5-HT3 receptors: Role in disease and target of drugs

Aapro, 2004, Granisetron: an update on its clinical use in the management of nausea and vomiting, Oncologist, 9, 673, 10.1634/theoncologist.9-6-673

Aapro, 2005, 5-HT(3)-receptor antagonists in the management of nausea and vomiting in cancer and cancer treatment, Oncology, 69, 97, 10.1159/000087979

Aapro, 2005, Palonosetron improves prevention of chemotherapy-induced nausea and vomiting in elderly patients, J Support Oncol, 3, 369

Abdel-Aziz, 2005, 5-HT3 receptor blocking activity of arylalkanes isolated from the rhizome of Zingiber officinale, Planta Med, 71, 609, 10.1055/s-2005-871265

Abdel-Aziz, 2006, Mode of action of gingerols and shogaols on 5-HT3 receptors: binding studies, cation uptake by the receptor channel and contraction of isolated guinea-pig ileum, Eur J Pharmacol, 530, 136, 10.1016/j.ejphar.2005.10.049

Abi-Dargham, 1993, Pharmacological and regional characterization of [3H]LY278584 binding sites in human brain, J Neurochem, 60, 730, 10.1111/j.1471-4159.1993.tb03208.x

Adler, 2005, Improved p50 auditory gating with ondansetron in medicated schizophrenia patients, Am J Psychiatry, 162, 386, 10.1176/appi.ajp.162.2.386

Aibiki, 2007, Impact of serotonin receptor-3 gene polymorphism on irritable bowel syndrome, Gastroenterology, 132, A134

Akhondzadeh, 2009, Added ondansetron for stable schizophrenia: a double blind, placebo controlled trial, Schizophr Res, 107, 206, 10.1016/j.schres.2008.08.004

Alhaider, 1991, Spinal 5-HT3 receptor-mediated antinociception: possible release of GABA, J Neurosci, 11, 1881, 10.1523/JNEUROSCI.11-07-01881.1991

Anderson, 2009, Examination of association of genes in the serotonin system to autism, Neurogenetics, 10, 209, 10.1007/s10048-009-0171-7

Andresen, 2008, Effects of 5-hydroxytryptamine (serotonin) type 3 antagonists on symptom relief and constipation in nonconstipated irritable bowel syndrome: a systematic review and meta-analysis of randomized controlled trials, Clin Gastroenterol Hepatol, 6, 545, 10.1016/j.cgh.2007.12.015

Andrews, 1988, Neuropharmacology of emesis induced by anti-cancer therapy, Trends Pharmacol Sci, 9, 334, 10.1016/0165-6147(88)90106-X

Anguelova, 2003, A systematic review of association studies investigating genes coding for serotonin receptors and the serotonin transporter: I. Affective disorde, Mol Psychiatry, 8, 574, 10.1038/sj.mp.4001328

Arias, 1999, Role of local anesthetics on both cholinergic and serotonergic ionotropic receptors, Neurosci Biobehav Rev, 23, 817, 10.1016/S0149-7634(99)00020-2

Arias, 2006, Molecular mechanisms and binding site locations for noncompetitive antagonists of nicotinic acetylcholine receptors, Int J Biochem Cell Biol, 38, 1254, 10.1016/j.biocel.2006.01.006

Armanini, 2002, History of the endocrine effects of licorice, Exp Clin Endocrinol Diabetes, 110, 257, 10.1055/s-2002-34587

Ashby, 1994, Effect produced by acute and chronic administration of the selective 5-HT3 receptor antagonist BRL 46470 on the number of spontaneously active midbrain dopamine cells in the rat, Drug Dev Res, 31, 228, 10.1002/ddr.430310310

Auranen, 2002, A genomewide screen for autism-spectrum disorders: evidence for a major susceptibility locus on chromosome 3q25-27, Am J Hum Genet, 71, 777, 10.1086/342720

Auranen, 2003, Evidence for allelic association on chromosome 3q25-27 in families with autism spectrum disorders originating from a subisolate of Finland, Mol Psychiatry, 8, 879, 10.1038/sj.mp.4001299

Bailey, 1995, Autism as a strongly genetic disorder: evidence from a British twin study, Psychol Med, 25, 63, 10.1017/S0033291700028099

Ballestero, 2005, Effects of quinine, quinidine, and chloroquine on alpha9alpha10 nicotinic cholinergic receptors, Mol Pharmacol, 68, 822, 10.1124/mol.105.014431

Barann, 2006, 5-HT3 receptors and emesis, Pharmacol Rep, 58, 253

Barann, 2000, Inhibition of 5-HT3 receptors by propofol: equilibrium and kinetic measurements, Neuropharmacology, 39, 1064, 10.1016/S0028-3908(99)00205-1

Barann, 1997, 5-HT3 receptors in outside-out patches of N1E-115 neuroblastoma cells: basic properties and effects of pentobarbital, Neuropharmacology, 36, 655, 10.1016/S0028-3908(97)00059-2

Barann, 1999, Inhibition by steroids of [14C]-guanidinium flux through the voltage-gated sodium channel and the cation channel of the 5-HT3 receptor of N1E-115 neuroblastoma cells, Naunyn Schmiedebergs Arch Pharmacol, 360, 234, 10.1007/s002109900089

Barann, 1993, Inhibition by anaesthetics of 14C-guanidinium flux through the voltage-gated sodium channel and the cation channel of the 5-HT3 receptor of N1E-115 neuroblastoma cells, Naunyn Schmiedebergs Arch Pharmacol, 347, 125, 10.1007/BF00169256

Barann, 2008, Molecular actions of propofol on human 5-HT3A receptors: enhancement as well as inhibition by closely related phenol derivatives, Anesth Analg, 106, 846, 10.1213/ane.0b013e318162ca7c

Barann, 2000, Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects, Naunyn Schmiedebergs Arch Pharmacol, 362, 255, 10.1007/s002100000288

Barann, 2002, Direct inhibition by cannabinoids of human 5-HT3A receptors: probable involvement of an allosteric modulatory site, Br J Pharmacol, 137, 589, 10.1038/sj.bjp.0704829

Barann, 1995, Increasing effect of ethanol on 5-HT3 receptor-mediated 14C-guanidinium influx in N1E-115 neuroblastoma cells, Naunyn Schmiedebergs Arch Pharmacol, 352, 149, 10.1007/BF00176768

Barann, 2006, Effects of tramadol and O-demethyl-tramadol on human 5-HT reuptake carriers and human 5-HT3A receptors: a possible mechanism for tramadol-induced early emesis, Eur J Pharmacol, 531, 54, 10.1016/j.ejphar.2005.11.054

Barnes, 1989, Identification and characterisation of 5-hydroxytryptamine 3 recognition sites in human brain tissue, J Neurochem, 53, 1787, 10.1111/j.1471-4159.1989.tb09244.x

Barnes, 1989, 5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissue, Nature, 338, 762, 10.1038/338762a0

Barnes, 2009, The 5-HT3 receptor—the relationship between structure and function, Neuropharmacology, 56, 273, 10.1016/j.neuropharm.2008.08.003

Barrera, 2005, Atomic force microscopy reveals the stoichiometry and subunit arrangement of 5-HT3 receptors, Proc Natl Acad Sci USA, 102, 12595, 10.1073/pnas.0503253102

Baumgarten, 1997

Belelli, 1995, Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit, Mol Pharmacol, 48, 1054

Berman, 2002, Condition-specific deactivation of brain regions by 5-HT3 receptor antagonist Alosetron, Gastroenterology, 123, 969, 10.1053/gast.2002.35990

Bertaccini, 2005, Homology modeling of a human glycine alpha 1 receptor reveals a plausible anesthetic binding site, J Chem Inf Model, 45, 128, 10.1021/ci0497399

Besret, 1998, [11C]S21007, a putative partial agonist for 5-HT3 receptors PET studies. Rat and primate in vivo biological evaluation, Life Science, 62, 115, 10.1016/S0024-3205(97)01058-8

Bigler, 1990, Morphine, morphine-6-glucuronide and morphine-3-glucuronide concentrations in plasma and cerebrospinal fluid during long-term high-dose intrathecal morphine administration, Pain, 41, 15, 10.1016/0304-3959(90)91103-P

Blower, 2002, 5-HT3-receptor antagonists and the cytochrome P450 system: clinical implications, Cancer J, 8, 405, 10.1097/00130404-200209000-00012

