-transmembrane domain 1 of 5-HT3A receptors links agonist binding to channel gating. Arginine 0-8 5-hydroxytryptamine receptor 3A Homo sapiens 50-56 14636070-3 2003 The secondary structure of detergent-solubilized 5-HT(3)R determined by curve fitting of the amide I band yielded 36% alpha-helix, 33% beta-strand, 15% beta-turn, and 16% nonregular structures, which remained unchanged upon reconstitution in lipid membranes. Amides 93-98 5-hydroxytryptamine receptor 3A Homo sapiens 49-57 14636070-4 2003 From hydrogen-deuterium exchange, the secondary structure of the water-accessible part of 5-HT(3)R was determined as 14% alpha-helix, 16% beta-strand, 26% beta-turn, and 14% nonregular structures. Hydrogen 5-13 5-hydroxytryptamine receptor 3A Homo sapiens 90-98 14636070-4 2003 From hydrogen-deuterium exchange, the secondary structure of the water-accessible part of 5-HT(3)R was determined as 14% alpha-helix, 16% beta-strand, 26% beta-turn, and 14% nonregular structures. Deuterium 14-23 5-hydroxytryptamine receptor 3A Homo sapiens 90-98 14636070-4 2003 From hydrogen-deuterium exchange, the secondary structure of the water-accessible part of 5-HT(3)R was determined as 14% alpha-helix, 16% beta-strand, 26% beta-turn, and 14% nonregular structures. Water 65-70 5-hydroxytryptamine receptor 3A Homo sapiens 90-98 12970351-4 2003 Arginine 222 (Arg-222), located at the distal end of the extracellular N-terminal domain immediately preceding the first transmembrane domain (TM1), is conserved in all 5-HT3A receptors and alpha7-nicotinic acetylcholine receptors that have been cloned. Arginine 0-8 5-hydroxytryptamine receptor 3A Homo sapiens 169-175 12970351-4 2003 Arginine 222 (Arg-222), located at the distal end of the extracellular N-terminal domain immediately preceding the first transmembrane domain (TM1), is conserved in all 5-HT3A receptors and alpha7-nicotinic acetylcholine receptors that have been cloned. Arginine 0-3 5-hydroxytryptamine receptor 3A Homo sapiens 169-175 12970351-5 2003 To elucidate the possible role of Arg-222 in the function of 5-HT3A receptors, we mutated the arginine residue to alanine (Ala) and expressed both the wild-type and the mutant receptor in human embryonic kidney 293 cells. Arginine 34-37 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 12970351-10 2003 The results suggest that the pre-TM1 amino acid residue Arg-222 may be involved in the transduction mechanism linking agonist binding to channel gating in 5-HT3A receptors. Arginine 56-59 5-hydroxytryptamine receptor 3A Homo sapiens 155-161 12660235-3 2003 To investigate the role of particular residues in ligand binding of the serotonin 5-HT3AS receptor (5-HT3R), glutamate amino acid residues at three different positions, Glu97, Glu224, and Glu235, in the extracellular N-terminal domain were substituted with aspartate and glutamine using site-directed mutagenesis. Aspartic Acid 257-266 5-hydroxytryptamine receptor 3A Homo sapiens 100-106 12867984-7 2003 Replacement of three arginine residues unique to the HA-stretch of the 5-HT3A subunit by their 5-HT3B subunit counterparts increased single-channel conductance 28-fold. Arginine 21-29 5-hydroxytryptamine receptor 3A Homo sapiens 71-77 12867984-9 2003 Our findings solve the conundrum of the anomalously low conductance of homomeric 5-HT3A receptors and indicate an important function for the HA-stretch in Cys-loop transmitter-gated ion channels. Cysteine 155-158 5-hydroxytryptamine receptor 3A Homo sapiens 81-87 12660235-3 2003 To investigate the role of particular residues in ligand binding of the serotonin 5-HT3AS receptor (5-HT3R), glutamate amino acid residues at three different positions, Glu97, Glu224, and Glu235, in the extracellular N-terminal domain were substituted with aspartate and glutamine using site-directed mutagenesis. Glutamine 271-280 5-hydroxytryptamine receptor 3A Homo sapiens 100-106 12660235-5 2003 A structural model of the ligand-binding domain of the 5-HT3R based on the acetylcholine binding protein revealed the position of the mutated amino acids. Acetylcholine 75-88 5-hydroxytryptamine receptor 3A Homo sapiens 55-61 12660235-8 2003 Comparison of the fluorescence properties of a fluorescein-labeled antagonist upon binding to wild type 5-HT3R and E235Q, allowed us to localize Glu235 within a distance of 1 nm around the ligand-binding site, as proposed by our model. Fluorescein 47-58 5-hydroxytryptamine receptor 3A Homo sapiens 104-110 12217367-1 2002 Electrostatic potential surface mapping of various aromatic ring systems contained in 5-HT(3)R agonists indicate that some agonists contain an aromatic moiety capable of a favorable cation-pi interaction next to the e-face of pyridine (or its bioisostere). pyridine 226-234 5-hydroxytryptamine receptor 3A Homo sapiens 86-94 12643925-0 2003 Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). meta-chlorophenylbiguanide 105-131 5-hydroxytryptamine receptor 3A Homo sapiens 72-96 12643925-0 2003 Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). 1-(3-chlorophenyl)biguanide 133-138 5-hydroxytryptamine receptor 3A Homo sapiens 72-96 12643925-0 2003 Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). meta-chlorophenylguanidine 144-170 5-hydroxytryptamine receptor 3A Homo sapiens 72-96 12643925-0 2003 Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). 2-amino-2-(2-methylenecyclopropyl)acetic acid 172-176 5-hydroxytryptamine receptor 3A Homo sapiens 72-96 12363396-8 2002 These results make unlikely the possibility that 5-HT3A and 5-HT3B receptor genes underlie variation in clinical response to clozapine. Clozapine 125-134 5-hydroxytryptamine receptor 3A Homo sapiens 49-55 12360456-1 2002 BACKGROUND & AIMS: The 5-HT3 receptor (5-HT3R) antagonist Alosetron (Alos) reduces the symptoms of female patients with diarrhea-predominant irritable bowel syndrome (IBS); yet, the mechanism(s) underlying this effect remains incompletely understood. alosetron 62-71 5-hydroxytryptamine receptor 3A Homo sapiens 27-41 12360456-1 2002 BACKGROUND & AIMS: The 5-HT3 receptor (5-HT3R) antagonist Alosetron (Alos) reduces the symptoms of female patients with diarrhea-predominant irritable bowel syndrome (IBS); yet, the mechanism(s) underlying this effect remains incompletely understood. alosetron 62-71 5-hydroxytryptamine receptor 3A Homo sapiens 43-49 12360456-1 2002 BACKGROUND & AIMS: The 5-HT3 receptor (5-HT3R) antagonist Alosetron (Alos) reduces the symptoms of female patients with diarrhea-predominant irritable bowel syndrome (IBS); yet, the mechanism(s) underlying this effect remains incompletely understood. alosetron 62-66 5-hydroxytryptamine receptor 3A Homo sapiens 27-41 12360456-1 2002 BACKGROUND & AIMS: The 5-HT3 receptor (5-HT3R) antagonist Alosetron (Alos) reduces the symptoms of female patients with diarrhea-predominant irritable bowel syndrome (IBS); yet, the mechanism(s) underlying this effect remains incompletely understood. alosetron 62-66 5-hydroxytryptamine receptor 3A Homo sapiens 43-49 12360456-0 2002 Condition-specific deactivation of brain regions by 5-HT3 receptor antagonist Alosetron. alosetron 78-87 5-hydroxytryptamine receptor 3A Homo sapiens 52-66 12360456-8 2002 RESULTS: Alos treatment, as compared with placebo, improved IBS symptoms and reduced rCBF in 5-HT3R containing regions of the EMS, but not in areas activated by pain. alosetron 9-13 5-hydroxytryptamine receptor 3A Homo sapiens 93-99 11495906-10 2001 Of the 20 proline residues in the 5-HT3A receptor subunit only Pro170 has adjacent residues that are favorable. Proline 10-17 5-hydroxytryptamine receptor 3A Homo sapiens 34-40 12079499-1 2002 BACKGROUND: Lerisetron, a competitive serotonin type 3 receptor (5-HT3R) antagonist, contains five functional groups capable of interacting with amino acids in the 5-HT3R binding site. lerisetron 12-22 5-hydroxytryptamine receptor 3A Homo sapiens 65-71 12079499-1 2002 BACKGROUND: Lerisetron, a competitive serotonin type 3 receptor (5-HT3R) antagonist, contains five functional groups capable of interacting with amino acids in the 5-HT3R binding site. lerisetron 12-22 5-hydroxytryptamine receptor 3A Homo sapiens 164-170 12079499-5 2002 RESULTS: Two analogs of lerisetron were synthesized to probe 5-HT3R functional group interactions with this compound. lerisetron 24-34 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 11259629-2 2001 Using the whole-cell voltage-clamp technique, we investigated desensitization kinetics of recombinant human and guinea pig alpha-homomeric 5-hydroxytryptamine type 3 (5-HT(3A)) receptors heterologously expressed in human embryonic kidney 293 cells. Serotonin 139-158 5-hydroxytryptamine receptor 3A Homo sapiens 167-174 11762972-2 2001 This is particularly relevant with the high-cost 5HT3 antiemetics, which include ondansetron, dolasetron and granisetron. Ondansetron 81-92 5-hydroxytryptamine receptor 3A Homo sapiens 49-53 11762972-2 2001 This is particularly relevant with the high-cost 5HT3 antiemetics, which include ondansetron, dolasetron and granisetron. dolasetron 94-104 5-hydroxytryptamine receptor 3A Homo sapiens 49-53 11762972-2 2001 This is particularly relevant with the high-cost 5HT3 antiemetics, which include ondansetron, dolasetron and granisetron. Granisetron 109-120 5-hydroxytryptamine receptor 3A Homo sapiens 49-53 11557597-6 2001 Application of the 5-HT (5-150 microM) and 5-HT(3)-R agonist 2-methyl-5-HT (5-150 microM) induced inward currents in a concentration-dependent manner. 2-methyl-5-HT 61-74 5-hydroxytryptamine receptor 3A Homo sapiens 43-52 11259629-4 2001 By constructing various chimeras and through site-directed mutagenesis, we have identified a single serine in the M1 region of the human 5-HT(3A) receptor sequence (S248) that, when substituted with threonine found in the equivalent guinea pig sequence (T254), conferred guinea pig-like kinetics on the time course of desensitization of the human receptor. Serine 100-106 5-hydroxytryptamine receptor 3A Homo sapiens 137-144 11259629-4 2001 By constructing various chimeras and through site-directed mutagenesis, we have identified a single serine in the M1 region of the human 5-HT(3A) receptor sequence (S248) that, when substituted with threonine found in the equivalent guinea pig sequence (T254), conferred guinea pig-like kinetics on the time course of desensitization of the human receptor. Threonine 199-208 5-hydroxytryptamine receptor 3A Homo sapiens 137-144 11111833-1 2000 Serotonin (5-HT) exerts fast excitatory responses by activation of 5-HT3 receptors, irrespective of whether they are homomerically composed of 5-HT3A subunits or heteromerically assembled of 5-HT3A and 5-HT3B subunits. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 191-197 11212100-0 2001 The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Tropisetron 21-32 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 11212100-1 2001 The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Tropisetron 30-41 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 11212100-2 2001 Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Ondansetron 38-49 5-hydroxytryptamine receptor 3A Homo sapiens 10-15 11212100-2 2001 Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. ly-278 54-60 5-hydroxytryptamine receptor 3A Homo sapiens 10-15 10997728-0 2000 Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects. barbituric acid 97-108 5-hydroxytryptamine receptor 3A Homo sapiens 18-24 10997728-4 2000 The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response. Ondansetron 31-42 5-hydroxytryptamine receptor 3A Homo sapiens 4-10 10608286-1 1999 In order to study the subunit composition of 5-HT3 receptors (5-HT3R), we report that (2-aminoethyl)methanethiosulfonate (MTSEA) can enhance the function of both nicotinic ACh receptors (nAChRs) comprised of alpha4/beta2 subunits, and heteromeric channels assembled from serotonin 5-HT3R and alpha4 nAChR subunits. methanethiosulfonate ethylammonium 86-120 5-hydroxytryptamine receptor 3A Homo sapiens 45-60 10639097-2 2000 Uniquely, 5-HT3 receptor subunits (5-HT3A and 5-HT3B) possess a positively charged lysine residue within the putative channel lining M2 domain (4" position). Lysine 83-89 5-hydroxytryptamine receptor 3A Homo sapiens 35-41 10639097-8 2000 Each of the mutants desensitized more slowly than the WT 5-HT3A receptor, with the arginine and glycine mutations exhibiting the greatest effect (5-fold reduction). Arginine 83-91 5-hydroxytryptamine receptor 3A Homo sapiens 57-63 10639097-8 2000 Each of the mutants desensitized more slowly than the WT 5-HT3A receptor, with the arginine and glycine mutations exhibiting the greatest effect (5-fold reduction). Glycine 96-103 5-hydroxytryptamine receptor 3A Homo sapiens 57-63 10608286-1 1999 In order to study the subunit composition of 5-HT3 receptors (5-HT3R), we report that (2-aminoethyl)methanethiosulfonate (MTSEA) can enhance the function of both nicotinic ACh receptors (nAChRs) comprised of alpha4/beta2 subunits, and heteromeric channels assembled from serotonin 5-HT3R and alpha4 nAChR subunits. methanethiosulfonate ethylammonium 86-120 5-hydroxytryptamine receptor 3A Homo sapiens 62-68 10608286-1 1999 In order to study the subunit composition of 5-HT3 receptors (5-HT3R), we report that (2-aminoethyl)methanethiosulfonate (MTSEA) can enhance the function of both nicotinic ACh receptors (nAChRs) comprised of alpha4/beta2 subunits, and heteromeric channels assembled from serotonin 5-HT3R and alpha4 nAChR subunits. methanethiosulfonate ethylammonium 86-120 5-hydroxytryptamine receptor 3A Homo sapiens 281-287 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 78-88 5-hydroxytryptamine receptor 3A Homo sapiens 59-64 10347245-6 1999 The magnitude of the shift increased with the number of residues (3, 5, or 7) exchanged, with septuple mutations of m5-HT3A and human 5-HT3A subunits producing a 161-fold decrease and 53-fold increase in the apparent affinity of (+)-Tc, respectively. Technetium 229-235 5-hydroxytryptamine receptor 3A Homo sapiens 117-123 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 78-88 5-hydroxytryptamine receptor 3A Homo sapiens 140-145 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 78-88 5-hydroxytryptamine receptor 3A Homo sapiens 140-145 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 147-150 5-hydroxytryptamine receptor 3A Homo sapiens 59-64 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 147-150 5-hydroxytryptamine receptor 3A Homo sapiens 140-145 10026168-4 1999 Comparison of the sequences of these two subunits with the 5HT3R shows that a tryptophan residue is found in the homologous position in the 5HT3R (Trp-89), suggesting that this residue may be involved in curare-5HT3R interactions. Tryptophan 147-150 5-hydroxytryptamine receptor 3A Homo sapiens 140-145 10026168-5 1999 Site-directed mutagenesis at position Trp-89 markedly reduces the affinity of the 5HT3R for the antagonists curare and granisetron but has little effect on the affinity for the agonist serotonin. Tryptophan 38-41 5-hydroxytryptamine receptor 3A Homo sapiens 82-87 9950429-7 1999 Heteromeric assemblies of 5-HT3A and 5-HT3B subunits display a large single-channel conductance (16 pS), low permeability to calcium ions, and a current-voltage relationship which resembles that of characterized neuronal 5-HT3 channels. Calcium 125-132 5-hydroxytryptamine receptor 3A Homo sapiens 26-32 9933581-8 1999 To test the hypothesis that the alpha4 subunit contributes to the lining of the pore of the resulting 5-HT3R channel, a mutant nicotinic alpha4 subunit with a reactive cysteine residue engineered into the putative pore region was constructed by substituting the leucine at position 285 (alpha4-L285C). Cysteine 168-176 5-hydroxytryptamine receptor 3A Homo sapiens 102-108 9933581-8 1999 To test the hypothesis that the alpha4 subunit contributes to the lining of the pore of the resulting 5-HT3R channel, a mutant nicotinic alpha4 subunit with a reactive cysteine residue engineered into the putative pore region was constructed by substituting the leucine at position 285 (alpha4-L285C). Leucine 262-269 5-hydroxytryptamine receptor 3A Homo sapiens 102-108 9933581-10 1999 When the alpha4-L285C subunit was co-expressed with the 5-HT3R subunit, both MTSET and silver nitrate (AgNO3), another cysteine-modifying reagent, significantly reduced the serotonin-induced current. Silver Nitrate 87-101 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 9933581-10 1999 When the alpha4-L285C subunit was co-expressed with the 5-HT3R subunit, both MTSET and silver nitrate (AgNO3), another cysteine-modifying reagent, significantly reduced the serotonin-induced current. Silver Nitrate 103-108 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 9933581-10 1999 When the alpha4-L285C subunit was co-expressed with the 5-HT3R subunit, both MTSET and silver nitrate (AgNO3), another cysteine-modifying reagent, significantly reduced the serotonin-induced current. Cysteine 119-127 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 9933581-10 1999 When the alpha4-L285C subunit was co-expressed with the 5-HT3R subunit, both MTSET and silver nitrate (AgNO3), another cysteine-modifying reagent, significantly reduced the serotonin-induced current. Serotonin 173-182 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 9164590-0 1997 Effects of 5-HT3, D1 and D2 receptor antagonists on ethanol- and cocaine-induced locomotion. Ethanol 52-59 5-hydroxytryptamine receptor 3A Homo sapiens 11-16 9680250-1 1998 D-Tubocurarine is a potent competitive antagonist of two members of the ligand-gated ion channel family, the muscle-type nicotinic acetylcholine receptor (AChR) and serotonin type-3 receptor (5HT3R). Tubocurarine 0-14 5-hydroxytryptamine receptor 3A Homo sapiens 192-197 9680250-2 1998 We have used a series of analogs of D-tubocurarine to determine the effects of methylation, stereoisomerization and halogenation on the interaction of D-tubocurarine with the 5HT3R. Tubocurarine 36-50 5-hydroxytryptamine receptor 3A Homo sapiens 175-180 9680250-2 1998 We have used a series of analogs of D-tubocurarine to determine the effects of methylation, stereoisomerization and halogenation on the interaction of D-tubocurarine with the 5HT3R. Tubocurarine 151-165 5-hydroxytryptamine receptor 3A Homo sapiens 175-180 9736758-1 1998 Serotonin (5-hydroxytryptamine) type 3 receptors (5-HT3R) and nicotinic acetylcholine receptors are structurally and functionally related proteins, yet distinct members of the family of ligand-gated ion channels. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 50-56 9164590-0 1997 Effects of 5-HT3, D1 and D2 receptor antagonists on ethanol- and cocaine-induced locomotion. Cocaine 65-72 5-hydroxytryptamine receptor 3A Homo sapiens 11-16 9164590-1 1997 The effects of acute treatment with 5-HT3 receptor antagonists, ondansetron and ICS 205-930, on the stimulation of activity induced by ethanol-and cocaine were examined. Ethanol 135-142 5-hydroxytryptamine receptor 3A Homo sapiens 36-41 9164590-1 1997 The effects of acute treatment with 5-HT3 receptor antagonists, ondansetron and ICS 205-930, on the stimulation of activity induced by ethanol-and cocaine were examined. Cocaine 147-154 5-hydroxytryptamine receptor 3A Homo sapiens 36-41 22298739-0 1995 The 5-HT3 antagonist ondansetron reduces gastrointestinal side effects induced by a specific serotonin re-uptake inhibitor in man. Ondansetron 21-32 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 8636782-4 1996 PATIENTS AND METHODS: We applied a novel statistical approach to investigate whether the efficacy of the 5HT3 receptor antagonist ICS 205-930 (tropisetron) is maintained over repeated cycles of weekly high-dose cisplatin. Cisplatin 211-220 5-hydroxytryptamine receptor 3A Homo sapiens 105-109 8848005-5 1995 A quantitative comparison of the pharmacological profiles of human and mouse recombinant 5-HT3R-AS receptor complexes revealed differences in the potencies of some antagonist or agonist compounds tested, the most dramatic example being (+)-tubocurarine, which demonstrated an approximately 1800-fold discrepancy in antagonist potency. Tubocurarine 236-252 5-hydroxytryptamine receptor 3A Homo sapiens 89-95 8856622-0 1996 Pathogenetic aspects of responsiveness to ondansetron (5-hydroxytryptamine type 3 receptor antagonist) in patients with primary fibromyalgia syndrome--a preliminary study. Ondansetron 42-53 5-hydroxytryptamine receptor 3A Homo sapiens 55-90 8856622-1 1996 OBJECTIVE: To study the efficacy of 5-hydroxytryptamine type 3 receptor (5-HT-3R) antagonist (ondansetron) vs paracetamol in primary fibromyalgia (FM) syndrome. Ondansetron 94-105 5-hydroxytryptamine receptor 3A Homo sapiens 36-71 8856622-1 1996 OBJECTIVE: To study the efficacy of 5-hydroxytryptamine type 3 receptor (5-HT-3R) antagonist (ondansetron) vs paracetamol in primary fibromyalgia (FM) syndrome. Ondansetron 94-105 5-hydroxytryptamine receptor 3A Homo sapiens 73-80 9455457-2 1996 This issue is a clinical analysis of the protective effect of a 5HT3 antagonist (Navoban-R; Sandoz Pharma Ltd., Basel, Switzerland) against chemotherapy--induced emesis (especially with the most emetic cytostatics--cisplatin and dacarbazine). navoban-r 81-90 5-hydroxytryptamine receptor 3A Homo sapiens 64-68 9455457-2 1996 This issue is a clinical analysis of the protective effect of a 5HT3 antagonist (Navoban-R; Sandoz Pharma Ltd., Basel, Switzerland) against chemotherapy--induced emesis (especially with the most emetic cytostatics--cisplatin and dacarbazine). Cisplatin 215-224 5-hydroxytryptamine receptor 3A Homo sapiens 64-68 9455457-2 1996 This issue is a clinical analysis of the protective effect of a 5HT3 antagonist (Navoban-R; Sandoz Pharma Ltd., Basel, Switzerland) against chemotherapy--induced emesis (especially with the most emetic cytostatics--cisplatin and dacarbazine). Dacarbazine 229-240 5-hydroxytryptamine receptor 3A Homo sapiens 64-68 8991800-0 1995 Effects of granisetron, a 5-HT3 receptor antagonist, on morphine-induced potentiation of brain stimulation reward. Granisetron 11-22 5-hydroxytryptamine receptor 3A Homo sapiens 26-31 7565620-11 1995 Transfection of COS-1 with human 5-HT3R cDNA induced specific binding of the 5-HT3R-selective radioligand [3H]YM060. Tritium 107-109 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 7565620-11 1995 Transfection of COS-1 with human 5-HT3R cDNA induced specific binding of the 5-HT3R-selective radioligand [3H]YM060. Tritium 107-109 5-hydroxytryptamine receptor 3A Homo sapiens 77-83 7565620-12 1995 Human 5-HT3R showed typical characteristics of the 5-HT3R, but its affinity for the 5-HT3R agonist m-chlorophenylbiguanide was much lower than that of rat 5-HT3R. 1-(3-chlorophenyl)biguanide 99-122 5-hydroxytryptamine receptor 3A Homo sapiens 6-12 7565620-14 1995 The potency of the agonists to induce inward current paralleled that to compete with the radioligand binding, and 2-methyl-5-hydroxytryptamine, a partial agonist for mouse 5-HT3R, was a full agonist for human 5-HT3R. 2-methyl-5-HT 114-142 5-hydroxytryptamine receptor 3A Homo sapiens 209-215 22298739-0 1995 The 5-HT3 antagonist ondansetron reduces gastrointestinal side effects induced by a specific serotonin re-uptake inhibitor in man. Serotonin 93-102 5-hydroxytryptamine receptor 3A Homo sapiens 4-9 7993957-1 1994 Results from animal studies have suggested that serotonin (5-HT) antagonists acting on the 5-HT3 receptor may have anxiolytic properties. Serotonin 48-57 5-hydroxytryptamine receptor 3A Homo sapiens 91-96 7808432-2 1994 The selective 5-HT3 receptor agonist 1-(m-chlorophenyl)-biguanide (mCPBG) caused a concentration-dependent increase in the cytoplasmic Ca2+ concentration ([Ca2+]i) in N1E-115 cells and in HEK 293 cells transfected with either the 5-HT3 A subunit or the 5-HT3 As subunit. 1-(3-chlorophenyl)biguanide 37-65 5-hydroxytryptamine receptor 3A Homo sapiens 230-237 7808432-2 1994 The selective 5-HT3 receptor agonist 1-(m-chlorophenyl)-biguanide (mCPBG) caused a concentration-dependent increase in the cytoplasmic Ca2+ concentration ([Ca2+]i) in N1E-115 cells and in HEK 293 cells transfected with either the 5-HT3 A subunit or the 5-HT3 As subunit. 1-(3-chlorophenyl)biguanide 67-72 5-hydroxytryptamine receptor 3A Homo sapiens 230-237 7993957-2 1994 We have assessed whether pretreatment with the 5-HT3 receptor antagonist BRL 46470 (1 mg orally) attenuates the increase in anxiety induced in healthy volunteers by intravenous infusion of m-chlorophenylpiperazine (mCPP: 0.08 mg/kg over 2 min). BRL 46470 73-82 5-hydroxytryptamine receptor 3A Homo sapiens 47-52 7993957-2 1994 We have assessed whether pretreatment with the 5-HT3 receptor antagonist BRL 46470 (1 mg orally) attenuates the increase in anxiety induced in healthy volunteers by intravenous infusion of m-chlorophenylpiperazine (mCPP: 0.08 mg/kg over 2 min). 1-(3-chlorophenyl)piperazine 189-213 5-hydroxytryptamine receptor 3A Homo sapiens 47-52 7993957-2 1994 We have assessed whether pretreatment with the 5-HT3 receptor antagonist BRL 46470 (1 mg orally) attenuates the increase in anxiety induced in healthy volunteers by intravenous infusion of m-chlorophenylpiperazine (mCPP: 0.08 mg/kg over 2 min). 1-(3-chlorophenyl)piperazine 215-219 5-hydroxytryptamine receptor 3A Homo sapiens 47-52 8032707-1 1994 Granisetron, a potent and selective 5-hydroxytryptamine receptor (5-HT3) antagonist was reported to be an effective antiemetic agent both in animal studies and in patients given highly emetogenic chemotherapy. Granisetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 66-71 7919451-1 1994 This review discusses the development and use of 5-hydroxytryptamine3 (5-HT3) antagonists, especially granisetron, for the treatment of chemotherapy-induced emesis. 