Target Information
Target General Infomation | |||||
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Target ID |
T84160
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Former ID |
TTDS00106
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Target Name |
5-Hydroxytryptamine 3 receptor
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Synonyms |
5-HT-3; 5-HT3 receptor; 5-HT3R; 5-hydroxytryptamine receptor 3; 5-hydroxytryptamine receptor type 3; Serotonin-gated ion channel receptor
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Target Type |
Successful
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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] | |||||
Sleep apnea [ICD10: G47.3] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
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.
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BioChemical Class |
Ion transport
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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 523218 | ClinicalTrials.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 525122 | ClinicalTrials.gov (NCT02389881) Safety, Tolerability, and Pharmacokinetics of Multiple-Dose TAK-058 in Healthy Participants. U.S. National Institutes of Health. | ||||
Ref 534522 | Determination 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 536188 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | ||||
Ref 536361 | Natural 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 544822 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001226) | ||||
Ref 544852 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001323) | ||||
Ref 544942 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001602) | ||||
Ref 544973 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001751) | ||||
Ref 544983 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001786) | ||||
Ref 544997 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830) | ||||
Ref 545075 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002051) | ||||
Ref 545348 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002948) | ||||
Ref 545507 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003534) | ||||
Ref 545543 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003649) | ||||
Ref 547758 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090) | ||||
Ref 526818 | 5-HT3 receptor antagonist effects of DAT-582, (R) enantiomer of AS-5370. Eur J Pharmacol. 1992 Jun 17;216(3):435-40. | ||||
Ref 526839 | Pancopride, 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 529185 | Analgesic 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 533337 | Binding 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 533601 | Inhibitory 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 533740 | Microdialysis 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 534071 | Cataractogenesis in rats induced by in utero exposure to RG 12915, a 5-HT3 antagonist. Fundam Appl Toxicol. 1995 Sep;27(2):270-6. | ||||
Ref 534182 | Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83-90. | ||||
Ref 534302 | The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging. 1997 Jan-Feb;18(1):21-8. | ||||
Ref 534513 | Effect 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 535971 | 5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13. | ||||
Ref 536039 | The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. | ||||
Ref 536188 | Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. | ||||
Ref 536290 | New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7. | ||||
Ref 537687 | BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4. | ||||
Ref 537932 | Reduction 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 538141 | Treatment 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 544998 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830) | ||||
Ref 547759 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090) | ||||
Ref 547882 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129) | ||||
Ref 549563 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040805) |
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