Boess, 1995, Ultrastructure of the 5-hydroxytryptamine3 receptor, J Neurochem, 64, 1401, 10.1046/j.1471-4159.1995.64031401.x

Bolton, 1994, A case–control family history study of autism, J Child Psychol Psychiatry, 35, 877, 10.1111/j.1469-7610.1994.tb02300.x

Borrelli, 2005, Effectiveness and safety of ginger in the treatment of pregnancy-induced nausea and vomiting, Obstet Gynecol, 105, 849, 10.1097/01.AOG.0000154890.47642.23

Böttner, 2009, Laser microdissection as a new tool to investigate site-specific gene expression in enteric ganglia of the human intestine, Neurogastroenterol Motil, 22, e52

Boyd, 2003, Cell surface expression of 5-hydroxytryptamine type 3 receptors is controlled by an endoplasmic reticulum retention signal, J Biol Chem, 278, 27681, 10.1074/jbc.M304938200

Boyd, 2002, Assembly and cell surface expression of homomeric and heteromeric 5-HT3 receptors: the role of oligomerization and chaperone proteins, Mol Cell Neurosci, 21, 38, 10.1006/mcne.2002.1160

Brady, 2007, Identification of 5-HT3A and 5-HT3B receptor subunits in human hippocampus, Neuropharmacology, 52, 1284, 10.1016/j.neuropharm.2007.01.009

Brejc, 2001, Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors, Nature, 411, 269, 10.1038/35077011

Brown, 1998, Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A), J Physiol, 507, 653, 10.1111/j.1469-7793.1998.653bs.x

Brüss, 2000, Modified 5-HT3A receptor function by co-expression of alternatively spliced human 5-HT3A receptor isoforms, Naunyn Schmiedebergs Arch Pharmacol, 362, 392, 10.1007/s002100000342

Bufton, 1993, Distribution and characterization of the [3H]granisetron-labelled 5-HT3 receptor in the human forebrain, Neuropharmacology, 32, 1325, 10.1016/0028-3908(93)90027-Z

Bulik, 1998, Heritability of binge-eating and broadly defined bulimia nervosa, Biol Psychiatry, 44, 1210, 10.1016/S0006-3223(98)00280-7

Butler, 1988, Pharmacological properties of GR38032F, a novel antagonist at 5-HT3 receptors, Br J Pharmacol, 94, 397, 10.1111/j.1476-5381.1988.tb11542.x

Campiani, 1997, Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure, Eur J Med Chem, 40, 3670, 10.1021/jm970376w

Cappelli, 2002, Novel potent 5-HT(3) receptor ligands based on the pyrrolidone structure: synthesis, biological evaluation, and computational rationalization of the ligand–receptor interaction modalities, Bioorg Med Chem, 10, 779, 10.1016/S0968-0896(01)00332-7

Chaiyakunapruk, 2006, The efficacy of ginger for the prevention of postoperative nausea and vomiting: a meta-analysis, Am J Obstet Gynecol, 194, 95, 10.1016/j.ajog.2005.06.046

Chameau, 2006, Serotonin 5-HT(3) receptors in the central nervous system, Cell Tissue Res, 326, 573, 10.1007/s00441-006-0255-8

Chang, 2006, Incidence of ischemic colitis and serious complications of constipation among patients using alosetron: systematic review of clinical trials and post-marketing surveillance data, Am J Gastroenterol, 101, 1069, 10.1111/j.1572-0241.2006.00459.x

Cheng, 2005, Cell surface expression of 5-hydroxytryptamine type 3 receptors is promoted by RIC-3, J Biol Chem, 280, 22502, 10.1074/jbc.M414341200

Cheng, 1973, Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction, Biochem Pharmacol, 22, 3099, 10.1016/0006-2952(73)90196-2

Chiossi, 2006, Hyperemesis gravidarum complicated by Wernicke encephalopathy: background, case report, and review of the literature, Obstet Gynecol Surv, 61, 255, 10.1097/01.ogx.0000206336.08794.65

Choi, 2003, Mechanism of block by fluoxetine of 5-hydroxytryptamine3 (5-HT3)-mediated currents in NCB-20 neuroblastoma cells, Biochem Pharmacol, 66, 2125, 10.1016/j.bcp.2003.08.012

Cole, 2006, Migraine, fibromyalgia, and depression among people with IBS: a prevalence study, BMC Gastroenterol, 6, 26, 10.1186/1471-230X-6-26

Combrink, 2009, Characterization of the naturally occurring Arg344His variant of the human 5-HT 3A receptor, Pharmacol Rep, 61, 785, 10.1016/S1734-1140(09)70134-3

Connolly, 2008, Trafficking of 5-HT(3) and GABA(A) receptors (Review), Mol Membr Biol, 25, 293, 10.1080/09687680801898503

Connolly, 2004, The Cys-loop superfamily of ligand-gated ion channels: the impact of receptor structure on function, Biochem Soc Trans, 32, 529, 10.1042/bst0320529

Coon, 2005, Evidence for linkage on chromosome 3q25-27 in a large autism extended pedigree, Hum Hered, 60, 220, 10.1159/000090546

Cornil, 2006, Functional significance of the rapid regulation of brain estrogen action: where do the estrogens come from?, Brain Res, 1126, 2, 10.1016/j.brainres.2006.07.098

Corringer, 2000, Nicotinic receptors at the amino acid level, Annu Rev Pharmacol Toxicol, 40, 431, 10.1146/annurev.pharmtox.40.1.431

Costall, 2004, 5-HT3 receptors, Curr Drug Targets CNS Neurol Disord, 3, 27, 10.2174/1568007043482624

Crettol, 2006, ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment, Clin Pharmacol Ther, 80, 668, 10.1016/j.clpt.2006.09.012

Das, 2003, The 5-HT3B subunit confers reduced sensitivity to picrotoxin when co-expressed with the 5-HT3A receptor, Brain Res Mol Brain Res, 119, 207, 10.1016/j.molbrainres.2003.09.003

Davies, 1999, The 5-HT3B subunit is a major determinant of serotonin-receptor function, Nature, 397, 359, 10.1038/16941

Davies, 2003, A novel class of ligand-gated ion channel is activated by Zn2+, J Biol Chem, 278, 712, 10.1074/jbc.M208814200

Dawes, 2005, Reductions in and relations between “craving” and drinking in a prospective, open-label trial of ondansetron in adolescents with alcohol dependence, Addict Behav, 30, 1630, 10.1016/j.addbeh.2005.07.004

De Ponti, 2004, Pharmacology of serotonin: what a clinician should know, Gut, 53, 1520, 10.1136/gut.2003.035568

Deeb, 2009, Direct subunit-dependent multimodal 5-hydroxytryptamine3 receptor antagonism by methadone, Mol Pharmacol, 75, 908, 10.1124/mol.108.053322

Deiml, 2004, Alpha-thujone reduces 5-HT3 receptor activity by an effect on the agonist-reduced desensitization, Neuropharmacology, 46, 192, 10.1016/j.neuropharm.2003.09.022

den Dunnen, 2000, Mutation nomenclature extensions and suggestions to describe complex mutations: a discussion, Hum Mutat, 15, 7, 10.1002/(SICI)1098-1004(200001)15:1<7::AID-HUMU4>3.0.CO;2-N

Doran, 2005, The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model, Drug Metab Dispos, 33, 165, 10.1124/dmd.104.001230

Dubin, 1999, The pharmacological and functional characteristics of the serotonin 5-HT(3A) receptor are specifically modified by a 5-HT(3B) receptor subunit, J Biol Chem, 274, 30799, 10.1074/jbc.274.43.30799

Ducci, 2009, HTR3B is associated with alcoholism with antisocial behavior and alpha EEG power—an intermediate phenotype for alcoholism and co-morbid behaviors, Alcohol, 43, 73, 10.1016/j.alcohol.2008.09.005

Eichhorn, 1996, Ondansetron treatment of L-DOPA-induced psychosis, Neurology, 47, 1608, 10.1212/WNL.47.6.1608-b

Einarson, 2004, The safety of ondansetron for nausea and vomiting of pregnancy: a prospective comparative study, Bjog, 111, 940, 10.1111/j.1471-0528.2004.00236.x

Eisensamer, 2003, Antidepressants are functional antagonists at the serotonin type 3 (5-HT3) receptor, Mol Psychiatry, 8, 994, 10.1038/sj.mp.4001314