5-hydroxytryptamine3 49-69 5-hydroxytryptamine receptor 3A Homo sapiens 71-76 7919451-1 1994 This review discusses the development and use of 5-hydroxytryptamine3 (5-HT3) antagonists, especially granisetron, for the treatment of chemotherapy-induced emesis. Granisetron 102-113 5-hydroxytryptamine receptor 3A Homo sapiens 71-76 7919451-3 1994 Granisetron, a new 5-HT3, is approximately 400 times more potent than metoclopramide and, unlike metoclopramide, does not produce extrapyramidal side effects. Granisetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 19-24 7690681-2 1993 Acute phase (0-24 hours after induction of chemotherapy) nausea and vomiting parallels plasma serotonin release, which explains the effectiveness of 5HT3 antagonists; serotonin release in the delayed phase (24-48 hours after induction), during which consistent antiemetic control remains elusive, has not been investigated. Serotonin 94-103 5-hydroxytryptamine receptor 3A Homo sapiens 149-153 8299095-2 1994 Ondansetron is a potent and highly specific antagonist of the 5-HT3 serotonin receptor. Ondansetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 62-86 2138064-2 1990 were given the 5HT3 antagonist Ondansetron (Glaxo) as an antiemetic. Ondansetron 31-42 5-hydroxytryptamine receptor 3A Homo sapiens 15-19 1838490-0 1991 [Ondansetron: a specific 5-HT3 serotonin receptor inhibitor, a new antiemetic in oncology]. Ondansetron 1-12 5-hydroxytryptamine receptor 3A Homo sapiens 25-49 2144721-0 1990 5-HT3 antagonist ondansetron--an effective outpatient antiemetic in cancer treatment. Ondansetron 17-28 5-hydroxytryptamine receptor 3A Homo sapiens 0-5 2144721-1 1990 Thirty children aged 2-16 years with malignant tumours who were receiving chemotherapy were treated with the 5-HT3 antagonist ondansetron. Ondansetron 126-137 5-hydroxytryptamine receptor 3A Homo sapiens 109-114 8347903-4 1993 DATA SYNTHESIS: Ondansetron, a potent and highly selective antagonist of serotonin at the 5-HT3 (subtype 3)-receptor, possesses potent antiemetic effects. Ondansetron 16-27 5-hydroxytryptamine receptor 3A Homo sapiens 90-116 8347903-4 1993 DATA SYNTHESIS: Ondansetron, a potent and highly selective antagonist of serotonin at the 5-HT3 (subtype 3)-receptor, possesses potent antiemetic effects. Serotonin 73-82 5-hydroxytryptamine receptor 3A Homo sapiens 90-116 7678181-7 1993 The effect of serotonin was mediated by 5-HT1A-type serotonin receptors (5-HT1AR) as indicated by mimicry exerted by 5-HT1AR agonists such as 8-OH-DPAT and (+)-ALK, partial antagonism by the 5-HT1AR antagonists pindolol and cyproheptadine, and lack of antagonism by the 5-HT2R antagonist ketanserin or the 5-HT3R antagonist ondansetron. Serotonin 14-23 5-hydroxytryptamine receptor 3A Homo sapiens 306-312 33807811-3 2021 The present study investigated the association of nine polymorphisms in the four 5-hydroxytryptamine receptor (HTR) genes HTR1A, HTR2A, HTR3A, and HTR2C and the gene encoding for the serotonin transporter SLC6A4 with MetS in patients with schizophrenia. Serotonin 81-100 5-hydroxytryptamine receptor 3A Homo sapiens 136-141 1831542-0 1990 Evaluation of the 5HT3 antagonist ondansetron (O) for cocaine (C)-like activity and abuse potential. Ondansetron 34-45 5-hydroxytryptamine receptor 3A Homo sapiens 18-22 33767348-7 2021 To gain further translational insights, we revealed that combined treatment of zonisamide (enhancing the GABAAR-alpha5 signaling) and granisetron (a selective 5-HT3R antagonist) alleviates mental dysfunction and yields a robust reversal of diet-induced obesity by reducing total calorie intake and altering food preference towards a healthy low-fat diet. Zonisamide 79-89 5-hydroxytryptamine receptor 3A Homo sapiens 159-165 33767348-7 2021 To gain further translational insights, we revealed that combined treatment of zonisamide (enhancing the GABAAR-alpha5 signaling) and granisetron (a selective 5-HT3R antagonist) alleviates mental dysfunction and yields a robust reversal of diet-induced obesity by reducing total calorie intake and altering food preference towards a healthy low-fat diet. Granisetron 134-145 5-hydroxytryptamine receptor 3A Homo sapiens 159-165 33807811-3 2021 The present study investigated the association of nine polymorphisms in the four 5-hydroxytryptamine receptor (HTR) genes HTR1A, HTR2A, HTR3A, and HTR2C and the gene encoding for the serotonin transporter SLC6A4 with MetS in patients with schizophrenia. Serotonin 183-192 5-hydroxytryptamine receptor 3A Homo sapiens 136-141 34467765-1 2021 In line with recent clinical trials demonstrating that ondansetron, a 5-HT3 receptor (5-HT3R) antagonist, ameliorates cognitive deficits of schizophrenia and the known procognitive effects of 5-HT6 receptor (5-HT6R) antagonists, we applied the hybridization strategy to design dual-acting 5-HT3/5-HT6R antagonists. Ondansetron 55-66 5-hydroxytryptamine receptor 3A Homo sapiens 70-84 34667294-1 2022 Serotonin type-3 receptor (5-HT3R) antagonists show potential as a treatment for cognitive deficits in schizophrenia. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 27-33 34467765-1 2021 In line with recent clinical trials demonstrating that ondansetron, a 5-HT3 receptor (5-HT3R) antagonist, ameliorates cognitive deficits of schizophrenia and the known procognitive effects of 5-HT6 receptor (5-HT6R) antagonists, we applied the hybridization strategy to design dual-acting 5-HT3/5-HT6R antagonists. Ondansetron 55-66 5-hydroxytryptamine receptor 3A Homo sapiens 86-92 34467765-2 2021 We identified the first-in-class compound FPPQ, which behaves as a 5-HT3R antagonist and a neutral antagonist 5-HT6R of the Gs pathway. FPPQ 42-46 5-hydroxytryptamine receptor 3A Homo sapiens 67-73 34467765-6 2021 Thus, combination of 5-HT3R antagonism and 5-HT6R antagonism, exemplified by FPPQ, contributes to alleviating the positive-like symptoms. FPPQ 77-81 5-hydroxytryptamine receptor 3A Homo sapiens 21-27 34285037-5 2021 CRC cell-originated 5-HT enhanced NLRP3 inflammasome activation in THP-1 cells and immortalized bone marrow-derived macrophages (iBMDM) via its ion channel receptor, HTR3A. Serotonin 20-24 5-hydroxytryptamine receptor 3A Homo sapiens 166-171 2525078-1 1989 The novel 5HT3 receptor antagonist GR38032F was evaluated in the control of emesis induced by the cyclophosphamide analogue ifosfamide. Ondansetron 35-43 5-hydroxytryptamine receptor 3A Homo sapiens 10-14 34202161-4 2021 To discover candidate genes involved in PG neurogenesis, the transcriptome profiling of sacral NC and developing PG was performed, and we identified the enrichment of the type 3 serotonin receptor (5-HT3, encoded by Htr3a and Htr3b). Serotonin 178-187 5-hydroxytryptamine receptor 3A Homo sapiens 216-221 34202161-5 2021 We determined that Htr3a is one of the first serotonin receptor genes that is up-regulated in sacral NC progenitors and is maintained in differentiating PG neurons. Serotonin 45-54 5-hydroxytryptamine receptor 3A Homo sapiens 19-24 34070942-10 2021 Overall, our data suggest that human parietal cells in culture, as well as from the gastric antrum, synthesize serotonin and release it after treatment with L-Arg via an HTR3-related mechanism. Serotonin 111-120 5-hydroxytryptamine receptor 3A Homo sapiens 170-174 34070942-10 2021 Overall, our data suggest that human parietal cells in culture, as well as from the gastric antrum, synthesize serotonin and release it after treatment with L-Arg via an HTR3-related mechanism. Arginine 157-162 5-hydroxytryptamine receptor 3A Homo sapiens 170-174 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 22-31 5-hydroxytryptamine receptor 3A Homo sapiens 140-171 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 22-31 5-hydroxytryptamine receptor 3A Homo sapiens 173-178 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 22-31 5-hydroxytryptamine receptor 3A Homo sapiens 200-204 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 22-31 5-hydroxytryptamine receptor 3A Homo sapiens 277-282 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 33-36 5-hydroxytryptamine receptor 3A Homo sapiens 140-171 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 33-36 5-hydroxytryptamine receptor 3A Homo sapiens 173-178 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 33-36 5-hydroxytryptamine receptor 3A Homo sapiens 200-204 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. Serotonin 33-36 5-hydroxytryptamine receptor 3A Homo sapiens 277-282 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. chromaffin 62-72 5-hydroxytryptamine receptor 3A Homo sapiens 173-178 35614045-3 2022 Here we revealed that serotonin (5HT) controls the numbers of chromaffin cells by acting upon their immediate progenitor "bridge" cells via 5-hydroxytryptamine receptor 3A (HTR3A), and the aggressive HTR3Ahigh human neuroblastoma cell lines reduce proliferation in response to HTR3A-specific agonists. chromaffin 62-72 5-hydroxytryptamine receptor 3A Homo sapiens 200-204 35017671-6 2022 A consistent and robust finding (five studies) was that ondansetron and tropisetron (5HT3 antagonist and alpha7-nicotinic receptor partial agonist) improved sensory gating in patients with schizophrenia. Tropisetron 72-83 5-hydroxytryptamine receptor 3A Homo sapiens 85-89 2529108-1 1989 Antagonists of 5-hydroxytryptamine type 3 (5HT3) receptors reduce the nausea induced by cisplatinum, but the effects of these agents on 5HT3 receptors in the human gut remain to be defined. Cisplatin 88-99 5-hydroxytryptamine receptor 3A Homo sapiens 43-47 35457612-0 2022 Serotonin Receptor HTR3A Gene Polymorphisms rs1985242 and rs1062613, E-Cigarette Use and Personality. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 19-24 35457612-3 2022 In this study we analyzed two polymorphisms-rs1985242 and rs1062613-in the serotonin receptor HTR3A gene in a group of e-cigarette users (n = 135) and controls (n = 106). Serotonin 75-84 5-hydroxytryptamine receptor 3A Homo sapiens 94-99 2525078-1 1989 The novel 5HT3 receptor antagonist GR38032F was evaluated in the control of emesis induced by the cyclophosphamide analogue ifosfamide. Cyclophosphamide 98-114 5-hydroxytryptamine receptor 3A Homo sapiens 10-14 2525078-1 1989 The novel 5HT3 receptor antagonist GR38032F was evaluated in the control of emesis induced by the cyclophosphamide analogue ifosfamide. Ifosfamide 124-134 5-hydroxytryptamine receptor 3A Homo sapiens 10-14 2525078-5 1989 This selective 5HT3 antagonist is effective and safe in the control of ifosfamide-induced emesis, even in patients resistant to high-dose metoclopramide. Ifosfamide 71-81 5-hydroxytryptamine receptor 3A Homo sapiens 15-19 2525078-5 1989 This selective 5HT3 antagonist is effective and safe in the control of ifosfamide-induced emesis, even in patients resistant to high-dose metoclopramide. Metoclopramide 138-152 5-hydroxytryptamine receptor 3A Homo sapiens 15-19 33668306-3 2021 In this study, chanoclavine, which has a ring structure similar to 5-hydroxytryptamine (5-HT), showed an interaction with the 5-HT3A receptor to regulate IBS. chanoclavine 15-27 5-hydroxytryptamine receptor 3A Homo sapiens 126-132 33869168-2 2021 This study was aim to investigate the mechanism of bilirubin in cholestasis mediating pain desensitization through 5-hydroxytryptamine 3A (5-HT3A ) receptor activation in spinal dorsal horn (SDH). Bilirubin 51-60 5-hydroxytryptamine receptor 3A Homo sapiens 139-145 33869168-11 2021 Bilirubin also increased GABA concentrations in CSF and GABAergic spontaneous inhibitory postsynaptic current in spinal cord, and directly induced inward currents in HEK293 cells which were overexpressed 5-HT3A receptor by lentivirus. Bilirubin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 204-210 33869168-12 2021 Conclusion: In conclusion, bilirubin induced pain desensitization in cholestasis by activating 5-HT3A receptor in spinal cord. Bilirubin 27-36 5-hydroxytryptamine receptor 3A Homo sapiens 95-101 33869168-13 2021 The activation of 5-HT3A receptor might regulate pain threshold by acting on the GABA pathway. gamma-Aminobutyric Acid 81-85 5-hydroxytryptamine receptor 3A Homo sapiens 18-24 33668306-3 2021 In this study, chanoclavine, which has a ring structure similar to 5-hydroxytryptamine (5-HT), showed an interaction with the 5-HT3A receptor to regulate IBS. Serotonin 67-86 5-hydroxytryptamine receptor 3A Homo sapiens 126-132 33668306-3 2021 In this study, chanoclavine, which has a ring structure similar to 5-hydroxytryptamine (5-HT), showed an interaction with the 5-HT3A receptor to regulate IBS. Serotonin 88-92 5-hydroxytryptamine receptor 3A Homo sapiens 126-132 33668306-4 2021 Although its derivatives are known to be involved in neurotransmitter receptors, the molecular physiological mechanism of the interaction between chanoclavine and the 5-HT3A receptor is unknown. chanoclavine 146-158 5-hydroxytryptamine receptor 3A Homo sapiens 167-173 33668306-7 2021 The 5-HT3A response induced by 5-HT was blocked by chanoclavine with half-maximal inhibitory response concentration (IC50) values of 107.2 microM. chanoclavine 51-63 5-hydroxytryptamine receptor 3A Homo sapiens 4-10 33668306-8 2021 Docking studies suggested that chanoclavine was positioned close F130 and N138 in the 5-HT3A receptor-binding site. chanoclavine 31-43 5-hydroxytryptamine receptor 3A Homo sapiens 86-92 33668306-8 2021 Docking studies suggested that chanoclavine was positioned close F130 and N138 in the 5-HT3A receptor-binding site. Bis[3-(triethoxysilyl)propyl]tetrasulfide 74-78 5-hydroxytryptamine receptor 3A Homo sapiens 86-92 33668306-13 2021 The results of the electrophysiological studies and of in silico simulation showed that chanoclavine has the potential to inhibit the hypergastric stimulation of the gut by inhibiting the stimulation of signal transduction through 5-HT3A receptor stimulation. chanoclavine 88-100 5-hydroxytryptamine receptor 3A Homo sapiens 231-237 33594077-0 2021 Asymmetric opening of the homopentameric 