General Information of Drug Therapeutic Target (DTT) (ID: TTNXLKE)

DTT Name 5-HT 3 receptor (5HT3R)
Synonyms 5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3
Gene Name NO-GeName
DTT Type
Successful target
[1]
Related Disease
Nausea/vomiting [ICD-11: MD90]
BioChemical Class
GPCR rhodopsin
UniProt ID
NOUNIPROTAC
TTD ID
T84160
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.

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
4 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Granisetron DMIUW25 Nausea and vomiting MD90 Approved [1], [2]
Ondansetron DMOTQ1I Chemotherapy-induced nausea MD90 Approved [3]
Ramosetron DMH7GN8 Nausea and vomiting MD90 Approved [4]
Y-25130 DMDPM7R Nausea and vomiting MD90 Approved [5]
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16 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lerisetron DMOTCIU Nausea MD90 Phase 3 [6]
Litoxetine DMKZRBP Mood disorder 6A60-6E23 Phase 3 [7]
Pancopride DMIRYU9 Nausea MD90 Phase 3 [8]
Renzapride DM7HQNX Irritable bowel syndrome DD91.0 Phase 3 [9]
Zatosetron maleate DMWDEFC Anxiety disorder 6B00-6B0Z Phase 3 [10]
AD04 DMLV9GS Alcohol dependence 6C40.2 Phase 2 [11]
DDP-225 DM9REBL Irritable bowel syndrome DD91.0 Phase 2 [12]
KB-6806 DMZ4MCG Chemotherapy-induced nausea MD90 Phase 2 [6]
Lintopride DMSHGWN Nausea MD90 Phase 2 [13]
Pumosetrag DMBUSNL Irritable bowel syndrome DD91.0 Phase 2 [14]
ADR-851 DM6NUCA Nausea and vomiting MD90 Phase 1 [15]
BIMU-1 DMBTSZD Cognitive impairment 6D71 Phase 1 [16]
CVN058 DMTSIYZ Schizophrenia 6A20 Phase 1 [17]
ITASETRON DMY1DFK Nausea MD90 Phase 1 [12]
TAK-058 DMX9EA0 Schizophrenia 6A20 Phase 1 [18], [19]
Tedatioxetine DMV5LGJ Generalized anxiety disorder 6B00 Phase 1 [12]
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⏷ Show the Full List of 16 Clinical Trial Drug(s)
17 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
RG-12915 DMXV28I Nausea MD90 Discontinued in Phase 3 [20]
BRL-46470 DMIHSOG Anxiety disorder 6B00-6B0Z Discontinued in Phase 2 [21]
DAT-582 DMY3M0J Nausea MD90 Discontinued in Phase 2 [22]
E-3620 DMWF95G Gastric motility disorder DA21 Discontinued in Phase 2 [12]
Fabesetron DMMSFK0 Irritable bowel syndrome DD91.0 Discontinued in Phase 2 [23]
Lurosetron DMYR2U3 Vomiting MD90 Discontinued in Phase 2 [24]
SR-57227 DMV4FT2 Major depressive disorder 6A70.3 Discontinued in Phase 2 [25]
Mirisetron maleate DMC2V5J Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [26]
SEP-226332 DMCQI25 Obstructive sleep apnea 7A41 Discontinued in Phase 1 [27]
WAY-100289 DM3GD7V Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [28]
BP4.879a DMN8FAG Schizophrenia 6A20 Terminated [29]
CR-3124 DM1MBG9 Substance use disorder 6C4Z Terminated [30]
GK-128 DM4RKDU Vomiting MD90 Terminated [31]
GR-65630 DMRPE3D Vomiting MD90 Terminated [32]
SC-52150 DMKWJ59 Vomiting MD90 Terminated [33]
SDZ-ICM-567 DMN5IY7 Anxiety disorder 6B00-6B0Z Terminated [34]
SRSS-021 DM8MZWR Vomiting MD90 Terminated [35]
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⏷ Show the Full List of 17 Discontinued Drug(s)
6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(R)-zacopride DMT6J51 Discovery agent N.A. Investigative [36]
BRL 43694A DMTM7W0 Discovery agent N.A. Investigative [37]
Ciproxifan DM9N8WM Dementia 6D80-6D86 Investigative [38]
S-21007 DMOJ9N6 Discovery agent N.A. Investigative [39]
SC-52491 DMJ576C Discovery agent N.A. Investigative [40]
SC-54750 DMEUTXG Discovery agent N.A. Investigative [40]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1 New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7.
2 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.
3 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.
4 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.
5 The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305.
6 Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
7 Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Eur J Pharmacol. 1993 Mar 2;232(2-3):139-45.
8 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.
9 Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome. Drugs R D. 2008;9(1):37-63.
10 Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. J Clin Psychopharmacol. 1999 Apr;19(2):125-31.
11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
13 The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
14 Novel partial 5HT3 agonist pumosetrag reduces acid reflux events in uninvestigated GERD patients after a standard refluxogenic meal: a randomized, double-blind, placebo-controlled pharmacodynamic study.Neurogastroenterol Motil.2014 Jan;26(1):13-20.
15 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.
16 Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45.
17 Clinical pipeline report, company report or official report of Cerevance.
18 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040805)
19 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
20 Cataractogenesis in rats induced by in utero exposure to RG 12915, a 5-HT3 antagonist. Fundam Appl Toxicol. 1995 Sep;27(2):270-6.
21 Evidence that the atypical 5-HT3 receptor ligand, [3H]-BRL46470, labels additional 5-HT3 binding sites compared to [3H]-granisetron. Br J Pharmacol. 1995 Sep;116(2):1781-8.
22 5-HT3 receptor antagonist effects of DAT-582, (R) enantiomer of AS-5370. Eur J Pharmacol. 1992 Jun 17;216(3):435-40.
23 Pharmacological characterization of FK1052, a dihydropyridoindole derivative, as a new serotonin 3 and 4 dual receptor antagonist. J Pharmacol Exp Ther. 1993 May;265(2):752-8.
24 US patent application no. 7,932,267, Use of α-glucosidase inhibitors to treat alphavirus infections.
25 Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83-90.
26 The effects of 5-HT3 receptor antagonists on cognitive performance in aged monkeys. Neurobiol Aging. 1997 Jan-Feb;18(1):21-8.
27 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020129)
28 The selective 5-HT3 receptor antagonist, WAY100289, enhances spatial memory in rats with ibotenate lesions of the forebrain cholinergic projection system. Psychopharmacology (Berl). 1995 Feb;117(3):318-32.
29 5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13.
30 Physicochemical and biopharmaceutical characterization of endo-2-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one (CR312... J Pharm Sci. 2006 Dec;95(12):2706-21.
31 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.
32 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.
33 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001830)
34 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.
35 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019090)
36 R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):283-9.
37 BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4.
38 The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20.
39 Effects of S-21007, a potent 5-HT3 partial agonist, in mouse anxiety. Zhongguo Yao Li Xue Bao. 1999 Sep;20(9):805-12.
40 Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5509-12.