Eisensamer, 2005, Antidepressants and antipsychotic drugs colocalize with 5-HT3 receptors in raft-like domains, J Neurosci, 25, 10198, 10.1523/JNEUROSCI.2460-05.2005

Ejsing, 2007, A review on the relation between the brain-serum concentration ratio of drugs and the influence of P-glycoprotein, Drug Metabol Drug Interact, 22, 113, 10.1515/DMDI.2007.22.2-3.113

Erspamer, 1937, Ricerche sul secreto delle cellule enterochromaffini, Boll Soc Med Chir Pavia, 51, 357

Evangelista, 2007, Drug evaluation: Pumosetrag for the treatment of irritable bowel syndrome and gastroesophageal reflux disease, Curr Opin Investig Drugs, 8, 416

Faerber, 2007, The neuronal 5-HT3 receptor network after 20years of research—evolving concepts in management of pain and inflammation, Eur J Pharmacol, 560, 1, 10.1016/j.ejphar.2007.01.028

Fairburn, 2003, Eating disorders, Lancet, 361, 407, 10.1016/S0140-6736(03)12378-1

Fan, 1994, Facilitation of 5-hydroxytryptamine3 receptor desensitization by fluoxetine, Neuroscience, 62, 515, 10.1016/0306-4522(94)90384-0

Fan, 1995, Cannabinoid agonists inhibit the activation of 5-HT3 receptors in rat nodose ganglion neurons, J Neurophysiol, 73, 907, 10.1152/jn.1995.73.2.907

Fan, 1995, Nonopioid mechanism of morphine modulation of the activation of 5-hydroxytryptamine type 3 receptors, Mol Pharmacol, 47, 491

Fan, 1994, Effects of cocaine on the serotonin-induced inward current in rat nodose ganglion neurons, J Pharmacol Exp Ther, 271, 262

Fan, 1994, Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons, Neuropharmacology, 33, 1573, 10.1016/0028-3908(94)90132-5

Faris, 2006, Evidence for a vagal pathophysiology for bulimia nervosa and the accompanying depressive symptoms, J Affect Disord, 92, 79, 10.1016/j.jad.2005.12.047

Faris, 2000, Effect of decreasing afferent vagal activity with ondansetron on symptoms of bulimia nervosa: a randomised, double-blind trial, Lancet, 355, 792, 10.1016/S0140-6736(99)09062-5

Fasching, 2008, Polymorphisms in the novel serotonin receptor subunit gene HTR3C show different risks for acute chemotherapy-induced vomiting after anthracycline chemotherapy, J Cancer Res Clin Oncol, 134, 1079, 10.1007/s00432-008-0387-1

Fiebich, 2004, Expression of 5-HT3A receptors in cells of the immune system, Scand J Rheumatol Suppl, 9, 10.1080/03009740410006952

Fink, 2007, 5-HT receptor regulation of neurotransmitter release, Pharmacol Rev, 59, 360, 10.1124/pr.59.07103

Foss, 1998, Prevention of apomorphine- or cisplatin-induced emesis in the dog by a combination of methylnaltrexone and morphine, Cancer Chemother Pharmacol, 42, 287, 10.1007/s002800050819

Fozard, 1984, MDL 72222: a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors, Naunyn Schmiedebergs Arch Pharmacol, 326, 36, 10.1007/BF00518776

Fozard, 1979, Blockade of serotonin receptors on autonomic neurones by (−)-cocaine and some related compounds, Eur J Pharmacol, 59, 195, 10.1016/0014-2999(79)90282-6

Frank, 2004, Investigation of the human serotonin receptor gene HTR3B in bipolar affective and schizophrenic patients, Am J Med Genet B Neuropsychiatr Genet, 131B, 1, 10.1002/ajmg.b.30070

Fukudo, 2009, Impact of Serotonin-3 receptor gene polymorphism on brain activation by rectal distention in human, Gastroenterology, 136, A170, 10.1016/S0016-5085(09)60768-X

Gaddum, 1954, Drugs which antagonize 5-hydroxytryptamine, Br J Pharmacol Chemother, 9, 240, 10.1111/j.1476-5381.1954.tb00848.x

Gaddum, 1957, Two kinds of tryptamine receptor, Br J Pharmacol Chemother, 12, 323, 10.1111/j.1476-5381.1957.tb00142.x

Gallo-Torres, 2006, Alosetron: ischemic colitis and serious complications of constipation, Am J Gastroenterol, 101, 1080, 10.1111/j.1572-0241.2006.00650.x

Gan, 2005, Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same?, CNS Drugs, 19, 225, 10.2165/00023210-200519030-00004

Gershon, 2004, Review article: serotonin receptors and transporters — roles in normal and abnormal gastrointestinal motility, Aliment Pharmacol Ther, 20, 3, 10.1111/j.1365-2036.2004.02180.x

Gershon, 2005, Nerves, reflexes, and the enteric nervous system: pathogenesis of the irritable bowel syndrome, J Clin Gastroenterol, 39, S184, 10.1097/01.mcg.0000156403.37240.30

Gershon, 2007, The serotonin signaling system: from basic understanding to drug development for functional GI disorders, Gastroenterology, 132, 397, 10.1053/j.gastro.2006.11.002

Glaum, 1988, Reversal of the antinociceptive effects of intrathecally administered serotonin in the rat by a selective 5-HT3 receptor antagonist, Neurosci Lett, 95, 313, 10.1016/0304-3940(88)90677-5

Godlewski, 2003, Cannabinoid receptor-independent inhibition by cannabinoid agonists of the peripheral 5-HT3 receptor-mediated von Bezold–Jarisch reflex, Br J Pharmacol, 138, 767, 10.1038/sj.bjp.0705114

Goecke, 2010, Two naturally occurring variants of the serotonin receptor gene HTR3C are associated with nausea in pregnancy, Acta Obstet Gynecol Scand, 89, 7, 10.3109/00016340903322727

Goodwin, 2008, Hyperemesis gravidarum, Obstet Gynecol Clin North Am, 35, 401, 10.1016/j.ogc.2008.04.002

Graeff, 1997, Serotonergic systems, Psychiatr Clin North Am, 20, 723, 10.1016/S0193-953X(05)70342-7

Green, 1995, Expression of recombinant homo-oligomeric 5-hydroxytryptamine3 receptors provides new insights into their maturation and structure, J Biol Chem, 270, 6056, 10.1074/jbc.270.11.6056

Gregory, 1998, 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting, A comparison of their pharmacology and clinical efficacy., Drugs, 55, 173, 10.2165/00003495-199855020-00002

Griebel, 1995, 5-Hydroxytryptamine-interacting drugs in animal models of anxiety disorders: more than 30years of research, Pharmacol Ther, 65, 319, 10.1016/0163-7258(95)98597-J

Gross, 2004, Genetic and environmental factors interact to influence anxiety, Neurotox Res, 6, 493, 10.1007/BF03033286

Grotenhermen, 2005, Cannabinoids, Curr Drug Targets CNS Neurol Disord, 4, 507, 10.2174/156800705774322111

Gu, 2008, Association between a polymorphism of the HTR3A gene and therapeutic response to risperidone treatment in drug-naive Chinese schizophrenia patients, Pharmacogenet Genomics, 18, 721, 10.1097/FPC.0b013e32830500e2

Gumilar, 2008, Tricyclic antidepressants inhibit homomeric Cys-loop receptors by acting at different conformational states, Eur J Pharmacol, 584, 30, 10.1016/j.ejphar.2008.01.023

Gunthorpe, 2001, Conversion of the ion selectivity of the 5-HT(3a) receptor from cationic to anionic reveals a conserved feature of the ligand-gated ion channel superfamily, J Biol Chem, 276, 10977, 10.1074/jbc.M009575200

Hammer, 1990, Serotonin3 receptor antagonists block anorectic responses to amino acid imbalance, Am J Physiol, 259, R627

Hammer, 2009, Functional variants of the serotonin receptor type 3A and B gene are associated with eating disorders, Pharmacogenet Genomics, 19, 790, 10.1097/FPC.0b013e32833132b3

Hammer, 2010, Replication of functional serotonin receptor type 3A and B variants in bipolar affective disorder: a European multicentre study, Medgen, 22

Hammer, C., Kollmannsberger, B., Strissel, P. L., Engel, J., Kreis, H., Lux, M. P., et al. (2010b). A Polymorphism in the Serotonin Receptor Subunit Gene HTR3D Shows Different Risks for Acute Chemotherapy-Induced Vomiting after Anthracycline Chemotherapy. Pharmacogenomics, 11(7), 943–950.