5-HT3A serotonin receptor in lipid bilayers. Lipid Bilayers 70-84 5-hydroxytryptamine receptor 3A Homo sapiens 41-66 33594077-3 2021 We report three structures of the Cys-loop 5-HT3A serotonin receptor (5HT3R) reconstituted into saposin-based lipid bilayer discs: a symmetric and an asymmetric apo state, and an asymmetric agonist-bound state. Cysteine 34-37 5-hydroxytryptamine receptor 3A Homo sapiens 43-68 33594077-3 2021 We report three structures of the Cys-loop 5-HT3A serotonin receptor (5HT3R) reconstituted into saposin-based lipid bilayer discs: a symmetric and an asymmetric apo state, and an asymmetric agonist-bound state. Cysteine 34-37 5-hydroxytryptamine receptor 3A Homo sapiens 70-75 33594077-3 2021 We report three structures of the Cys-loop 5-HT3A serotonin receptor (5HT3R) reconstituted into saposin-based lipid bilayer discs: a symmetric and an asymmetric apo state, and an asymmetric agonist-bound state. Lipid Bilayers 110-123 5-hydroxytryptamine receptor 3A Homo sapiens 43-68 33594077-3 2021 We report three structures of the Cys-loop 5-HT3A serotonin receptor (5HT3R) reconstituted into saposin-based lipid bilayer discs: a symmetric and an asymmetric apo state, and an asymmetric agonist-bound state. Lipid Bilayers 110-123 5-hydroxytryptamine receptor 3A Homo sapiens 70-75 33419241-6 2020 Palonosetron, a serotonin type 3 receptor (5-hydroxytryptamine receptor 3 (5-HT3R)) antagonist, was identified by both CLUE and FAERS analyses. Palonosetron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 75-81 33555084-3 2021 Here, we analyze the use of NK1 RA-5-HT3 RA-dexamethasone for antiemetic prophylaxis associated with HEC and carboplatin. HEC 101-104 5-hydroxytryptamine receptor 3A Homo sapiens 35-40 33555084-3 2021 Here, we analyze the use of NK1 RA-5-HT3 RA-dexamethasone for antiemetic prophylaxis associated with HEC and carboplatin. Carboplatin 109-120 5-hydroxytryptamine receptor 3A Homo sapiens 35-40 33572981-3 2021 A member of a novel class of antidepressants, vortioxetine, which is a serotonin partial agonist reuptake inhibitor (SPARI), also exhibits a higher affinity for serotonin transporter, serotonin receptors type 1A (5-HT1AR) and type 3 (5-HT3R), and 5-HT7R. Vortioxetine 46-58 5-hydroxytryptamine receptor 3A Homo sapiens 234-240 33572981-3 2021 A member of a novel class of antidepressants, vortioxetine, which is a serotonin partial agonist reuptake inhibitor (SPARI), also exhibits a higher affinity for serotonin transporter, serotonin receptors type 1A (5-HT1AR) and type 3 (5-HT3R), and 5-HT7R. Serotonin 161-170 5-hydroxytryptamine receptor 3A Homo sapiens 234-240 33252737-1 2021 5-hydroxytryptamine receptor subtype 3 (5-HT3R) is a pentameric ligand-gated ion channel (pLGIC) involved in neuronal signaling. Serotonin 0-19 5-hydroxytryptamine receptor 3A Homo sapiens 40-46 32736413-4 2020 HTR3A is the main subunit of 5-hydroxytryptamine 3 (5-HT3) receptors, which are the only ligand-gated ion channels in 7 families of 5-HT receptors. Serotonin 29-48 5-hydroxytryptamine receptor 3A Homo sapiens 0-5 33059577-7 2021 The serotonin type-3 receptors (5-HT3R) are well renowned to be expressed in the central nervous system (CNS) in regions which have significance in the vomiting reflex, perception of pain, the reward system, cognition, depression and anxiety control. Serotonin 4-13 5-hydroxytryptamine receptor 3A Homo sapiens 32-38 33059577-9 2021 The 5-HT3RA inhibit the binding of serotonin to post synaptic 5-HT3R and increase its availability to other receptors like 5-HT1A, 1B and 1D as well as 5-HT2 receptors and produces anti-depressant-like effect. Serotonin 35-44 5-hydroxytryptamine receptor 3A Homo sapiens 4-10 32946769-9 2020 Thus, our kinetic analysis revealed that terpenoids are efficacious agonists for 5-HT3A receptors. Terpenes 41-51 5-hydroxytryptamine receptor 3A Homo sapiens 81-87 32736413-4 2020 HTR3A is the main subunit of 5-hydroxytryptamine 3 (5-HT3) receptors, which are the only ligand-gated ion channels in 7 families of 5-HT receptors. Serotonin 52-56 5-hydroxytryptamine receptor 3A Homo sapiens 0-5 32336093-2 2020 Using a simplified model of the pore of the 5HT3 receptor (5HT3R) which restrains the backbone structure to that of the parent channel protein from which it is derived we compare additive with polarizable models in describing the behavior of water in nanopores. Water 242-247 5-hydroxytryptamine receptor 3A Homo sapiens 44-57 32899016-2 2020 The Bezold-Jarisch reflex, causing postspinal hypotension, has been shown to be antagonized by serotonin type 3 (5-HT3) blockade. Serotonin 95-104 5-hydroxytryptamine receptor 3A Homo sapiens 113-118 32899016-3 2020 Our aim was to assess if routine prophylactic administration of the 5-HT3 antagonist ondansetron (ODS) attenuates postspinal change in maternal blood pressure.Elective CS under SpA were retrospectively analyzed. Ondansetron 85-96 5-hydroxytryptamine receptor 3A Homo sapiens 68-73 32479847-2 2020 In addition to its potent antioxidant effects, agmatine is an endogenous neuromodulator and has wide spectrum molecular actions on different receptor subtypes (NMDA, Imidazoline 1-2, alpha-2 adrenoreceptor, 5-HT2a, 5-HT3) and cellular signaling pathways (MAPK, PKA, NO, BDNF). Agmatine 47-55 5-hydroxytryptamine receptor 3A Homo sapiens 215-220 33315977-2 2020 Several studies have also shown that changes in serotonin receptors, especially 5HTR2A and 5HTR3A, can play an important role in incidence of cancers. Serotonin 48-57 5-hydroxytryptamine receptor 3A Homo sapiens 92-97 33315977-11 2020 Conclusion: The results indicated an increase in the mRNA expression of serotonin receptors (5HTR2A and 5HTR3A) in the tumor tissue compared to the marginal zone, which due to the mitogenic nature of these receptors, is likely to induce more proliferation of cancer cells. Serotonin 72-81 5-hydroxytryptamine receptor 3A Homo sapiens 105-110 32130678-7 2020 Luciferase reporter assay and biotin-avidin pull-down assay showed miR-1256 can directly target 5-hydroxytryptamine receptor 3A (HTR3A) in PTC cells. Biotin 30-36 5-hydroxytryptamine receptor 3A Homo sapiens 96-127 32130678-7 2020 Luciferase reporter assay and biotin-avidin pull-down assay showed miR-1256 can directly target 5-hydroxytryptamine receptor 3A (HTR3A) in PTC cells. Biotin 30-36 5-hydroxytryptamine receptor 3A Homo sapiens 129-134 32336093-2 2020 Using a simplified model of the pore of the 5HT3 receptor (5HT3R) which restrains the backbone structure to that of the parent channel protein from which it is derived we compare additive with polarizable models in describing the behavior of water in nanopores. Water 242-247 5-hydroxytryptamine receptor 3A Homo sapiens 59-64 32250181-1 2020 Ondansetron HCl is a (5-HT3) serotonin receptor antagonist, used as anti-emetic drug in combination with anticancer agents. Ondansetron 0-15 5-hydroxytryptamine receptor 3A Homo sapiens 22-47 32431598-5 2020 Also, macromolecular docking followed by 100 ns molecular dynamics (MD) simulations suggested that the interaction energy of the P2X4 receptor with 5-HT3A receptor is similar at the holo and the apo state of the P2X4 receptor, and the interacting 5-HT3A receptor decreased the ATP binding energy of P2X4 receptor. Adenosine Triphosphate 277-280 5-hydroxytryptamine receptor 3A Homo sapiens 148-154 32390801-4 2020 Methods: A set of 29 SNPs of genes of serotonin receptors HTR1A, HTR1B, HTR2A, HTR2C, HTR3A, HTR3B, and HTR6 was studied in a population of 449 Caucasians (226 females and 223 males) with verified clinical diagnosis of schizophrenia (according to ICD-10: F20). Serotonin 38-47 5-hydroxytryptamine receptor 3A Homo sapiens 86-91 31868947-3 2020 Several studies have related polymorphisms (SNPs) in the serotonin receptor-3 (HTR3) genes to be associated with pain modulation and endogenous pain suppression. Serotonin 57-66 5-hydroxytryptamine receptor 3A Homo sapiens 79-83 31868947-5 2020 Here, we investigated the effect of a 5"UTR SNP in the serotonergic receptor HTR3A gene (rs1062613) on striatal dopamine D2/D3 receptor (DRD2) availability and reward-associated DA release in response to unpredictable monetary rewards in 23 women with FMS and 17 age-matched healthy female controls. Dopamine 178-180 5-hydroxytryptamine receptor 3A Homo sapiens 77-82 31835640-1 2019 Vortioxetine is a novel, multimodal antidepressant with unique targets, including the inhibition of the serotonin transporter (SET), of serotonin 5-HT3 (5-HT3R), and of 5-HT7 (5-HT7R) receptors and partial agonism to serotonin 5-HT1A (5-HT1AR) receptors in humans. Vortioxetine 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 146-151 31873866-3 2020 The 5-hydroxytryptamine (5-HT) receptor 3 antagonist alosetron is approved for women only since it largely lacks efficacy in men. alosetron 53-62 5-hydroxytryptamine receptor 3A Homo sapiens 4-41 31871207-0 2020 Microsecond-timescale simulations suggest 5-HT-mediated preactivation of the 5-HT3A serotonin receptor. Serotonin 42-46 5-hydroxytryptamine receptor 3A Homo sapiens 77-83 31871207-0 2020 Microsecond-timescale simulations suggest 5-HT-mediated preactivation of the 5-HT3A serotonin receptor. Serotonin 84-93 5-hydroxytryptamine receptor 3A Homo sapiens 77-83 31871207-3 2020 Here, we perform multiple all-atom MD simulations of the homomeric 5-hydroxytryptamine 3A (5-HT3A) serotonin receptor for 15 to 20 mus to demonstrate that such timescales are critical to observe the equilibration of a pLGIC from its crystalized conformation to a membrane-bound conformation. Serotonin 67-86 5-hydroxytryptamine receptor 3A Homo sapiens 91-97 31871207-3 2020 Here, we perform multiple all-atom MD simulations of the homomeric 5-hydroxytryptamine 3A (5-HT3A) serotonin receptor for 15 to 20 mus to demonstrate that such timescales are critical to observe the equilibration of a pLGIC from its crystalized conformation to a membrane-bound conformation. Serotonin 99-108 5-hydroxytryptamine receptor 3A Homo sapiens 91-97 31871207-4 2020 These timescales, which are an order of magnitude longer than any previous simulation of 5-HT3A, allow us to observe the dynamic binding and unbinding of 5-hydroxytryptamine (5-HT) (i.e., serotonin) to the binding pocket located on the extracellular domain (ECD) and allosteric regulation of the transmembrane domain (TMD) from synergistic 5-HT binding. Serotonin 154-173 5-hydroxytryptamine receptor 3A Homo sapiens 89-95 31871207-4 2020 These timescales, which are an order of magnitude longer than any previous simulation of 5-HT3A, allow us to observe the dynamic binding and unbinding of 5-hydroxytryptamine (5-HT) (i.e., serotonin) to the binding pocket located on the extracellular domain (ECD) and allosteric regulation of the transmembrane domain (TMD) from synergistic 5-HT binding. Serotonin 188-197 5-hydroxytryptamine receptor 3A Homo sapiens 89-95 31871207-4 2020 These timescales, which are an order of magnitude longer than any previous simulation of 5-HT3A, allow us to observe the dynamic binding and unbinding of 5-hydroxytryptamine (5-HT) (i.e., serotonin) to the binding pocket located on the extracellular domain (ECD) and allosteric regulation of the transmembrane domain (TMD) from synergistic 5-HT binding. Serotonin 175-179 5-hydroxytryptamine receptor 3A Homo sapiens 89-95 32616964-0 2020 X-Ray Crystal Structure of a 2-Amino-3,4-dihydroquinazoline 5-HT3 Serotonin Receptor Antagonist and Related Analogs. 