Target Information

Target General Infomation
Target ID
T84160
Former ID
TTDS00106
Target Name
5-Hydroxytryptamine 3 receptor
Synonyms
5-HT-3; 5-HT3 receptor; 5-HT3R; 5-hydroxytryptamine receptor 3; 5-hydroxytryptamine receptor type 3; Serotonin-gated ion channel receptor
Target Type
Successful
Disease Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Chemotherapy-induced nausea [ICD9: 787, 787.0; ICD10: R11]
Chemotherapy-induced emesis [ICD9: 787; ICD10: R11]
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66]
Emesis [ICD9: 787; ICD10: R11]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Nausea and vomiting associated with chemotherapy [ICD10: R11]
Nausea; Vomiting; Testicular germ cell tumor; Emesis [ICD9: 140-199, 183, 186, 210-229, 220, 222.0, 787, 787.0; ICD10: C00-C75, C56, C62, C7A, C7B, D10-D36, D27, D29.2, D3A, R11]
Nausea [ICD10: R11]
Schizophrenia [ICD9: 295; ICD10: F20]
Sleep apnea [ICD10: G47.3]
Vomiting and nausea [ICD9: 787, 787.0; ICD10: R11]
Function
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel.
BioChemical Class
Ion transport
Drugs and Mode of Action
Drug(s) Granisetron Drug Info Approved Nausea and vomiting associated with chemotherapy [551871]
Ondansetron Drug Info Approved Chemotherapy-induced nausea [536361], [539441]
YM060 Drug Info Phase 4 Irritable bowel syndrome [523218]
Lerisetron Drug Info Phase 3 Nausea; Vomiting; Testicular germ cell tumor; Emesis [536188]
Pancopride Drug Info Phase 3 Nausea [544973]
KB-6806 Drug Info Phase 2 Chemotherapy-induced emesis [536188]
Ondansetron Drug Info Phase 2 Alcohol use disorders [536361], [539441]
ADR-851 Drug Info Phase 1 Vomiting and nausea [544852]
TAK-058 Drug Info Phase 1 Schizophrenia [525122]
RG-12915 Drug Info Discontinued in Phase 3 Nausea [544983]
DAT-582 Drug Info Discontinued in Phase 2 Nausea [544822]
Lurosetron Drug Info Discontinued in Phase 2 Emesis [545348]
SR-57227 Drug Info Discontinued in Phase 2 Major depressive disorder [467653], [544942]
Mirisetron maleate Drug Info Discontinued in Phase 1 Anxiety disorder [545543]
SEP-226332 Drug Info Discontinued in Phase 1 Sleep apnea [547881]
GK-128 Drug Info Terminated Emesis [545075]
GR-65630 Drug Info Terminated Emesis [545507]
SC-52150 Drug Info Terminated Emesis [544997]
SDZ-ICM-567 Drug Info Terminated Anxiety disorder [534522]
SRSS-021 Drug Info Terminated Emesis [547758]
Modulator ADR-851 Drug Info [529185]
GK-128 Drug Info [534513]
GR-65630 Drug Info [533337]
Lurosetron Drug Info [550949]
Mirisetron maleate Drug Info [534302]
SC-52150 Drug Info [544998]
SR-57227 Drug Info [534182]
YM060 Drug Info [533601]
Antagonist BRL 43694A Drug Info [537687]
Ciproxifan Drug Info [536039]
DAT-582 Drug Info [526818]
Granisetron Drug Info [536290], [537932]
KB-6806 Drug Info [536188]
Lerisetron Drug Info [536188]
LY278584 Drug Info [535971]
RG-12915 Drug Info [534071]
SDZ-ICM-567 Drug Info [533740]
SEP-226332 Drug Info [547882]
SRSS-021 Drug Info [547759]
TAK-058 Drug Info [549563], [551871]
Agonist Ondansetron Drug Info [538141]
Inhibitor Pancopride Drug Info [526839]
References
Ref 467653(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4316).
Ref 523218ClinicalTrials.gov (NCT01225237) A Study to Evaluate Efficacy of Ramosetron on Diarrhea-predominant Irritable Bowel Syndrome (IBS) in Male Patients. U.S. National Institutes of Health.
Ref 525122ClinicalTrials.gov (NCT02389881) Safety, Tolerability, and Pharmacokinetics of Multiple-Dose TAK-058 in Healthy Participants. U.S. National Institutes of Health.
Ref 534522Determination of SDZ ICM 567 in blood and muscle microdialysis samples by microbore liquid chromatography with ultraviolet and fluorescence detection. J Chromatogr B Biomed Sci Appl. 1997 Oct 24;700(1-2):191-200.
Ref 536188Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 539441(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2290).
Ref 544822Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001226)
Ref 544852Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001323)
Ref 544942Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001602)
Ref 544973Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001751)
Ref 544983Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001786)
Ref 544997Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)
Ref 545075Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002051)
Ref 545348Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002948)
Ref 545507Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003534)
Ref 545543Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003649)
Ref 547758Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)
Ref 547881Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 5268185-HT3 receptor antagonist effects of DAT-582, (R) enantiomer of AS-5370. Eur J Pharmacol. 1992 Jun 17;216(3):435-40.
Ref 526839Pancopride, a potent and long-acting 5-HT3 receptor antagonist, is orally effective against anticancer drug-evoked emesis. Eur J Pharmacol. 1992 Nov 10;222(2-3):257-64.
Ref 529185Analgesic effects of S and R isomers of the novel 5-HT3 receptor antagonists ADR-851 and ADR-882 in rats. Eur J Pharmacol. 1991 Oct 29;204(1):117-9.
Ref 533337Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species. Eur J Pharmacol. 1989 Jan 10;159(2):157-64.
Ref 533601Inhibitory effect of YM060 on 5-HT3 receptor-mediated depolarization in colonic myenteric neurons of the guinea pig. Eur J Pharmacol. 1995 Sep 5;283(1-3):107-12.
Ref 533740Microdialysis sampling to determine the pharmacokinetics of unbound SDZ ICM 567 in blood and brain in awake, freely-moving rats. Pharm Res. 1995 Feb;12(2):291-4.
Ref 534071Cataractogenesis in rats induced by in utero exposure to RG 12915, a 5-HT3 antagonist. Fundam Appl Toxicol. 1995 Sep;27(2):270-6.
Ref 534182Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83-90.
Ref 534302The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging. 1997 Jan-Feb;18(1):21-8.
Ref 534513Effect of a novel 5-hydroxytryptamine3 (5-HT3) receptor antagonist, GK-128, on 5-HT3 receptors mediating contractions and relaxations in guinea-pig distal colon. Gen Pharmacol. 1997 Sep;29(3):353-9.
Ref 5359715-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13.
Ref 536039The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
Ref 536188Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 536290New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.
Ref 537687BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4.
Ref 537932Reduction of rectal sensitivity and post-prandial motility by granisetron, a 5 HT3-receptor antagonist, in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1993 Apr;7(2):175-80.
Ref 538141Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70.
Ref 544998Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)
Ref 547759Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)
Ref 547882Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)
Ref 549563Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040805)
Ref 550949US patent application no. 7,932,267, Use of α-glucosidase inhibitors to treat alphavirus infections.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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