Hamon, 1989, 5-HT3 receptor binding sites are on capsaicin-sensitive fibres in the rat spinal cord, Eur J Pharmacol, 164, 315, 10.1016/0014-2999(89)90472-X

Hanna, 2000, Evidence for expression of heteromeric serotonin 5-HT(3) receptors in rodents, J Neurochem, 75, 240, 10.1046/j.1471-4159.2000.0750240.x

Hannon, 2008, Molecular biology of 5-HT receptors, Behav Brain Res, 195, 198, 10.1016/j.bbr.2008.03.020

Hapfelmeier, 2003, Co-expression of the 5-HT3B serotonin receptor subunit alters the biophysics of the 5-HT3 receptor, Biophys J, 84, 1720, 10.1016/S0006-3495(03)74980-7

Harmer, 2006, 5HT(3) antagonism abolishes the emotion potentiated startle effect in humans, Psychopharmacology (Berl), 186, 18, 10.1007/s00213-006-0337-z

Harrell, 2003, Improvements in hippocampal-dependent learning and decremental attention in 5-HT(3) receptor overexpressing mice, Learn Mem, 10, 410, 10.1101/lm.56103

Haus, 2000, Oral treatment of fibromyalgia with tropisetron given over 28days: influence on functional and vegetative symptoms, psychometric parameters and pain, Scand J Rheumatol Suppl, 113, 55

Hayrapetyan, 2005, Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity, Brain Res Mol Brain Res, 142, 146, 10.1016/j.molbrainres.2005.09.011

Helekar, 1997, Peptidyl prolyl cis–trans isomerase activity of cyclophilin A in functional homo-oligomeric receptor expression, Proc Natl Acad Sci USA, 94, 5432, 10.1073/pnas.94.10.5432

Hermann, 1996, Functional antagonistic properties of clozapine at the 5-HT3 receptor, Biochem Biophys Res Commun, 225, 957, 10.1006/bbrc.1996.1278

Hewlett, 2003, Pilot trial of ondansetron in the treatment of 8 patients with obsessive–compulsive disorder, J Clin Psychiatry, 64, 1025, 10.4088/JCP.v64n0907

Ho, 2006, Pharmacology, pharmacogenetics, and clinical efficacy of 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting, Curr Opin Anaesthesiol, 19, 606, 10.1097/01.aco.0000247340.61815.38

Hodge, 2008, Deletion of the 5-HT(3A)-receptor subunit blunts the induction of cocaine sensitization, Genes Brain Behav, 7, 96, 10.1111/j.1601-183X.2007.00332.x

Hodge, 2006, Understanding how the brain perceives alcohol: neurobiological basis of ethanol discrimination, Alcohol Clin Exp Res, 30, 203, 10.1111/j.1530-0277.2006.00024.x

Hodge, 2004, 5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking, Neuropsychopharmacology, 29, 1807, 10.1038/sj.npp.1300498

Hogg, 2005, Allosteric modulation of ligand-gated ion channels, Biochem Pharmacol, 70, 1267, 10.1016/j.bcp.2005.06.010

Holbrook, 2009, Characterisation of 5-HT3C, 5-HT3D and 5-HT3E receptor subunits: evolution, distribution and function, J Neurochem, 108, 384, 10.1111/j.1471-4159.2008.05775.x

Hold, 2000, Alpha-thujone (the active component of absinthe): gamma-aminobutyric acid type A receptor modulation and metabolic detoxification, Proc Natl Acad Sci USA, 97, 3826, 10.1073/pnas.070042397

Hollander, 2003, Targeted treatments for symptom domains in child and adolescent autism, Lancet, 362, 732, 10.1016/S0140-6736(03)14236-5

Hubbard, 2000, Functional differences between splice variants of the murine 5-HT(3A) receptor: possible role for phosphorylation, Brain Res Mol Brain Res, 81, 101, 10.1016/S0169-328X(00)00138-8

Hui, 1993, 5-HT3 antagonists reduce morphine self-administration in rats, Br J Pharmacol, 110, 1341, 10.1111/j.1476-5381.1993.tb13966.x

Humphrey, 1999, Review article: the therapeutic potential of 5-HT3 receptor antagonists in the treatment of irritable bowel syndrome, Aliment Pharmacol Ther, 13, 31, 10.1046/j.1365-2036.1999.00003.x-i2

Hussy, 1994, Functional properties of a cloned 5-hydroxytryptamine ionotropic receptor subunit: comparison with native mouse receptors, J Physiol, 481, 311, 10.1113/jphysiol.1994.sp020441

Iidaka, 2005, A variant C178T in the regulatory region of the serotonin receptor gene HTR3A modulates neural activation in the human amygdala, J Neurosci, 25, 6460, 10.1523/JNEUROSCI.5261-04.2005

Ireland, 1987, Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve, Br J Pharmacol, 90, 229, 10.1111/j.1476-5381.1987.tb16844.x

Jenkins, 1996, Actions of general anaesthetics on 5-HT3 receptors in N1E-115 neuroblastoma cells, Br J Pharmacol, 117, 1507, 10.1111/j.1476-5381.1996.tb15314.x

Jenkins, 2001, Evidence for a common binding cavity for three general anesthetics within the GABAA receptor, J Neurosci, 21, 10.1523/JNEUROSCI.21-06-j0002.2001

Jensen, 2008, 3B but which 3B and that's just one of the questions: the heterogeneity of human 5-HT3 receptors, Trends Pharmacol Sci, 29, 437, 10.1016/j.tips.2008.06.001

Ji, 2008, An association between serotonin receptor 3B gene (HTR3B) and treatment-resistant schizophrenia (TRS) in a Japanese population, Nagoya J Med Sci, 70, 11

Jiang, 1994, Anorectic response to amino acid imbalance: a selective serotonin3 effect?, Pharmacol Biochem Behav, 47, 59, 10.1016/0091-3057(94)90111-2

Johnson, 2004, Role of the serotonergic system in the neurobiology of alcoholism: implications for treatment, CNS Drugs, 18, 1105, 10.2165/00023210-200418150-00005

Johnson, 2006, A preliminary randomized, double-blind, placebo-controlled study of the safety and efficacy of ondansetron in the treatment of cocaine dependence, Drug Alcohol Depend, 84, 256, 10.1016/j.drugalcdep.2006.02.011

Johnson, 2002, Ondansetron reduces the craving of biologically predisposed alcoholics, Psychopharmacology (Berl), 160, 408, 10.1007/s00213-002-1002-9

Jones, 2002, The medical benefit of 5-HT research, Pharmacol Biochem Behav, 71, 555, 10.1016/S0091-3057(01)00745-6

Jonsson, 2004, Monoamine related functional gene variants and relationships to monoamine metabolite concentrations in CSF of healthy volunteers, BMC Psychiatry, 4, 4, 10.1186/1471-244X-4-4

Jordt, 2004, Mustard oils and cannabinoids excite sensory nerve fibres through the TRP channel ANKTM1, Nature, 427, 260, 10.1038/nature02282

Kaiser, 2004, Investigation of the association between 5-HT3A receptor gene polymorphisms and efficiency of antiemetic treatment with 5-HT3 receptor antagonists, Pharmacogenetics, 14, 271, 10.1097/00008571-200405000-00001

Kalantar, 2003, Familial aggregation of irritable bowel syndrome: a prospective study, Gut, 52, 1703, 10.1136/gut.52.12.1703

Kapeller, 2008, First evidence for an association of a functional variant in the microRNA-510 target site of the serotonin receptor-type 3E gene with diarrhea predominant irritable bowel syndrome, Hum Mol Genet, 17, 2967, 10.1093/hmg/ddn195

Kapeller, 2009, A coding variant in the serotonin receptor 3C subunit is associated with diarrhea-predominant irritable bowel syndrome, Gastroenterology, 136, A155, 10.1016/S0016-5085(09)60701-0

Karnovsky, 2003, A cluster of novel serotonin receptor 3-like genes on human chromosome 3, Gene, 319, 137, 10.1016/S0378-1119(03)00803-5

Kato, 2006, Effects of the serotonin type 2A, 3A and 3B receptor and the serotonin transporter genes on paroxetine and fluvoxamine efficacy and adverse drug reactions in depressed Japanese patients, Neuropsychobiology, 53, 186, 10.1159/000094727