1,4-dihydroquinazolin-2-amine 29-59 5-hydroxytryptamine receptor 3A Homo sapiens 60-84 31835640-1 2019 Vortioxetine is a novel, multimodal antidepressant with unique targets, including the inhibition of the serotonin transporter (SET), of serotonin 5-HT3 (5-HT3R), and of 5-HT7 (5-HT7R) receptors and partial agonism to serotonin 5-HT1A (5-HT1AR) receptors in humans. Vortioxetine 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 153-159 31582575-5 2019 In the present study, we used voltage-clamp fluorometry (VCF) to measure conformational changes in regions surrounding the orthosteric binding site of the human 5-HT3A (h5-HT3A) receptor during binding of 5-HT and different classes of 5-HT3 receptor ligands. Serotonin 161-165 5-hydroxytryptamine receptor 3A Homo sapiens 170-176 30992726-5 2019 In the presented work, we summarize the synthesis, photochromic properties and in vitro characterization of azobenzene-based photochromic derivatives of published 5-HT3R antagonists. azobenzene 108-118 5-hydroxytryptamine receptor 3A Homo sapiens 163-169 31409663-0 2019 Triple arginines as molecular determinants for pentameric assembly of the intracellular domain of 5-HT3A receptors. Arginine 7-16 5-hydroxytryptamine receptor 3A Homo sapiens 98-104 30797147-0 2019 Potential roles of 5-HT3 receptor (5-HT3R) antagonists in modulating the effects of nicotine. Nicotine 84-92 5-hydroxytryptamine receptor 3A Homo sapiens 19-33 30797147-0 2019 Potential roles of 5-HT3 receptor (5-HT3R) antagonists in modulating the effects of nicotine. Nicotine 84-92 5-hydroxytryptamine receptor 3A Homo sapiens 35-41 30797147-1 2019 5-HT3R antagonists such as ondansetron, granisetron and tropisetron have been clinically used to treat nausea and vomiting in chemotherapy patients. Ondansetron 27-38 5-hydroxytryptamine receptor 3A Homo sapiens 0-6 30797147-1 2019 5-HT3R antagonists such as ondansetron, granisetron and tropisetron have been clinically used to treat nausea and vomiting in chemotherapy patients. Granisetron 40-51 5-hydroxytryptamine receptor 3A Homo sapiens 0-6 30797147-1 2019 5-HT3R antagonists such as ondansetron, granisetron and tropisetron have been clinically used to treat nausea and vomiting in chemotherapy patients. Tropisetron 56-67 5-hydroxytryptamine receptor 3A Homo sapiens 0-6 30797147-5 2019 This review gathered existing studies conducted investigating the potential of "-setron" class of 5-HT3R antagonists in modulating nicotine effects. Nicotine 131-139 5-hydroxytryptamine receptor 3A Homo sapiens 98-104 30797147-6 2019 We proposed that the mechanism where 5-HT3R antagonists mediate the effects of nicotine could be attributed by both direct at 5-HT3R and indirect mechanism in nicotine addiction downstream regulation. Nicotine 79-87 5-hydroxytryptamine receptor 3A Homo sapiens 37-43 30797147-6 2019 We proposed that the mechanism where 5-HT3R antagonists mediate the effects of nicotine could be attributed by both direct at 5-HT3R and indirect mechanism in nicotine addiction downstream regulation. Nicotine 79-87 5-hydroxytryptamine receptor 3A Homo sapiens 126-132 30797147-6 2019 We proposed that the mechanism where 5-HT3R antagonists mediate the effects of nicotine could be attributed by both direct at 5-HT3R and indirect mechanism in nicotine addiction downstream regulation. Nicotine 159-167 5-hydroxytryptamine receptor 3A Homo sapiens 37-43 28869563-8 2017 The representative putative targets of the alkaloids are inflammation-related proteins (MAPK14, PTGS2, PTGS2, and F2) and pruritus-related proteins (HRH1, TRPA1, HTR3A, and HTR6). Alkaloids 43-52 5-hydroxytryptamine receptor 3A Homo sapiens 162-167 30317998-1 2019 BACKGROUND: Vortioxetine is a multimodal antidepressant drug with combined effects on SERT as an inhibitor, 5-HT1A as agonist and 5-HT3A as an antagonist. Vortioxetine 12-24 5-hydroxytryptamine receptor 3A Homo sapiens 130-136 30317998-2 2019 Series of vortioxetine analogs have been reported as multi antidepressant compounds and they block serotonin transport into the neuronal cells, activate the postsynaptic 5-HT1A receptors and eliminate the low activity of 5-HT3A receptors. Vortioxetine 10-22 5-hydroxytryptamine receptor 3A Homo sapiens 221-227 30405756-4 2018 HTR3A was then knocked down via a lentivirus-mediated shRNA system to detect the effect of HTR3A silencing on cell proliferation and apoptosis by MTT, colony formation, flow cytometry and western blotting assays in CRC. monooxyethylene trimethylolpropane tristearate 146-149 5-hydroxytryptamine receptor 3A Homo sapiens 91-96 29508995-5 2018 Examination of a range of receptor modulators, including ethanol, thymol, 5-hydroxyindole, and 5-chloroindole, which can affect the 5-HT3A receptor and ELIC, suggest that these compounds act via the transmembrane domain, except for 5-hydroxyindole, which can compete with 5-HT at the orthosteric binding site. Ethanol 57-64 5-hydroxytryptamine receptor 3A Homo sapiens 132-138 29508995-5 2018 Examination of a range of receptor modulators, including ethanol, thymol, 5-hydroxyindole, and 5-chloroindole, which can affect the 5-HT3A receptor and ELIC, suggest that these compounds act via the transmembrane domain, except for 5-hydroxyindole, which can compete with 5-HT at the orthosteric binding site. Thymol 66-72 5-hydroxytryptamine receptor 3A Homo sapiens 132-138 29508995-5 2018 Examination of a range of receptor modulators, including ethanol, thymol, 5-hydroxyindole, and 5-chloroindole, which can affect the 5-HT3A receptor and ELIC, suggest that these compounds act via the transmembrane domain, except for 5-hydroxyindole, which can compete with 5-HT at the orthosteric binding site. 5-hydroxyindole 74-89 5-hydroxytryptamine receptor 3A Homo sapiens 132-138 29508995-5 2018 Examination of a range of receptor modulators, including ethanol, thymol, 5-hydroxyindole, and 5-chloroindole, which can affect the 5-HT3A receptor and ELIC, suggest that these compounds act via the transmembrane domain, except for 5-hydroxyindole, which can compete with 5-HT at the orthosteric binding site. 5-chloroindole 95-109 5-hydroxytryptamine receptor 3A Homo sapiens 132-138 29508995-5 2018 Examination of a range of receptor modulators, including ethanol, thymol, 5-hydroxyindole, and 5-chloroindole, which can affect the 5-HT3A receptor and ELIC, suggest that these compounds act via the transmembrane domain, except for 5-hydroxyindole, which can compete with 5-HT at the orthosteric binding site. 5-hydroxyindole 232-247 5-hydroxytryptamine receptor 3A Homo sapiens 132-138 29508995-6 2018 The data throw further light on the importance of coupling interface in Cys-loop receptors and provide a platform for examining the mechanism of action of compounds that act in the extracellular domain of the 5-HT3A receptor and the transmembrane domain of ELIC. Cysteine 72-75 5-hydroxytryptamine receptor 3A Homo sapiens 209-215 29620694-3 2018 The aim of this study was to determine whether genetic variations in the genes encoding muscarinic and serotonergic receptors (CHRM2, CHRM3, HTR2, HTR3, HTR4, and HTR7) explain the variations in incidence of constipation and anticholinergic symptoms during clozapine treatment. Clozapine 257-266 5-hydroxytryptamine receptor 3A Homo sapiens 147-151 29448118-9 2018 L-type calcium channel blocking antihypertensives (CCBs), were associated with a 3.18 mg/dL (95% CI -6.18 to -0.18) decrease in glucose during GTT, and serotonin receptor type 3 (5HT-3) antagonist antinausea medications were associated with a 3.54 mg/dL (95% CI 1.86-5.23) increase in glucose during GTT. ccbs 51-55 5-hydroxytryptamine receptor 3A Homo sapiens 152-184 30257860-0 2018 Modeling and Mutational Analysis of the Binding Mode for the Multimodal Antidepressant Drug Vortioxetine to the Human 5-HT3A Receptor. Vortioxetine 92-104 5-hydroxytryptamine receptor 3A Homo sapiens 118-124 30257860-6 2018 We have investigated the binding mode of vortioxetine at the human 5-HT3A receptor through computational and in vitro experiments to provide insight into the molecular mechanisms behind the unique pharmacological profile of the drug. Vortioxetine 41-53 5-hydroxytryptamine receptor 3A Homo sapiens 67-73 29972203-7 2018 The CML-induced serotonin release was reduced by the HTR3 antagonist granisetron. Serotonin 16-25 5-hydroxytryptamine receptor 3A Homo sapiens 53-57 29972203-7 2018 The CML-induced serotonin release was reduced by the HTR3 antagonist granisetron. Granisetron 69-80 5-hydroxytryptamine receptor 3A Homo sapiens 53-57 28439104-3 2018 In this study, we show that a serotonin type 3 receptor (5HT3R) agonist induces antidepressant effects as well as hippocampal neurogenesis independent of fluoxetine (a commonly used SSRI). Fluoxetine 154-164 5-hydroxytryptamine receptor 3A Homo sapiens 30-62 28615161-10 2017 Decreasing the glucose concentration also decreased both basal and 5-HT3R agonist-induced increase in the frequency of spontaneous glutamate inputs onto NTS-CA neurons. Glucose 15-22 5-hydroxytryptamine receptor 3A Homo sapiens 67-73 28615161-10 2017 Decreasing the glucose concentration also decreased both basal and 5-HT3R agonist-induced increase in the frequency of spontaneous glutamate inputs onto NTS-CA neurons. Glutamic Acid 131-140 5-hydroxytryptamine receptor 3A Homo sapiens 67-73 28948091-0 2017 Successful treatment with risperidone increases 5-HT 3A receptor gene expression in patients with paranoid schizophrenia - data from a prospective study. Risperidone 26-37 5-hydroxytryptamine receptor 3A Homo sapiens 48-55 28948091-1 2017 INTRODUCTION: The relationship between peripheral 5-HT3A receptor mRNA level and risperidone efficiency in paranoid schizophrenia patients is still unknown. Risperidone 81-92 5-hydroxytryptamine receptor 3A Homo sapiens 50-56 28948091-9 2017 CONCLUSIONS: Successful treatment with risperidone increases 5-HT3A receptor gene expression in patients with paranoid schizophrenia, indicating that 5-HT3A receptor may be involved in the mechanism of risperidone effect. Risperidone 39-50 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 28948091-9 2017 CONCLUSIONS: Successful treatment with risperidone increases 5-HT3A receptor gene expression in patients with paranoid schizophrenia, indicating that 5-HT3A receptor may be involved in the mechanism of risperidone effect. Risperidone 39-50 5-hydroxytryptamine receptor 3A Homo sapiens 150-156 28948091-9 2017 CONCLUSIONS: Successful treatment with risperidone increases 5-HT3A receptor gene expression in patients with paranoid schizophrenia, indicating that 5-HT3A receptor may be involved in the mechanism of risperidone effect. Risperidone 202-213 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 28948091-9 2017 CONCLUSIONS: Successful treatment with risperidone increases 5-HT3A receptor gene expression in patients with paranoid schizophrenia, indicating that 5-HT3A receptor may be involved in the mechanism of risperidone effect. Risperidone 202-213 5-hydroxytryptamine receptor 3A Homo sapiens 150-156 27874067-7 2016 Moreover, activation of 5-HTR3 and 5-HTR4 both significantly inhibited the opening of mPTP. 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine 86-90 5-hydroxytryptamine receptor 3A Homo sapiens 26-30 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 5-hydroxytryptamine receptor 3A Homo sapiens 118-142 27926574-4 2017 Serotonin in mammal species has multiple neural markers, including receptors (5-HT1-7), serotonin transporter, and volume transmission, which are present in brain areas involved in memory. Serotonin 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 78-85 27816366-3 2017 5-Hydroxytryptamine receptor 3 (5-HT3) antagonists like ondansetron and ramosetron are commonly used for preventing PONV, but the optimal choice remains unclear. Ondansetron 56-67 5-hydroxytryptamine receptor 3A Homo sapiens 0-30 27816366-3 2017 5-Hydroxytryptamine receptor 3 (5-HT3) antagonists like ondansetron and ramosetron are commonly used for preventing PONV, but the optimal choice remains unclear. ramosetron 72-82 5-hydroxytryptamine receptor 3A Homo sapiens 0-30 27866853-4 2016 Using the serotonin receptor (5-HT3R) structure as an example, we demonstrate the use of molecular dynamics to aid the functional annotation of channel structures via simulation of the behavior of water within the pore. Water 197-202 5-hydroxytryptamine receptor 3A Homo sapiens 30-36 28002447-9 2016 Women carrying the C/T & T/T (HTR3A) genotype had less reduction of pain intensity (P = 0.041) and area (P = 0.005), and women with the C/C genotype (HTR3B) had less reduction of pain intensity (P = 0.030), duration (P = 0.030) and area compared to men (P = 0.017). Adenosine Monophosphate 24-27 5-hydroxytryptamine receptor 3A Homo sapiens 34-39 27870735-9 2016 CONCLUSION: Combination of a 5-HT3 receptor antagonist and dexamethasone is significantly more effective than 5-HT3 antagonist alone in preventing PONV after laparoscopic surgeries, with possible improvement in postoperative analgesia. Dexamethasone 59-72 5-hydroxytryptamine receptor 3A Homo sapiens 110-115 27677804-0 2016 Novel mechanism of modulation at a ligand-gated ion channel; action of 5-Cl-indole at the 5-HT3 A receptor. 