Kato, 2010, Review and meta-analysis of antidepressant pharmacogenetic findings in major depressive disorder, Mol Psychiatry, 15, 473, 10.1038/mp.2008.116

Katounina, 1998, Synthesis and biological investigations of [18F]MR18445, a 5-HT3 receptor partial agonist, Bioorg Med Chem, 6, 789, 10.1016/S0968-0896(98)00035-2

Kayser, 2007, Mechanical, thermal and formalin-induced nociception is differentially altered in 5-HT1A−/−, 5-HT1B−/−, 5-HT2A−/−, 5-HT3A−/− and 5-HTT−/− knock-out male mice, Pain, 130, 235, 10.1016/j.pain.2006.11.015

Kelley, 2003, Targeted gene deletion of the 5-HT3A receptor subunit produces an anxiolytic phenotype in mice, Eur J Pharmacol, 461, 19, 10.1016/S0014-2999(02)02960-6

Kelley, 2003, A cytoplasmic region determines single-channel conductance in 5-HT3 receptors, Nature, 424, 321, 10.1038/nature01788

Kenakin, 2004, Allosteric modulators: the new generation of receptor antagonist, Mol Interv, 4, 222, 10.1124/mi.4.4.6

Kendler, 1991, The genetic epidemiology of bulimia nervosa, Am J Psychiatry, 148, 1627, 10.1176/ajp.148.12.1627

Kilpatrick, 1990, 1-(m-chlorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist, Eur J Pharmacol, 182, 193, 10.1016/0014-2999(90)90513-6

Kilpatrick, 1987, Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding, Nature, 330, 746, 10.1038/330746a0

Kim, 2005, Effect of ginseng saponins on a rat visceral hypersensitivity model, Biol Pharm Bull, 28, 2120, 10.1248/bpb.28.2120

Kim, 2005, Effects of Korean red ginseng extract on cisplatin-induced nausea and vomiting, Arch Pharm Res, 28, 680, 10.1007/BF02969358

Koike, 2005, Tropisetron improves deficits in auditory P50 suppression in schizophrenia, Schizophr Res, 76, 67, 10.1016/j.schres.2004.12.016

Kooyman, 1994, Interaction between enantiomers of mianserin and ORG3770 at 5-HT3 receptors in cultured mouse neuroblastoma cells, Neuropharmacology, 33, 501, 10.1016/0028-3908(94)90081-7

Krasowski, 1999, General anaesthetic actions on ligand-gated ion channels, Cell Mol Life Sci, 55, 1278, 10.1007/s000180050371

Kris, 2006, American Society of Clinical Oncology guideline for antiemetics in oncology: update 2006, Am J Clin Oncol, 24, 2932, 10.1200/JCO.2006.06.9591

Krzywkowski, 2008, High-frequency HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT3AB receptor, Proc Natl Acad Sci USA, 105, 722, 10.1073/pnas.0708454105

Krzywkowski, 2007, Naturally occurring variations in the human 5-HT3A gene profoundly impact 5-HT3 receptor function and expression, Pharmacogenet Genomics, 17, 255, 10.1097/FPC.0b013e3280117269

Kurzwelly, 2004, Pharmacological and electrophysiological properties of the naturally occurring Pro391Arg variant of the human 5-HT3A receptor, Pharmacogenetics, 14, 165, 10.1097/00008571-200403000-00004

Kyriakides, 1999, Management of opioid-induced pruritus: a role for 5-HT3 antagonists?, Br J Anaesth, 82, 439, 10.1093/bja/82.3.439

Lankiewicz, 2000, Phosphorylation of the 5-hydroxytryptamine3 (5-HT3) receptor expressed in HEK293 cells, Receptors Channels, 7, 9

Lecrubier, 1993, A randomized double-blind placebo-controlled study of tropisetron in the treatment of outpatients with generalized anxiety disorder, Psychopharmacology (Berl), 112, 129, 10.1007/BF02247373

Lee, 2007, Identification of ginsenoside interaction sites in 5-HT3A receptors, Neuropharmacology, 52, 1139, 10.1016/j.neuropharm.2006.12.001

Lee, 2008, Differential regulations of quercetin and its glycosides on ligand-gated ion channels, Biol Pharm Bull, 31, 611, 10.1248/bpb.31.611

Lembo, 2007, Influence of genetics on irritable bowel syndrome, gastro-oesophageal reflux and dyspepsia: a twin study, Aliment Pharmacol Ther, 25, 1343, 10.1111/j.1365-2036.2007.03326.x

Lennertz, 2010, A coding variant of the novel serotonin receptor subunit 5-HT3E influences sustained attention in schizophrenia patients, Eur Neuropsychopharmacol, 20, 414, 10.1016/j.euroneuro.2010.02.012

Levinson, 1998, Genome scan of schizophrenia, Am J Psychiatry, 155, 741

Levkovitz, 2005, The effect of Ondansetron on memory in schizophrenic patients, Brain Res Bull, 65, 291, 10.1016/j.brainresbull.2003.09.022

Levran, 2009, Heroin addiction in African Americans: a hypothesis-driven association study, Genes Brain Behav, 8, 531, 10.1111/j.1601-183X.2009.00501.x

Levy, 2001, Irritable bowel syndrome in twins: heredity and social learning both contribute to etiology, Gastroenterology, 121, 799, 10.1053/gast.2001.27995

Li, 2009, Familial risks of psychotic disorders and schizophrenia among siblings based on hospitalizations in Sweden, Psychiatry Res, 166, 1, 10.1016/j.psychres.2007.12.003

Liu, 2006, Herbal medicines for treatment of irritable bowel syndrome, Cochrane Database Syst Rev, 10.1002/14651858.CD004116.pub2

Lochner, 2010, Agonists and antagonists bind to an A–A interface in the heteromeric 5-HT3AB receptor, Biophys J, 98, 1494, 10.1016/j.bpj.2009.12.4313

Lummis, 1997, Radioligand binding and photoaffinity labelling studies show a direct interaction of phenothiazines at 5-HT3 receptors, Neuropharmacology, 36, 665, 10.1016/S0028-3908(97)00054-3

Lummis, 2008, The novel 5-HT3B receptor subunits brain1 and brain2 differentially alter 5-HT3 receptor function

Machu, 1994, Alcohols and anesthetics enhance the function of 5-hydroxytryptamine3 receptors expressed in Xenopus laevis oocytes, J Pharmacol Exp Ther, 271, 898

Madisch, 2004, Treatment of irritable bowel syndrome with herbal preparations: results of a double-blind, randomized, placebo-controlled, multi-centre trial, Aliment Pharmacol Ther, 19, 271, 10.1111/j.1365-2036.2004.01859.x

Maingret, 2001, The endocannabinoid anandamide is a direct and selective blocker of the background K(+) channel TASK-1, EMBO J, 20, 47, 10.1093/emboj/20.1.47

Malinowska, 1995, Inhibitory effect of ethanol on the 5-hydroxytryptamine-induced Bezold–Jarisch reflex—involvement of peripheral 5-HT3 receptors, Eur J Pharmacol, 293, 71, 10.1016/0926-6917(95)90020-9

Maricq, 1991, Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel, Science, 254, 432, 10.1126/science.1718042

Martinez-Martin, 2010, Parkinson disease: depression and anxiety in Parkinson disease, Nat Rev Neurol, 6, 243, 10.1038/nrneurol.2010.49

Maura, 1992, 5-Hydroxytryptamine3 receptors sited on cholinergic axon terminals of human cerebral cortex mediate inhibition of acetylcholine release, J Neurochem, 58, 2334, 10.1111/j.1471-4159.1992.tb10983.x

Mayer, 2002, The effect of the 5-HT3 receptor antagonist, alosetron, on brain responses to visceral stimulation in irritable bowel syndrome patients, Aliment Pharmacol Ther, 16, 1357, 10.1046/j.1365-2036.2002.01287.x

Maziade, 1995, Linkage results on 11Q21-22 in Eastern Quebec pedigrees densely affected by schizophrenia, Am J Med Genet, 60, 522, 10.1002/ajmg.1320600607

McCann, 1997, Effects of the 5-HT3 antagonist, ondansetron, on the behavioral and physiological effects of pentagastrin in patients with panic disorder and social phobia, Neuropsychopharmacology, 17, 360, 10.1016/S0893-133X(97)00085-7