5-cl-indole 71-82 5-hydroxytryptamine receptor 3A Homo sapiens 90-97 27677804-3 2016 We have investigated the pharmacological action of Cl-indole upon the 5-HT3 A receptor and identified that this positive allosteric modulator possesses a novel mechanism of action for LGICs. cl-indole 51-60 5-hydroxytryptamine receptor 3A Homo sapiens 70-77 27677804-6 2016 However, in the presence of Cl-indole, termination of 5-HT application revealed tail currents mediated via the 5-HT3 A receptor that were independent of the preceding 5-HT concentration but were antagonized by the 5-HT3 receptor antagonist, ondansetron. cl-indole 28-37 5-hydroxytryptamine receptor 3A Homo sapiens 111-118 27677804-6 2016 However, in the presence of Cl-indole, termination of 5-HT application revealed tail currents mediated via the 5-HT3 A receptor that were independent of the preceding 5-HT concentration but were antagonized by the 5-HT3 receptor antagonist, ondansetron. Ondansetron 241-252 5-hydroxytryptamine receptor 3A Homo sapiens 111-118 27677804-8 2016 Furthermore, the presence of 5-HT revealed a concentration-dependent increase in the affinity of Cl-indole for the orthosteric binding site of the human 5-HT3 A receptor. cl-indole 97-106 5-hydroxytryptamine receptor 3A Homo sapiens 153-160 27144979-0 2016 The association of HTR3A mRNA expression and craving in Han Chinese alcohol-dependent patients: a preliminary study. Alcohols 68-75 5-hydroxytryptamine receptor 3A Homo sapiens 19-24 27144979-8 2016 RESULTS: HTR3A mRNA expression levels and acetylation levels of H3K9 in the HTR3A promoter region were significantly higher in the alcohol-dependent patients. Alcohols 131-138 5-hydroxytryptamine receptor 3A Homo sapiens 9-14 27144979-8 2016 RESULTS: HTR3A mRNA expression levels and acetylation levels of H3K9 in the HTR3A promoter region were significantly higher in the alcohol-dependent patients. Alcohols 131-138 5-hydroxytryptamine receptor 3A Homo sapiens 76-81 27144979-11 2016 CONCLUSION: The current findings suggest that HTR3A mRNA expression levels were positively correlated with craving in Han Chinese alcohol-dependent patients. Alcohols 130-137 5-hydroxytryptamine receptor 3A Homo sapiens 46-51 26869399-5 2016 Our results indicate that DPA is an allosteric modulator of GABArho1 receptors with an IC50 of 1.6 microM, an enhancer of alpha7 nicotinic receptors at relatively high concentrations of DPA, and has little, if any, effect on 5-HT3A receptors. dipicrylamine 26-29 5-hydroxytryptamine receptor 3A Homo sapiens 225-231 27050932-4 2016 Vortioxetine (VRX) is a multimodal antidepressant with a unique mechanism of action, by acting as 5-HT3A, 5-HT1D and 5-HT7 receptor antagonist, partial agonist at the 5-HT1A and 5-HT1B receptors and inhibitor at the 5-HT transporter. Vortioxetine 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 98-104 27050932-4 2016 Vortioxetine (VRX) is a multimodal antidepressant with a unique mechanism of action, by acting as 5-HT3A, 5-HT1D and 5-HT7 receptor antagonist, partial agonist at the 5-HT1A and 5-HT1B receptors and inhibitor at the 5-HT transporter. Vortioxetine 14-17 5-hydroxytryptamine receptor 3A Homo sapiens 98-104 27044837-3 2016 In brain, Zn(2+) has been identified as a ligand, capable of activating and inhibiting the receptors including the NMDA-type glutamate receptors (NMDARs), GABAA receptors, nicotinic acetylcholine receptors (nAChRs), glycine receptors (glyR) and serotonin receptors (5-HT3). Zinc 10-12 5-hydroxytryptamine receptor 3A Homo sapiens 266-272 26869399-8 2016 In silico modeling of DPA docking to GABArho1, alpha7 nicotinic, and 5-HT3A receptors suggests that a hydrophobic pocket within the Cys-loop and the M4 segment in GABArho1, located at the extracellular/membrane interface, facilitates the interaction with DPA that leads to inhibition of the receptor. dipicrylamine 22-25 5-hydroxytryptamine receptor 3A Homo sapiens 69-75 26869399-8 2016 In silico modeling of DPA docking to GABArho1, alpha7 nicotinic, and 5-HT3A receptors suggests that a hydrophobic pocket within the Cys-loop and the M4 segment in GABArho1, located at the extracellular/membrane interface, facilitates the interaction with DPA that leads to inhibition of the receptor. Cysteine 132-135 5-hydroxytryptamine receptor 3A Homo sapiens 69-75 26456648-5 2015 Whereas the action of all of these substances is well described, less is known about the effect of terpenoids or fragrances on 5-HT3A receptors. Terpenes 99-109 5-hydroxytryptamine receptor 3A Homo sapiens 127-133 26701104-0 2015 Influence of the 5-HT3A Receptor Gene Polymorphism and Childhood Sexual Trauma on Central Serotonin Activity. Serotonin 90-99 5-hydroxytryptamine receptor 3A Homo sapiens 17-23 26576669-10 2016 Selective 5-HT3R antagonists (ondansetron, tropisetron and granisetron) showed positive results on negative symptoms and/or cognitive impairments in phase II trials. Ondansetron 30-41 5-hydroxytryptamine receptor 3A Homo sapiens 10-16 26576669-10 2016 Selective 5-HT3R antagonists (ondansetron, tropisetron and granisetron) showed positive results on negative symptoms and/or cognitive impairments in phase II trials. Tropisetron 43-54 5-hydroxytryptamine receptor 3A Homo sapiens 10-16 26576669-10 2016 Selective 5-HT3R antagonists (ondansetron, tropisetron and granisetron) showed positive results on negative symptoms and/or cognitive impairments in phase II trials. Granisetron 59-70 5-hydroxytryptamine receptor 3A Homo sapiens 10-16 26456648-8 2015 A screening of two odorous mixes containing a total of 200 substances revealed that the monoterpenes, thymol and carvacrol, act as both weak partial agonists and positive modulators on the 5-HT3A receptor. Monoterpenes 88-100 5-hydroxytryptamine receptor 3A Homo sapiens 189-195 26456648-8 2015 A screening of two odorous mixes containing a total of 200 substances revealed that the monoterpenes, thymol and carvacrol, act as both weak partial agonists and positive modulators on the 5-HT3A receptor. Thymol 102-108 5-hydroxytryptamine receptor 3A Homo sapiens 189-195 26456648-8 2015 A screening of two odorous mixes containing a total of 200 substances revealed that the monoterpenes, thymol and carvacrol, act as both weak partial agonists and positive modulators on the 5-HT3A receptor. carvacrol 113-122 5-hydroxytryptamine receptor 3A Homo sapiens 189-195 26456648-10 2015 In our study, we identified new modulators of 5-HT3A receptors out of the classes of monoterpenes and vanilloid substances that frequently occur in various plants. Monoterpenes 85-97 5-hydroxytryptamine receptor 3A Homo sapiens 46-52 26456648-10 2015 In our study, we identified new modulators of 5-HT3A receptors out of the classes of monoterpenes and vanilloid substances that frequently occur in various plants. Capsaicin 102-111 5-hydroxytryptamine receptor 3A Homo sapiens 46-52 25277140-3 2014 Here we examine the effects of proguanil and its metabolites on the electrophysiology and ligand-binding properties of human 5-HT3A receptors expressed in Xenopus oocytes and human embryonic kidney 293 cells, respectively. Proguanil 31-40 5-hydroxytryptamine receptor 3A Homo sapiens 125-131 26073329-2 2015 METHODS: Codon-optimized cDNA of human 5-HT3A was inserted into a modified BacMam vector, which contained an IgG leader sequence, an 8xHis tag linked with two-Maltose Binding Proteins (MBP), and a TEV protease cleavage site. Maltose 159-166 5-hydroxytryptamine receptor 3A Homo sapiens 39-45 26073329-3 2015 The BacMam construct was used to generate baculoviruses for expression of 5-HT3A in HEK293F cells. bacmam 4-10 5-hydroxytryptamine receptor 3A Homo sapiens 74-80 26073329-9 2015 RESULTS: The BacMam system yielded 0.5 milligram of the human 5-HT3A receptor per liter of cells. bacmam 13-19 5-hydroxytryptamine receptor 3A Homo sapiens 62-68 25948478-7 2015 Br-IQ17B is selective over other subtypes such as alpha4beta2 and alpha3beta4, but it blocks 5-HT3A receptors. br-iq17b 0-8 5-hydroxytryptamine receptor 3A Homo sapiens 93-99 25863270-0 2015 Fast and slow interactions of n-alkanols with human 5-HT3A receptors: Implications for anesthetic mechanisms. n-alkanols 30-40 5-hydroxytryptamine receptor 3A Homo sapiens 52-58 25428414-2 2015 To identify biomarkers predicting effectiveness of the 5-HT3 R antagonist (ramosetron) in IBS-D. METHODS: Irritable bowel syndrome-D Japanese subjects received 2.5 or 5 mug of ramosetron once daily for 4 weeks. ramosetron 75-85 5-hydroxytryptamine receptor 3A Homo sapiens 55-62 26565961-5 2015 Facilitation of pain behaviour induced by GAL in the DMH was reversed by lidocaine in the DRt and by ondansetron, a 5HT3R antagonist, in the spinal cord. Dimenhydrinate 53-56 5-hydroxytryptamine receptor 3A Homo sapiens 116-121 26565961-5 2015 Facilitation of pain behaviour induced by GAL in the DMH was reversed by lidocaine in the DRt and by ondansetron, a 5HT3R antagonist, in the spinal cord. Ondansetron 101-112 5-hydroxytryptamine receptor 3A Homo sapiens 116-121 25485645-0 2015 The effects of varenicline on sensory gating and exploratory behavior with pretreatment with nicotinic or 5-HT3A receptor antagonists. Varenicline 15-26 5-hydroxytryptamine receptor 3A Homo sapiens 106-112 25485645-3 2015 Varenicline, a nonselective neuronal nicotinic receptor (NNR) agonist and full agonist of 5-HT3A receptors, helps reduce smoking among schizophrenic patients. Varenicline 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 90-96 25485645-8 2015 Collectively, these results indicate that varenicline at low-to-moderate doses may be beneficial against impaired sensory gating in schizophrenia; however, higher doses may induce anxiogenic effects, which can be prevented with antagonists of NNRs or 5-HT3A receptors. Varenicline 42-53 5-hydroxytryptamine receptor 3A Homo sapiens 251-257 25409778-2 2014 Here we show that the ionotropic serotonin receptor 3A (5-HT(3A)R) is specifically expressed in CGE-derived migrating interneurons and upregulated while they invade the developing cortex. Clopidogrel 96-99 5-hydroxytryptamine receptor 3A Homo sapiens 33-54 25409778-2 2014 Here we show that the ionotropic serotonin receptor 3A (5-HT(3A)R) is specifically expressed in CGE-derived migrating interneurons and upregulated while they invade the developing cortex. Clopidogrel 96-99 5-hydroxytryptamine receptor 3A Homo sapiens 56-63 22458709-1 2014 5-hydroxytryptamine 3 (5HT3) receptors are important modulators of mesostriatal dopaminergic transmission and have been implicated in the pathophysiology of cocaine reward, withdrawal and self-administration. Cocaine 157-164 5-hydroxytryptamine receptor 3A Homo sapiens 23-27 24590579-0 2014 Direct effects of morphine but not of fentanyl-type opioids on human 5-HT3A receptors in outside-out patch-clamp studies. Morphine 18-26 5-hydroxytryptamine receptor 3A Homo sapiens 69-75 24590579-4 2014 Therefore, this study focuses on the interaction of morphine and fentanyl-type opioids (alfentanil, remifentanil and sufentanil) with 5-HT3A receptors. Morphine 52-60 5-hydroxytryptamine receptor 3A Homo sapiens 134-140 24590579-4 2014 Therefore, this study focuses on the interaction of morphine and fentanyl-type opioids (alfentanil, remifentanil and sufentanil) with 5-HT3A receptors. Fentanyl 65-73 5-hydroxytryptamine receptor 3A Homo sapiens 134-140 24590579-4 2014 Therefore, this study focuses on the interaction of morphine and fentanyl-type opioids (alfentanil, remifentanil and sufentanil) with 5-HT3A receptors. Alfentanil 88-98 5-hydroxytryptamine receptor 3A Homo sapiens 134-140 24590579-4 2014 Therefore, this study focuses on the interaction of morphine and fentanyl-type opioids (alfentanil, remifentanil and sufentanil) with 5-HT3A receptors. Remifentanil 100-112 5-hydroxytryptamine receptor 3A Homo sapiens 134-140 24590579-4 2014 Therefore, this study focuses on the interaction of morphine and fentanyl-type opioids (alfentanil, remifentanil and sufentanil) with 5-HT3A receptors. Sufentanil 117-127 5-hydroxytryptamine receptor 3A Homo sapiens 134-140 24590579-11 2014 CONCLUSIONS: Morphine is an opioid compound exhibiting special antagonistic interaction with 5-HT3A receptors. Morphine 13-21 5-hydroxytryptamine receptor 3A Homo sapiens 93-99 25238823-5 2014 The expression of enzymes involved in 5HT synthesis and their receptors varied markedly in beta-pancreatic cells during pregnancy, in parallel with an increase in their insulin secretion potential (probably through the action of Htr3a) and an increase in beta-cell mass (through the action of Htr2b and Htr1d). Serotonin 38-41 5-hydroxytryptamine receptor 3A Homo sapiens 229-234 24283776-1 2014 BACKGROUND AND PURPOSE: It has been proposed that arginine residues lining the intracellular portals of the homomeric 5-HT3 A receptor cause electrostatic repulsion of cation flow, accounting for a single-channel conductance substantially lower than that of the 5-HT3 AB heteromer. Arginine 50-58 5-hydroxytryptamine receptor 3A Homo sapiens 118-125 24283776-3 2014 EXPERIMENTAL APPROACH: Mutations were introduced into the portal region of the human 5-HT3 A homopentamer, such that putative salt bridges were broken by neutralizing anionic partners. Salts 126-130 5-hydroxytryptamine receptor 3A Homo sapiens 85-92 22458709-2 2014 In addition, the 5HT3 antagonist ondansetron is effective in treating early-onset, but not late-onset, alcohol-dependent subjects. Ondansetron 33-44 5-hydroxytryptamine receptor 3A Homo sapiens 17-21 24128813-3 2013 To test this hypothesis we mutated a series of residues in the 5-HT3A receptor subunit (Tyr(73), Phe(130), Ser(163), and Asp(165)) and in the 5-HT3B receptor subunit (His(73), Phe(130), Glu(170), and Tyr(143)) that were previously predicted by in silico docking studies to interact with palonosetron. Tyrosine 88-91 5-hydroxytryptamine receptor 3A Homo sapiens 63-69 24388024-6 2014 Seventeen percent of patients given 5HT3R antagonists (n=242) and 22% of controls (n=220) had postoperative QTc exceeding 500 milliseconds. qtc 108-111 5-hydroxytryptamine receptor 3A Homo sapiens 36-41 24388024-10 2014 The QTc was prolonged, but not significantly, in diabetic patients given 5HT3R antagonists (P=.16). qtc 4-7 5-hydroxytryptamine receptor 3A Homo sapiens 73-78 24128813-7 2013 Overall, the data support a binding site for palonosetron at the classic orthosteric binding pocket between two 5-HT3A receptor subunits but not at allosteric sites previously identified by in silico modelling and docking. Palonosetron 45-57 5-hydroxytryptamine receptor 3A Homo sapiens 112-118 24030822-2 2013 Consistent with these models, two arginine residues (Arg(436) and Arg(440)) within the MA helix of 5-hydroxytryptamine type 3A (5-HT3A) receptors act singularly as rate-limiting determinants of single-channel conductance (gamma). Arginine 34-42 5-hydroxytryptamine receptor 3A Homo sapiens 128-134 23792067-4 2013 RESULTS: Phenol, pyrrole and alkyl amines, constituents of 5-HT, even at high concentrations, cannot activate 5-HT3A receptors but they can inhibit them. Phenol 9-15 5-hydroxytryptamine receptor 3A Homo sapiens 110-116 23792067-4 2013 RESULTS: Phenol, pyrrole and alkyl amines, constituents of 5-HT, even at high concentrations, cannot activate 5-HT3A receptors but they can inhibit them. Pyrroles 17-24 5-hydroxytryptamine receptor 3A Homo sapiens 110-116 23792067-4 2013 RESULTS: Phenol, pyrrole and alkyl amines, constituents of 5-HT, even at high concentrations, cannot activate 5-HT3A receptors but they can inhibit them. alkyl amines 29-41 5-hydroxytryptamine receptor 3A Homo sapiens 110-116 24030822-4 2013 We probed the majority of residues within the MA helix of the human 5-HT3A subunit using alanine- and arginine-scanning mutagenesis and the substituted cysteine accessibility method to determine their relative influences upon gamma. Cysteine 152-160 5-hydroxytryptamine receptor 3A Homo sapiens 68-74 24030822-2 2013 Consistent with these models, two arginine residues (Arg(436) and Arg(440)) within the MA helix of 5-hydroxytryptamine type 3A (5-HT3A) receptors act singularly as rate-limiting determinants of single-channel conductance (gamma). Arginine 53-56 5-hydroxytryptamine receptor 3A Homo sapiens 128-134 24030822-2 2013 Consistent with these models, two arginine residues (Arg(436) and Arg(440)) within the MA helix of 5-hydroxytryptamine type 3A (5-HT3A) receptors act singularly as rate-limiting determinants of single-channel conductance (gamma). Arginine 66-69 5-hydroxytryptamine receptor 3A Homo sapiens 128-134 24030822-2 2013 Consistent with these models, two arginine residues (Arg(436) and Arg(440)) within the MA helix of 5-hydroxytryptamine type 3A (5-HT3A) receptors act singularly as rate-limiting determinants of single-channel conductance (gamma). Serotonin 99-118 5-hydroxytryptamine receptor 3A Homo sapiens 128-134 24030822-4 2013 We probed the majority of residues within the MA helix of the human 5-HT3A subunit using alanine- and arginine-scanning mutagenesis and the substituted cysteine accessibility method to determine their relative influences upon gamma. Alanine 89-96 5-hydroxytryptamine receptor 3A Homo sapiens 68-74 24030822-4 2013 We probed the majority of residues within the MA helix of the human 5-HT3A subunit using alanine- and arginine-scanning mutagenesis and the substituted cysteine accessibility method to determine their relative influences upon gamma. Arginine 102-110 5-hydroxytryptamine receptor 3A Homo sapiens 68-74 23897038-2 2013 In this study, they explored additional markers of ondansetron treatment response in alcoholics by examining polymorphisms in the HTR3A and HTR3B genes, which regulate directly the function and binding of 5-HT3 receptors to ondansetron. Ondansetron 51-62 5-hydroxytryptamine receptor 3A Homo sapiens 130-135 23810831-7 2013 Replacement of the D loop amino acid triplet RQY of the 5-HT3A subunit, with the aligned residues from the 5-HT3B subunit, QEV, converts 5-HT to a weak partial agonist in both the homomer and heteromer, but does not compromise activation by mCPBG. 1-(3-chlorophenyl)biguanide 241-246 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 23897038-2 2013 In this study, they explored additional markers of ondansetron treatment response in alcoholics by examining polymorphisms in the HTR3A and HTR3B genes, which regulate directly the function and binding of 5-HT3 receptors to ondansetron. Ondansetron 224-235 5-hydroxytryptamine receptor 3A Homo sapiens 130-135 23897038-6 2013 RESULTS: Individuals carrying one or more of genotypes rs1150226-AG and rs1176713-GG in HTR3A and rs17614942-AC in HTR3B showed a significant overall mean difference between ondansetron and placebo in drinks per drinking day (22.50; effect size=0.867), percentage of heavy drinking days (220.58%; effect size=0.780), and percentage of days abstinent (18.18%; effect size=0.683). Ondansetron 174-185 5-hydroxytryptamine receptor 3A Homo sapiens 88-93 23822584-4 2013 KEY RESULTS: Dopamine, quipazine and VUF10166 were partial agonists at wild type 5-HT3A and 5-HT3AB receptors, with quipazine and VUF10166 causing a long-lived (>20 min) inhibition of subsequent agonist responses. Dopamine 13-21 5-hydroxytryptamine receptor 3A Homo sapiens 81-87 23822584-4 2013 KEY RESULTS: Dopamine, quipazine and VUF10166 were partial agonists at wild type 5-HT3A and 5-HT3AB receptors, with quipazine and VUF10166 causing a long-lived (>20 min) inhibition of subsequent agonist responses. Quipazine 23-32 5-hydroxytryptamine receptor 3A Homo sapiens 81-87 23822584-4 2013 KEY RESULTS: Dopamine, quipazine and VUF10166 were partial agonists at wild type 5-HT3A and 5-HT3AB receptors, with quipazine and VUF10166 causing a long-lived (>20 min) inhibition of subsequent agonist responses. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 37-45 5-hydroxytryptamine receptor 3A Homo sapiens 81-87 23822584-6 2013 A T6"S substitution in the 5-HT3A subunit decreased EC50 and increased Rmax of dopamine and quipazine at both homomeric and heteromeric receptors. Dopamine 79-87 5-hydroxytryptamine receptor 3A Homo sapiens 27-33 23822584-6 2013 A T6"S substitution in the 5-HT3A subunit decreased EC50 and increased Rmax of dopamine and quipazine at both homomeric and heteromeric receptors. Quipazine 92-101 5-hydroxytryptamine receptor 3A Homo sapiens 27-33 23822584-8 2013 CONCLUSIONS AND IMPLICATIONS: These results indicate that a mutation in the pore lining domain in both 5-HT3A and 5-HT3AB receptors alters the relative efficacy of a series of agonists, changing some (e.g. quipazine) from apparent antagonists to potent and efficacious agonists. Quipazine 206-215 5-hydroxytryptamine receptor 3A Homo sapiens 103-115 23305320-4 2013 Topotecan inhibited 5-HT-gated current through homomeric 5-HT3A receptors. Topotecan 0-9 5-hydroxytryptamine receptor 3A Homo sapiens 57-63 23640722-0 2013 Structure-activity relationships of quinoxaline-based 5-HT3A and 5-HT3AB receptor-selective ligands. Quinoxalines 36-47 5-hydroxytryptamine receptor 3A Homo sapiens 54-60 23640722-3 2013 During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [(3)H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 33-79 5-hydroxytryptamine receptor 3A Homo sapiens 200-206 23640722-3 2013 During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [(3)H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 81-89 5-hydroxytryptamine receptor 3A Homo sapiens 200-206 23640722-4 2013 Fragment hit exploration, initiated from VUF10166 and 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol, resulted in a series of compounds with higher affinity at either 5-HT3A or 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 41-49 5-hydroxytryptamine receptor 3A Homo sapiens 162-168 23640722-4 2013 Fragment hit exploration, initiated from VUF10166 and 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol, resulted in a series of compounds with higher affinity at either 5-HT3A or 5-HT3AB receptors. 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol 54-95 5-hydroxytryptamine receptor 3A Homo sapiens 162-168 23640722-6 2013 At the extremes of the new compounds were 2-amino-3-(4-methylpiperazin-1-yl)quinoxaline, which showed 11-fold selectivity for the 5-HT3A receptor, and 2-(4-methylpiperazin-1-yl)quinoxaline, which showed an 8.3-fold selectivity for the 5-HT3AB receptor. 2-amino-3-(4-methylpiperazin-1-yl)quinoxaline 42-87 5-hydroxytryptamine receptor 3A Homo sapiens 130-136 23594147-5 2013 KEY RESULTS: Cl-indole (1-100 muM) potentiated agonist (5-HT) and particularly partial agonist [(S)-zacopride, DDP733, RR210, quipazine, dopamine, 2-methyl-5-HT, SR57227A, meta chlorophenyl biguanide] induced h5-HT3A receptor-mediated responses. 5-chloroindole 13-22 5-hydroxytryptamine receptor 3A Homo sapiens 210-216 23126479-4 2013 Furthermore, it has been reported that the 5-HTR3 antagonist ondansetron is efficacious in the treatment of Gilles de la Tourette syndrome (GTS). Ondansetron 61-72 5-hydroxytryptamine receptor 3A Homo sapiens 45-49 23290502-1 2013 BACKGROUND: Pharmacologic studies implicate a significant role of genes encoding the serotonin transporter (SLC6A4) and the 5-HT3AB subunits HTR3A and HTR3B in nicotine dependence (ND). Nicotine 160-168 5-hydroxytryptamine receptor 3A Homo sapiens 141-146 23321066-1 2013 Human serotonin receptor 3A (5-HT3A) is a ligand-gated ion channel regulated by serotonin. Serotonin 6-15 5-hydroxytryptamine receptor 3A Homo sapiens 29-35 23321066-4 2013 The purified P9-5-HT3A was efficiently reconstituted into proteoliposomes, and the serotonin-dependent ion-channel activity of P9-5-HT3A was observed by measuring the increased fluorescence of Fluo-3 attributed to the formation of a complex with the Ca(2+) ions released from the proteoliposomes. Serotonin 83-92 5-hydroxytryptamine receptor 3A Homo sapiens 16-22 23321066-4 2013 The purified P9-5-HT3A was efficiently reconstituted into proteoliposomes, and the serotonin-dependent ion-channel activity of P9-5-HT3A was observed by measuring the increased fluorescence of Fluo-3 attributed to the formation of a complex with the Ca(2+) ions released from the proteoliposomes. Serotonin 83-92 5-hydroxytryptamine receptor 3A Homo sapiens 130-136 23321066-4 2013 The purified P9-5-HT3A was efficiently reconstituted into proteoliposomes, and the serotonin-dependent ion-channel activity of P9-5-HT3A was observed by measuring the increased fluorescence of Fluo-3 attributed to the formation of a complex with the Ca(2+) ions released from the proteoliposomes. Fluo-3 193-199 5-hydroxytryptamine receptor 3A Homo sapiens 16-22 23321066-4 2013 The purified P9-5-HT3A was efficiently reconstituted into proteoliposomes, and the serotonin-dependent ion-channel activity of P9-5-HT3A was observed by measuring the increased fluorescence of Fluo-3 attributed to the formation of a complex with the Ca(2+) ions released from the proteoliposomes. Fluo-3 193-199 5-hydroxytryptamine receptor 3A Homo sapiens 130-136 23321066-5 2013 Alanine substitution for Trp178 of 5-HT3A abolished the serotonin-dependent ion-channel activity, confirming the importance of Trp178 as a ligand-binding site. Alanine 0-7 5-hydroxytryptamine receptor 3A Homo sapiens 35-41 23321066-5 2013 Alanine substitution for Trp178 of 5-HT3A abolished the serotonin-dependent ion-channel activity, confirming the importance of Trp178 as a ligand-binding site. Serotonin 56-65 5-hydroxytryptamine receptor 3A Homo sapiens 35-41 23321066-6 2013 Furthermore, the ion-channel activity of the reconstituted P9-5-HT3A was effectively blocked by treatment with ondansetron, an antagonist of 5-HT3A. Ondansetron 111-122 5-hydroxytryptamine receptor 3A Homo sapiens 62-68 23321066-6 2013 Furthermore, the ion-channel activity of the reconstituted P9-5-HT3A was effectively blocked by treatment with ondansetron, an antagonist of 5-HT3A. Ondansetron 111-122 5-hydroxytryptamine receptor 3A Homo sapiens 141-147 22924764-7 2013 Additionally, methylation levels of 6 CpGs (including cg08989585) in the HTR3A promoter region were analyzed in the replication sample. cg08989585 54-64 5-hydroxytryptamine receptor 3A Homo sapiens 73-78 22700043-0 2012 Outcome definitions and clinical predictors influence pharmacogenetic associations between HTR3A gene polymorphisms and response to clozapine in patients with schizophrenia. Clozapine 132-141 5-hydroxytryptamine receptor 3A Homo sapiens 91-96 22700043-3 2012 Functionally important HTR3A gene single-nucleotide polymorphisms (SNPs) were reported to be associated with response to clozapine. Clozapine 121-130 5-hydroxytryptamine receptor 3A Homo sapiens 23-28 22700043-4 2012 OBJECTIVE: The aim of this study was to investigate how the association between HTR3A gene SNP and response to clozapine is influenced by various clinical predictors and by differing outcome definitions in patients with treatment-resistant schizophrenia (TRS). Clozapine 111-120 5-hydroxytryptamine receptor 3A Homo sapiens 80-85 22306960-0 2012 VUF10166, a novel compound with differing activities at 5-HT3A and 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 0-8 5-hydroxytryptamine receptor 3A Homo sapiens 56-62 23115686-2 2012 Palonosetron, the newest 5-HT3 antagonist, has potent antiemetic property. Palonosetron 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 25-30 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. Serotonin 122-141 5-hydroxytryptamine receptor 3A Homo sapiens 150-155 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. Serotonin 122-141 5-hydroxytryptamine receptor 3A Homo sapiens 276-281 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. cinv 225-229 5-hydroxytryptamine receptor 3A Homo sapiens 150-155 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. cinv 225-229 5-hydroxytryptamine receptor 3A Homo sapiens 276-281 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. Serotonin 54-63 5-hydroxytryptamine receptor 3A Homo sapiens 150-155 22644261-1 2012 BACKGROUND: Previous reports suggested that selective serotonin reuptake inhibitors (SSRI) could decrease the activity of 5-hydroxytryptamine type 3 (5-HT3) antagonists against acute chemotherapy-induced nausea and vomiting (CINV), possibly through serotonin accumulation for 5-HT3 receptors. Serotonin 54-63 5-hydroxytryptamine receptor 3A Homo sapiens 276-281 22644261-7 2012 CONCLUSIONS: Our findings reinforce the hypothesis that SSRI decrease the antiemetic activity of the 5-HT3 serotonin antagonist ondansetron, resulting in higher rates of acute vomiting in cancer patients despite adequate antiemetic prophylaxis. Serotonin 107-116 5-hydroxytryptamine receptor 3A Homo sapiens 101-106 22644261-7 2012 CONCLUSIONS: Our findings reinforce the hypothesis that SSRI decrease the antiemetic activity of the 5-HT3 serotonin antagonist ondansetron, resulting in higher rates of acute vomiting in cancer patients despite adequate antiemetic prophylaxis. Ondansetron 128-139 5-hydroxytryptamine receptor 3A Homo sapiens 101-106 22589534-8 2012 The PU02 binding site in the 5-HT(3)R corresponds to allosteric sites in anionic Cys-loop receptors, which emphasizes the uniform nature of the molecular events underlying signaling through the receptors. PU 02 4-8 5-hydroxytryptamine receptor 3A Homo sapiens 29-37 22306960-2 2012 VUF10166 displaced [3H]granisetron binding to 5-HT3A receptors expressed in human embryonic kidney cells with high affinity (K(i) = 0.04 nM) but was less potent at 5-HT3AB receptors (K(i) = 22 nM). 