McDougle, 2005, Neurochemistry in the pathophysiology of autism, J Clin Psychiatry, 66, 9

Meineke, 2008, Functional characterization of a -100_-102delAAG deletion–insertion polymorphism in the promoter region of the HTR3B gene, Pharmacogenet Genomics, 18, 219, 10.1097/FPC.0b013e3282f51092

Melke, 2003, A polymorphism in the serotonin receptor 3A (HTR3A) gene and its association with harm avoidance in women, Arch Gen Psychiatry, 60, 1017, 10.1001/archpsyc.60.10.1017

Michel, 2005, Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors, Gastroenterology, 128, 1317, 10.1053/j.gastro.2005.02.005

Mihic, 1997, Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors, Nature, 389, 385, 10.1038/38738

Millan, 2003, The neurobiology and control of anxious states, Prog Neurobiol, 70, 83, 10.1016/S0301-0082(03)00087-X

Millar, 2008, RIC-3: a nicotinic acetylcholine receptor chaperone, Br J Pharmacol, 153, S177, 10.1038/sj.bjp.0707661

Miquel, 2002, Differential subcellular localization of the 5-HT3-As receptor subunit in the rat central nervous system, Eur J Neurosci, 15, 449, 10.1046/j.0953-816x.2001.01872.x

Mitchell, 2008, Neurosteroid modulation of GABAA receptors: molecular determinants and significance in health and disease, Neurochem Int, 52, 588, 10.1016/j.neuint.2007.10.007

Miyake, 1995, Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species, Mol Pharmacol, 48, 407

Miyazawa, 2003, Structure and gating mechanism of the acetylcholine receptor pore, Nature, 423, 949, 10.1038/nature01748

Mizoguchi, 2009, New therapy for neuropathic pain, Int Rev Neurobiol, 85, 249, 10.1016/S0074-7742(09)85019-8

Monk, 2004, Identification and importance of N-glycosylation of the human 5-hydroxytryptamine3A receptor subunit, Biochem Pharmacol, 68, 1787, 10.1016/j.bcp.2004.06.034

Morales, 2002, Differential composition of 5-hydroxytryptamine3 receptors synthesized in the rat CNS and peripheral nervous system, J Neurosci, 22, 6732, 10.1523/JNEUROSCI.22-15-06732.2002

Morelli, 2009, Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure–activity relationships, Eur J Med Chem, 52, 3548, 10.1021/jm900018b

Morris, 2000, Upstream open reading frames as regulators of mRNA translation, Mol Cell Biol, 20, 8635, 10.1128/MCB.20.23.8635-8642.2000

Mott, 2001, Open probability of homomeric murine 5-HT3A serotonin receptors depends on subunit occupancy, J Physiol, 535, 427, 10.1111/j.1469-7793.2001.00427.x

Mukerji, 1996, Immunological characterization and transmembrane topology of 5-hydroxytryptamine3 receptors by functional epitope tagging, J Neurochem, 66, 1027, 10.1046/j.1471-4159.1996.66031027.x

Müller, 2004, Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron, Scand J Rheumatol Suppl, 44, 10.1080/03009740410007032

Niesler, 2001, Association between the 5′ UTR variant C178T of the serotonin receptor gene HTR3A and bipolar affective disorder, Pharmacogenetics, 11, 471, 10.1097/00008571-200108000-00002

Niesler, 2001, Serotonin receptor gene HTR3A variants in schizophrenic and bipolar affective patients, Pharmacogenetics, 11, 21, 10.1097/00008571-200102000-00003

Niesler, 2003, Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E, Gene, 310, 101, 10.1016/S0378-1119(03)00503-1

Niesler, 2007, Characterization of the novel human serotonin receptor subunits 5-HT3C, 5-HT3D, and 5-HT3E, Mol Pharmacol, 72, 8, 10.1124/mol.106.032144

Nothdurfter, 2010, Impact of lipid raft integrity on 5-HT3 receptor function and its modulation by antidepressants, Neuropsychopharmacology, 35, 1510, 10.1038/npp.2010.20

Nutt, 2006, Understanding the neurobiology of comorbidity in anxiety disorders, CNS Spectr, 11, 13, 10.1017/S1092852900025803

Oz, 2004, Differential effects of endogenous and synthetic cannabinoids on voltage-dependent calcium fluxes in rabbit T-tubule membranes: comparison with fatty acids, Eur J Pharmacol, 502, 47, 10.1016/j.ejphar.2004.08.052

Oz, 2002, Endogenous cannabinoid, anandamide, acts as a noncompetitive inhibitor on 5-HT3 receptor-mediated responses in Xenopus oocytes, Synapse, 46, 150, 10.1002/syn.10121

Oz, 2002, Direct noncompetitive inhibition of 5-HT(3) receptor-mediated responses by forskolin and steroids, Arch Biochem Biophys, 404, 293, 10.1016/S0003-9861(02)00279-5

Parker, 1996, Autoradiographic distribution of [3H]-(S)-zacopride-labelled 5-HT3 receptors in human brain, J Neurol Sci, 144, 119, 10.1016/S0022-510X(96)00211-0

Paterson, 2008, A novel, oral 5HT3 partial agonist, DDP733, improves overall response in patients with irritable bowel syndrome and constipation (IBS-c): a randomized, double blind, placebo-controlled, parallel-group, dose-ranging study, Gastroenterology, 134, A546, 10.1016/S0016-5085(08)62551-2

Paterson, 2008, A randomized, double-blind, placebo-controlled trial with a novel dual noradrenergic reuptake inhibitor (NARI) and 5-HT3 antagonist: results of a phase II 8-week study in female patients with diarrhea predominant irritable bowel syndrome (D-IBS), Gastroenterology, 134, A50, 10.1016/S0016-5085(08)60240-1

Pato, 1991, Sustained plasma concentrations of fluoxetine and/or norfluoxetine four and eight weeks after fluoxetine discontinuation, J Clin Psychopharmacol, 11, 224, 10.1097/00004714-199106000-00024

Pereira, 2002, Unconventional ligands and modulators of nicotinic receptors, J Neurobiol, 53, 479, 10.1002/neu.10146

Pertwee, 2009, Emerging strategies for exploiting cannabinoid receptor agonists as medicines, Br J Pharmacol, 156, 397, 10.1111/j.1476-5381.2008.00048.x

Peters, 2010, Novel structural determinants of single channel conductance and ion selectivity in 5-hydroxytryptamine type 3 and nicotinic acetylcholine receptors, Journal de Physiologie, 588, 587, 10.1113/jphysiol.2009.183137

Peters, 2010, 5-HT3 receptors

Preston, G. C. (1994). 5-HT3 antagonists and disorders of cognition. In: Racagni, G., Brunello, N., Langer, S.Z., editors. Recent advances in the treatment of neurodegenerative disorders and cognitive dysfunction. 7. International Academy of Biomedical Drug Research; Karger, Basel, Switzerland: 89–93.

Przegalinski, 2005, WIN 55, 212–2-induced reduction of cocaine hyperlocomotion: possible inhibition of 5-HT(3) receptor function, Eur J Pharmacol, 517, 68, 10.1016/j.ejphar.2005.05.014

Quirk, 2004, Three putative N-glycosylation sites within the murine 5-HT3A receptor sequence affect plasma membrane targeting, ligand binding, and calcium influx in heterologous mammalian cells, J Neurosci Res, 77, 498, 10.1002/jnr.20185

Racz, 2008, Anandamide effects on 5-HT(3) receptors in vivo, Eur J Pharmacol, 596, 98, 10.1016/j.ejphar.2008.08.012

Rajkumar, 2010, The auspicious role of the 5-HT3 receptor in depression: a probable neuronal target?, J Psychopharmacol, 24, 455, 10.1177/0269881109348161

Ramamoorthy, 2008, Antidepressant-like effects of serotonin type-3 antagonist, ondansetron: an investigation in behaviour-based rodent models, Behav Pharmacol, 19, 29, 10.1097/FBP.0b013e3282f3cfd4

Ramirez, 1996, Involvement of GABA systems in acetylcholine release induced by 5-HT3 receptor blockade in slices from rat entorhinal cortex, Brain Res, 712, 274, 10.1016/0006-8993(95)01471-3

Rammes, 2004, Antipsychotic drugs antagonize human serotonin type 3 receptor currents in a noncompetitive manner, Mol Psychiatry, 9, 846, 10.1038/sj.mp.4001490

Rammes, 2009, Identification of a domain which affects kinetics and antagonistic potency of clozapine at 5-HT3 receptors, PLoS ONE, 4, e6715, 10.1371/journal.pone.0006715

Rammes, 2007, Modulation of ligand-gated ion channels by antidepressants and antipsychotics, Mol Neurobiol, 35, 160, 10.1007/s12035-007-0006-1

Rapport, 1948, Serum vasoconstrictor, serotonin; isolation and characterization, J Biol Chem, 176, 1243, 10.1016/S0021-9258(18)57137-4

Rayes, 2009, Number and locations of agonist binding sites required to activate homomeric Cys-loop receptors, J Neurosci, 29, 6022, 10.1523/JNEUROSCI.0627-09.2009

Redrobe, 1997, Partial role of 5-HT2 and 5-HT3 receptors in the activity of antidepressants in the mouse forced swimming test, Eur J Pharmacol, 325, 129, 10.1016/S0014-2999(97)00115-5

Rehnström, 2009, Allelic variants in HTR3C show association with autism, Am J Med Genet B Neuropsychiatr Genet, 150B, 741, 10.1002/ajmg.b.30882

Ricci, 2005, Serotonin type 3 receptors stimulate offensive aggression in Syrian hamsters, Behav Brain Res, 156, 19, 10.1016/j.bbr.2004.05.003

Richardson, 1985, Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs, Nature, 316, 126, 10.1038/316126a0

Riyazi, 2007, The effect of the volatile oil from ginger rhizomes (Zingiber officinale), its fractions and isolated compounds on the 5-HT3 receptor complex and the serotoninergic system of the rat ileum, Planta Med, 73, 355, 10.1055/s-2007-967171

Rojas, 2008, Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor, Anesth Analg, 107, 469, 10.1213/ane.0b013e318172fa74

Rojas, 2010, Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function, Eur J Pharmacol, 626, 193, 10.1016/j.ejphar.2009.10.002

Rosier, 1995, Regional assignment of 68 new human gene transcripts on chromosome 11, Genome Res, 5, 60, 10.1101/gr.5.1.60

Rueffert, 2009, Do variations in the 5-HT3A and 5-HT3B serotonin receptor genes (HTR3A and HTR3B) influence the occurrence of postoperative vomiting?, Anesth Analg, 109, 1442, 10.1213/ane.0b013e3181b2359b

Rupprecht, 2001, Neuroactive steroids: molecular mechanisms of action and implications for neuropsychopharmacology, Brain Res Brain Res Rev, 37, 59, 10.1016/S0165-0173(01)00123-0

Rüsch, 2007, Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital, Eur J Pharmacol, 573, 60, 10.1016/j.ejphar.2007.07.009

Ryan, 2009, Ginger for chemotherapy-related nausea in cancer patients: a URCC CCOP randomized, double-blind, placebo-controlled clinical trial of 644 cancer patients, J Clin Oncol, 27, 10.1200/jco.2009.27.15_suppl.9511

Sakurai-Yamashita, 2000, Differential localization of 5-hydroxytryptamine3 and 5-hydroxytryptamine4 receptors in the human rectum, Life Sci, 66, 31, 10.1016/S0024-3205(99)00558-5

Samborski, 2004, Intra-articular treatment of arthritides and activated osteoarthritis with the 5-HT3 receptor antagonist tropisetron. A double-blind study compared with methylprednisolone, Scand J Rheumatol Suppl, 51, 10.1080/03009740410007050

Sato, 1998, Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut, J Med Chem, 41, 3015, 10.1021/jm9801004

Scarpellini, 2008, Renzapride: a new drug for the treatment of constipation in the irritable bowel syndrome, Expert Opin Investig Drugs, 17, 1663, 10.1517/13543784.17.11.1663

Schuhmacher, 2009, Influence of 5-HT3 receptor subunit genes HTR3A, HTR3B, HTR3C, HTR3D and HTR3E on treatment response to antipsychotics in schizophrenia, Pharmacogenet Genomics, 19, 843, 10.1097/FPC.0b013e3283313296

Schworer, 1995, Relief of cholestatic pruritus by a novel class of drugs: 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists: effectiveness of ondansetron, Pain, 61, 33, 10.1016/0304-3959(94)00145-5

Schworer, 1993, Treatment of pruritus: a new indication for serotonin type 3 receptor antagonists, Clin Investig, 71, 659, 10.1007/BF00184497

Sepulveda, 1994, Chlorpromazine and QX222 block 5-HT3 receptors in N1E-115 neuroblastoma cells, Neuropharmacology, 33, 493, 10.1016/0028-3908(94)90080-9

Silverstone, 1992, Does ondansetron attenuate amphetamine-induced behaviour in human volunteers?, Psychopharmacology (Berl), 107, 140, 10.1007/BF02244979

Simmen, 2006, Binding of STW 5 (Iberogast) and its components to intestinal 5-HT, muscarinic M3, and opioid receptors, Phytomedicine, 13, 51, 10.1016/j.phymed.2006.03.012

Simpson, 1992, Concentration of ondansetron in cerebrospinal fluid following oral dosing in volunteers, Psychopharmacology (Berl), 109, 497, 10.1007/BF02247730

Siniscalchi, 1991, Influence of acute and chronic chlorimipramine treatment on the 5-HT receptor-mediated modulation of acetylcholine release from the cerebral cortex of freely moving guinea-pigs, Br J Pharmacol, 102, 837, 10.1111/j.1476-5381.1991.tb12262.x

Sirota, 2000, Use of the selective serotonin 3 receptor antagonist ondansetron in the treatment of neuroleptic-induced tardive dyskinesia, Am J Psychiatry, 157, 287, 10.1176/appi.ajp.157.2.287

Smöller, 2003, Family, twin, and adoption studies of bipolar disorder, Am J Med Genet C Semin Med Genet, 123C, 48, 10.1002/ajmg.c.20013

Sneyd, 1998, A meta-analysis of nausea and vomiting following maintenance of anaesthesia with propofol or inhalational agents, Eur J Anaesthesiol, 15, 433, 10.1097/00003643-199807000-00009

Solt, 2005, General anesthetic-induced channel gating enhancement of 5-hydroxytryptamine type 3 receptors depends on receptor subunit composition, J Pharmacol Exp Ther, 315, 771, 10.1124/jpet.105.090621

Spier, 2000, The role of tryptophan residues in the 5-Hydroxytryptamine(3) receptor ligand binding domain, J Biol Chem, 275, 5620, 10.1074/jbc.275.8.5620

Spier, 1999, Antibodies against the extracellular domain of the 5-HT3 receptor label both native and recombinant receptors, Brain Res Mol Brain Res, 67, 221, 10.1016/S0169-328X(99)00055-8

Stevens, 2005, Molecular properties important for inhaled anesthetic action on human 5-HT3A receptors, Anesth Analg, 100, 1696, 10.1213/01.ANE.0000151720.36988.09

Stevens, 2005, Modulation of human 5-hydroxytryptamine type 3AB receptors by volatile anesthetics and n-alcohols, J Pharmacol Exp Ther, 314, 338, 10.1124/jpet.105.085076

Stratz, 2000, The use of 5-HT3 receptor antagonists in various rheumatic diseases—a clue to the mechanism of action of these agents in fibromyalgia?, Scand J Rheumatol Suppl, 113, 66

Stratz, 2004, Treatment of chronic low back pain with tropisetron, Scand J Rheumatol Suppl, 76, 10.1080/03009740410007113

Stratz, 2004, Treatment of systemic sclerosis with the 5-HT3 receptor antagonist tropisetron, Scand J Rheumatol Suppl, 59, 10.1080/03009740410007078

Stratz, 2008, Identification of 5-HT3 receptors on human platelets: increased surface immunoreactivity after activation with adenosine diphosphate (ADP) and thrombin receptor-activating peptide (TRAP), Thromb Haemost, 99, 784, 10.1160/TH07-10-0630

Stratz, 2002, Treatment of tendopathies with tropisetron, Rheumatol Int, 22, 219, 10.1007/s00296-002-0233-8

Sugai, 2006, The effect of 5-hydroxytryptamine 3A and 3B receptor genes on nausea induced by paroxetine, Pharmacogenomics J, 6, 351, 10.1038/sj.tpj.6500382

Sun, 2008, Modulation of 5-HT3 receptor desensitization by the light chain of microtubule-associated protein 1B expressed in HEK 293 cells, J Physiol, 586, 751, 10.1113/jphysiol.2007.136440