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 0-8 5-hydroxytryptamine receptor 3A Homo sapiens 46-52 22306960-2 2012 VUF10166 displaced [3H]granisetron binding to 5-HT3A receptors expressed in human embryonic kidney cells with high affinity (K(i) = 0.04 nM) but was less potent at 5-HT3AB receptors (K(i) = 22 nM). Tritium 20-22 5-hydroxytryptamine receptor 3A Homo sapiens 46-52 22306960-3 2012 Dissociation of [3H]granisetron in the presence of VUF10166 was best fit with a single time constant (t(1/2) = 53 min) at 5-HT3A receptors, but with two time constants (t(1/2) = 55 and 2.4 min) at 5-HT3AB receptors. Tritium 17-19 5-hydroxytryptamine receptor 3A Homo sapiens 122-128 22306960-3 2012 Dissociation of [3H]granisetron in the presence of VUF10166 was best fit with a single time constant (t(1/2) = 53 min) at 5-HT3A receptors, but with two time constants (t(1/2) = 55 and 2.4 min) at 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 51-59 5-hydroxytryptamine receptor 3A Homo sapiens 122-128 22306960-4 2012 Electrophysiological studies in oocytes revealed that VUF10166 inhibited 5-HT-induced responses at 5-HT3A receptors at nanomolar concentrations, but inhibition and recovery were too slow to determine an IC50. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 54-62 5-hydroxytryptamine receptor 3A Homo sapiens 99-105 22306960-7 2012 At 5-HT3A receptors, VUF10166 at higher concentrations also behaved as a partial agonist (EC50 = 5.2 muM; R(max) = 0.24) but did not elicit significant responses at 5-HT3AB receptors at <=100 muM. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 21-29 5-hydroxytryptamine receptor 3A Homo sapiens 3-9 22306960-9 2012 The ability of VUF10166 to distinguish between 5-HT3A and 5-HT3AB receptors could help evaluate differences between these receptor types and has potential therapeutic value. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 15-23 5-hydroxytryptamine receptor 3A Homo sapiens 47-53 23050164-2 2012 Ondansetron is a 5-hydroxytryptamine (5-HT(3), serotonin) receptor antagonist used as antiemetic prophylaxis preceding chemotherapy administration. Ondansetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 38-66 23050164-2 2012 Ondansetron is a 5-hydroxytryptamine (5-HT(3), serotonin) receptor antagonist used as antiemetic prophylaxis preceding chemotherapy administration. Serotonin 17-36 5-hydroxytryptamine receptor 3A Homo sapiens 38-66 22694192-3 2012 The results of molecular dynamics simulations and computational alanine scanning mutagenesis studies applied here to the homomeric human 5-HT(3A)-R disclose an aromatic "hot" cluster in the centre of the interface formed by residues W178 (principal subunit), Y68, Y83, W85 and Y148 (complementary subunit). Alanine 64-71 5-hydroxytryptamine receptor 3A Homo sapiens 137-144 21420406-1 2011 BACKGROUND & AIMS: 5-Hydroxytryptamine (5-HT)3 receptor (5-HT3R) antagonists are effective in treating patients with irritable bowel syndrome (IBS) and have anxiolytic effects. Adenosine Monophosphate 12-15 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 21948949-6 2011 Recently, we showed that channels functioned when the entire 5-HT3A M3-M4 loop was replaced by the heptapeptide M3-M4 loop sequence from GLIC, a bacterial Cys-loop neurotransmitter gated ion channel homologue from Gloebacter violaceus. Cysteine 155-158 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 22044840-0 2011 Anticancer drug irinotecan inhibits homomeric 5-HT3A and heteromeric 5-HT3AB receptor responses. Irinotecan 16-26 5-hydroxytryptamine receptor 3A Homo sapiens 46-52 21477640-3 2011 Here, we report that CBD and THC inhibited the function of human 5-HT(3A) receptors (h5-HT(3A)Rs) expressed in HEK 293 cells. Cannabidiol 21-24 5-hydroxytryptamine receptor 3A Homo sapiens 65-72 21477640-3 2011 Here, we report that CBD and THC inhibited the function of human 5-HT(3A) receptors (h5-HT(3A)Rs) expressed in HEK 293 cells. Dronabinol 29-32 5-hydroxytryptamine receptor 3A Homo sapiens 65-72 21420406-1 2011 BACKGROUND & AIMS: 5-Hydroxytryptamine (5-HT)3 receptor (5-HT3R) antagonists are effective in treating patients with irritable bowel syndrome (IBS) and have anxiolytic effects. Serotonin 23-42 5-hydroxytryptamine receptor 3A Homo sapiens 61-67 20168265-2 2010 In this study, we further investigated the role of the subunits A and B of the HTR3 receptor using 140 schizophrenia patients taking clozapine for 6 months. Clozapine 133-142 5-hydroxytryptamine receptor 3A Homo sapiens 79-83 20694841-3 2010 Prucalopride, the newest European Medicines Agency-approved 5-hydroxytryptamine receptor 4 (5-HT(4)) agonist, is effective in the treatment of chronic constipation with improved cardiovascular safety relative to older 5-HT(4) drugs; similarly, ramosetron, the 5-hydroxytryptamine receptor 3 (5-HT(3)) antagonist, appears efficacious in diarrhea-predominant IBS. prucalopride 0-12 5-hydroxytryptamine receptor 3A Homo sapiens 260-290 20694966-7 2010 CONCLUSIONS: These findings suggest that the HTR3A CC genotype may be associated with alterations in brain structures central to emotion processing, particularly when exposed to stress, and further highlight the potential role of the serotonin system in the pathophysiology of affective disorders. Serotonin 234-243 5-hydroxytryptamine receptor 3A Homo sapiens 45-50 21454663-7 2011 The P(Ca)/P(Cs) of 3.8 previously reported for the 5-HT(3)A(QDA) construct was reduced to 0.13 and 0.06 by the D127N and D127K mutations, respectively, with lesser, but clearly significant, effects caused by the D113N (1.04) and D113K (0.60) substitutions. Cesium 12-14 5-hydroxytryptamine receptor 3A Homo sapiens 51-59 21454663-9 2011 The data identify two key residues in the extracellular vestibule of the 5-HT(3)A receptor that markedly influence gamma, P(Ca)/P(Cs), and additionally the suppression of gamma by Ca(2+). Cesium 130-132 5-hydroxytryptamine receptor 3A Homo sapiens 73-81 21246737-2 2011 The design, synthesis, and functional characterisation of benzamide analogues at the 5-HT3A receptor yielded substantial information concerning the analogues as 5-HT3 receptor agonists. benzamide 58-67 5-hydroxytryptamine receptor 3A Homo sapiens 85-91 20724042-1 2010 Inhibition of the 5-hydroxytryptamine receptor (5-HT(3)R), a member of the Cys-loop superfamily of Ligand-Gated Ion Channels (LGICs), has been recognized to have important antiemetic effects. Cysteine 75-78 5-hydroxytryptamine receptor 3A Homo sapiens 48-56 20724042-2 2010 With respect to the many other drugs already in use, such as the first generation 5-HT(3)R antagonist granisetron, palonosetron, a second generation antagonist, clearly demonstrates superior inhibition potency towards the 5-HT(3)Rs. Granisetron 102-113 5-hydroxytryptamine receptor 3A Homo sapiens 82-90 20724042-2 2010 With respect to the many other drugs already in use, such as the first generation 5-HT(3)R antagonist granisetron, palonosetron, a second generation antagonist, clearly demonstrates superior inhibition potency towards the 5-HT(3)Rs. Palonosetron 115-127 5-hydroxytryptamine receptor 3A Homo sapiens 82-90 20724042-3 2010 Five different receptor monomers, the 5-HT(3)R A-E, have been identified although the A and B subunits are the only known to build functional receptors, the homopentameric 5-HT(3A)R and the heteropentameric 5-HT(3B-A)R (with BBABA subunit arrangement). bbaba 225-230 5-hydroxytryptamine receptor 3A Homo sapiens 38-46 20724042-6 2010 The results of docking studies of the natural agonist serotonin and the antagonists palonosetron and granisetron into the modelled homomeric and heteromeric 5-HT(3)R binding interfaces, provide a possible rationalization both of the higher potency of palonosetron with respect to other antagonists, and of its previously reported allosteric binding and positive cooperativity properties. Serotonin 54-63 5-hydroxytryptamine receptor 3A Homo sapiens 157-165 20724042-6 2010 The results of docking studies of the natural agonist serotonin and the antagonists palonosetron and granisetron into the modelled homomeric and heteromeric 5-HT(3)R binding interfaces, provide a possible rationalization both of the higher potency of palonosetron with respect to other antagonists, and of its previously reported allosteric binding and positive cooperativity properties. Palonosetron 84-96 5-hydroxytryptamine receptor 3A Homo sapiens 157-165 20724042-6 2010 The results of docking studies of the natural agonist serotonin and the antagonists palonosetron and granisetron into the modelled homomeric and heteromeric 5-HT(3)R binding interfaces, provide a possible rationalization both of the higher potency of palonosetron with respect to other antagonists, and of its previously reported allosteric binding and positive cooperativity properties. Granisetron 101-112 5-hydroxytryptamine receptor 3A Homo sapiens 157-165 20724042-6 2010 The results of docking studies of the natural agonist serotonin and the antagonists palonosetron and granisetron into the modelled homomeric and heteromeric 5-HT(3)R binding interfaces, provide a possible rationalization both of the higher potency of palonosetron with respect to other antagonists, and of its previously reported allosteric binding and positive cooperativity properties. Palonosetron 251-263 5-hydroxytryptamine receptor 3A Homo sapiens 157-165 20849671-2 2010 The best studied members of the Cys-loop family are nACh, 5-HT3, GABAA and glycine receptors. Cysteine 32-35 5-hydroxytryptamine receptor 3A Homo sapiens 58-63 20166948-3 2010 This review covers the authors" work performed during the past decade in the development of 5-HT(3)R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. arylpiperazine 135-149 5-hydroxytryptamine receptor 3A Homo sapiens 92-100 20166948-3 2010 This review covers the authors" work performed during the past decade in the development of 5-HT(3)R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. Quipazine 173-182 5-hydroxytryptamine receptor 3A Homo sapiens 92-100 20166948-3 2010 This review covers the authors" work performed during the past decade in the development of 5-HT(3)R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. Quipazine 184-193 5-hydroxytryptamine receptor 3A Homo sapiens 92-100 20166948-3 2010 This review covers the authors" work performed during the past decade in the development of 5-HT(3)R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. arylpiperazines 199-214 5-hydroxytryptamine receptor 3A Homo sapiens 92-100 19188483-3 2009 In contrast to the mouse receptor, coapplication of colchicine with 5-HT (<1 microM) strongly enhanced 5-HT-evoked currents in oocytes expressing human 5-HT(3A)Rs. Colchicine 52-62 5-hydroxytryptamine receptor 3A Homo sapiens 155-162 19513770-8 2009 The positive wave is assigned to 5-HT3A receptors in the free membrane that drive a potassium outward current through the adherent membrane. Potassium 84-93 5-hydroxytryptamine receptor 3A Homo sapiens 33-39 19513770-9 2009 The negative wave is attributed to 5-HT3A receptors in the adherent membrane that are activated with a delay due to serotonin diffusion. Serotonin 116-125 5-hydroxytryptamine receptor 3A Homo sapiens 35-41 20124604-0 2009 Expression changes of serotonin receptor gene subtype 5HT3a in peripheral blood mononuclear cells from schizophrenic patients treated with haloperidol and Olanzapin. Haloperidol 139-150 5-hydroxytryptamine receptor 3A Homo sapiens 54-59 20124604-0 2009 Expression changes of serotonin receptor gene subtype 5HT3a in peripheral blood mononuclear cells from schizophrenic patients treated with haloperidol and Olanzapin. Olanzapine 155-164 5-hydroxytryptamine receptor 3A Homo sapiens 54-59 19184136-8 2009 These data suggest that variation within genes on the serotonin pathway, particularly HTR3A, may have modest effects on autism risk. Serotonin 54-63 5-hydroxytryptamine receptor 3A Homo sapiens 86-91 19232535-11 2009 These results suggest that 5-HT(3)R activation, coupled with increased intracellular calcium, can transiently alter postsynaptic excitability in IC neurons. Calcium 85-92 5-hydroxytryptamine receptor 3A Homo sapiens 27-35