Suzuki, 2002, Superficial NK1-expressing neurons control spinal excitability through activation of descending pathways, Nat Neurosci, 5, 1319, 10.1038/nn966

Suzuki, 2004, Descending facilitatory control of mechanically evoked responses is enhanced in deep dorsal horn neurones following peripheral nerve injury, Brain Res, 1019, 68, 10.1016/j.brainres.2004.05.108

Suzuki, 2004, Inhibitory effect of glucocorticoids on human-cloned 5-hydroxytryptamine3A receptor expressed in Xenopus oocytes, Anesthesiology, 101, 660, 10.1097/00000542-200409000-00014

Thompson, 2007, The antimalarial drugs quinine, chloroquine and mefloquine are antagonists at 5-HT3 receptors, Br J Pharmacol, 151, 666, 10.1038/sj.bjp.0707238

Thompson, 2006, 5-HT3 receptors, Curr Pharm Des, 12, 3615, 10.2174/138161206778522029

Thompson, 2007, The 5-HT3 receptor as a therapeutic target, Expert Opin Ther Targets, 11, 527, 10.1517/14728222.11.4.527

Thompson, 2008, Antimalarial drugs inhibit human 5-HT(3) and GABA(A) but not GABA(C) receptors, Br J Pharmacol, 153, 1686, 10.1038/bjp.2008.34

Thompson, 2006, Characterization of 5-HT3 receptor mutations identified in schizophrenic patients, J Mol Neurosci, 30, 273, 10.1385/JMN:30:3:273

Tremblay, 2003, Variations in the 5-hydroxytryptamine type 3B receptor gene as predictors of the efficacy of antiemetic treatment in cancer patients, J Clin Oncol, 21, 2147, 10.1200/JCO.2003.05.164

Tsuang, 1996, Genetic influences on DSM-III-R drug abuse and dependence: a study of 3,372 twin pairs, Am J Med Genet, 67, 473, 10.1002/(SICI)1096-8628(19960920)67:5<473::AID-AJMG6>3.0.CO;2-L

Tzvetkov, 2007, Tissue-specific alternative promoters of the serotonin receptor gene HTR3B in human brain and intestine, Gene, 386, 52, 10.1016/j.gene.2006.08.002

Ueta, 2007, Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors, Reg Anesth Pain Med, 32, 462, 10.1097/00115550-200711000-00002

Unwin, 2005, Refined structure of the nicotinic acetylcholine receptor at 4A resolution, J Mol Biol, 346, 967, 10.1016/j.jmb.2004.12.031

Urban, 2008, The site of anesthetic action, Handb Exp Pharmacol, 3, 10.1007/978-3-540-74806-9_1

Urban, 2006, Interactions of anesthetics with their targets: non-specific, specific or both?, Pharmacol Ther, 111, 729, 10.1016/j.pharmthera.2005.12.005

Usyatinsky, 2008, AMR-SER-67: a novel and selective high affinity 5-HT3 receptor partial agonist, Fund Clin Pharmacol, 22

Van Hooft, 1995, Phosphorylation controls conductance of 5-HT3 receptor ligand-gated ion channels, Recept Channels, 3, 7

Verberg, 2005, Hyperemesis gravidarum, a literature review, Hum Reprod Update, 11, 527, 10.1093/humupd/dmi021

Vries De, 2007, Serotonin receptor 3a polymorphism C178t is associated with visceral hypersensitivity in GERD, Gastroenterology, 132, A276

Wallis, 1978, The action of 5-hydroxytryptamine on single neurones of the rabbit superior cervical ganglion, Neuropharmacology, 17, 1023, 10.1016/0028-3908(78)90028-X

Walstab, 2007, Aequorin luminescence-based assay for 5-hydroxytryptamine (serotonin) type 3 receptor characterization, Anal Biochem, 368, 185, 10.1016/j.ab.2007.06.007

Walstab, 2008, Naturally occurring variants in the HTR3B gene significantly alter properties of human heteromeric 5-hydroxytryptamine-3A/B receptors, Pharmacogenet Genomics, 18, 793, 10.1097/FPC.0b013e3283050117

Walstab, J., Hammer, C., Lasitschka, F., Moeller, D., Connolly, C. N., Rappold, G., et al. (2010). RIC-3 exclusively enhances the surface expression of human homomeric 5-hydroxytryptamine type 3A (5-HT3A) receptors, despite direct interactions with 5-HT3A, C, D and E subunits. J Biol Chem, Jun 3 [Epub ahead of print].

Wang, 2009, The antiemetic interaction of Delta9-tetrahydrocannabinol when combined with tropisetron or dexamethasone in the least shrew, Pharmacol Biochem Behav, 91, 367, 10.1016/j.pbb.2008.08.008

Washburn, 1994, Anorectic responses to dietary amino acid imbalance: effects of vagotomy and tropisetron, Am J Physiol, 266, R1922

Weiss, 1995, Assignment of a human homolog of the mouse Htr3 receptor gene to chromosome 11q23.1-q23.2, Genomics, 29, 304, 10.1006/geno.1995.1254

Wetzel, 1998, Functional antagonism of gonadal steroids at the 5-hydroxytryptamine type 3 receptor, Mol Endocrinol, 12, 1441, 10.1210/mend.12.9.0163

White, 1991, Ondansetron in treatment of schizophrenia, Lancet, 337, 1173, 10.1016/0140-6736(91)92851-R

Windemuth, 2008, Physiogenomic analysis of localized FMRI brain activity in schizophrenia, Ann Biomed Eng, 36, 877, 10.1007/s10439-008-9475-2

Wittmann, 2006, The effects of morphine on human 5-HT3A receptors, Anesth Analg, 103, 747, 10.1213/01.ane.0000229706.84471.4d

Wittmann, 2008, The effects of fentanyl-like opioids and hydromorphone on human 5-HT3A receptors, Anesth Analg, 107, 107, 10.1213/ane.0b013e31817342c2

Wolf, 2000, Preclinical and clinical pharmacology of the 5-HT3 receptor antagonists, Scand J Rheumatol Suppl, 113, 37, 10.1080/030097400446625

Wong, 1995, The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro, Br J Pharmacol, 114, 851, 10.1111/j.1476-5381.1995.tb13282.x

Woolley, 1954, A biochemical and pharmacological suggestion about certain mental disorders, Proc Natl Acad Sci USA, 40, 228, 10.1073/pnas.40.4.228

Wu, 2000, Non-competitive inhibition of 5-HT3 receptor-mediated currents by progesterone in rat nodose ganglion neurons, Neurosci Lett, 278, 37, 10.1016/S0304-3940(99)00883-6

Yamada, 2006, Distinguishable haplotype blocks in the HTR3A and HTR3B region in the Japanese reveal evidence of association of HTR3B with female major depression, Biol Psychiatry, 60, 192, 10.1016/j.biopsych.2005.11.008

Zeitz, 2002, The 5-HT3 subtype of serotonin receptor contributes to nociceptive processing via a novel subset of myelinated and unmyelinated nociceptors, J Neurosci, 22, 1010, 10.1523/JNEUROSCI.22-03-01010.2002

Zhang, 2006, Beneficial effects of ondansetron as an adjunct to haloperidol for chronic, treatment-resistant schizophrenia: a double-blind, randomized, placebo-controlled study, Schizophr Res, 88, 102, 10.1016/j.schres.2006.07.010

Zhang, 1997, Volatile general anaesthetic actions on recombinant nACh alpha 7, 5-HT3 and chimeric nACh alpha 7-5-HT3 receptors expressed in Xenopus oocytes, Br J Pharmacol, 120, 353, 10.1038/sj.bjp.0700934

Zhou, 1996, Pharmacologic characteristics of potentiation of 5-HT3 receptors by alcohols and diethyl ether in NCB-20 neuroblastoma cells, J Pharmacol Exp Ther, 278, 732

Zoldan, 1995, Psychosis in advanced Parkinson's disease: treatment with ondansetron, a 5-HT3 receptor antagonist, Neurology, 45, 1305, 10.1212/WNL.45.7.1305

Zoldan, 1996, Ondansetron, a 5-HT3 antagonist for visual hallucinations and paranoid delusional disorder associated with chronic L-DOPA therapy in advanced Parkinson's disease, Adv Neurol, 69, 541

Zygmunt, 1999, Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide, Nature, 400, 452, 10.1038/22761