General Information of DTT (ID: TTPC4TU)

DTT Name 5-HT 3A receptor (HTR3A) DTT Info
Gene Name HTR3A

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
6 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alosetron DML2A03 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [1]
Dolasetron DMMG26Z Nausea MD90 Approved [2]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [3]
Palonosetron DMBHMOX Nausea MD90 Approved [4]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [5]
Tropisetron DMNSJ7V Fibromyalgia MG30.01 Approved [3]
------------------------------------------------------------------------------------
⏷ Show the Full List of 6 Approved Drug(s)
1 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cilansetron DMP0NGX Irritable bowel syndrome DD91.0 Phase 3 [6]
------------------------------------------------------------------------------------
5 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BEMESETRON DMSPJX9 N. A. N. A. Discontinued in Phase 3 [7]
Norcisapride DMJSKUI Gastroesophageal reflux disease DA22.Z Discontinued in Phase 2 [8]
YM-114 DML2IXO Nausea MD90 Discontinued in Phase 2 [9]
AS-8112 DMIFDPL Vomiting MD90 Terminated [11]
BP4.879a DMN8FAG Schizophrenia 6A20 Terminated [12]
------------------------------------------------------------------------------------
1 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
ATI-17000 DMZJVR5 Irritable bowel syndrome DD91.0 Preclinical [10]
------------------------------------------------------------------------------------
35 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid DMKF3U6 Discovery agent N.A. Investigative [13]
(S)-zacopride DM6BON2 Discovery agent N.A. Investigative [14]
1-(biphenyl-4-yl)-3-(4-(piperidin-1-yl)butyl)urea DM5KZ74 Discovery agent N.A. Investigative [15]
1-phenylbiguanide DMA4XGL Discovery agent N.A. Investigative [16]
10,11-dihydro-5H-dibenzo[b,f]azepine DMS5ICY Discovery agent N.A. Investigative [17]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole DMCG1HE Discovery agent N.A. Investigative [18]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole DM1V7EF Discovery agent N.A. Investigative [19]
2-(4-Methyl-piperazin-1-yl)-quinoline DMB8OY6 Discovery agent N.A. Investigative [20]
2-methyl-5-HT DM1S5CB N. A. N. A. Investigative [21]
3alpha-(1'-Methyl-2'-Indolecarbonyloxy)-tropane DMCNX34 Discovery agent N.A. Investigative [22]
3alpha-(2'-Indolecarbonyloxy)-nortropane DM3BRYJ Discovery agent N.A. Investigative [22]
4-((naphthalen-2-yloxy)methyl)piperidine DMIQHYZ Discovery agent N.A. Investigative [23]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [24]
4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane DMA9DHE Discovery agent N.A. Investigative [25]
5,6-dichloro-3,4-dihydroquinazolin-2-amine DMN1S35 Discovery agent N.A. Investigative [26]
5-chloro-3,4-dihydroquinazolin-2-amine DMKEFJ0 Discovery agent N.A. Investigative [26]
5-hydroxyindole DMI0GMB Discovery agent N.A. Investigative [27]
6-(4-Methyl-piperazin-1-yl)-phenanthridine DM1HAWR Discovery agent N.A. Investigative [20]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile DM6I5K1 Discovery agent N.A. Investigative [23]
A-987306 DMU34BK Discovery agent N.A. Investigative [28]
bilobalide DM09Z35 Discovery agent N.A. Investigative [29]
BRL-24682 DMSB4EW Discovery agent N.A. Investigative [30]
CP-810123 DMXDG13 Discovery agent N.A. Investigative [25]
FLUPENTIXOLE DMELB5S Discovery agent N.A. Investigative [17]
MESULERGINE DMKGWAH Discovery agent N.A. Investigative [31]
meta-chlorphenylbiguanide DMEA8GP Discovery agent N.A. Investigative [32]
PH-709829 DM5GY6Z Discovery agent N.A. Investigative [33]
QUIPAZINE DMPY6IG Discovery agent N.A. Investigative [34]
SEROTONIN DMOFCRY Discovery agent N.A. Investigative [20]
TMB-8 DMCN2B8 Discovery agent N.A. Investigative [35]
trichloroethanol DMNALMF Discovery agent N.A. Investigative [36]
[3H](S)-zacopride DM0B54M Discovery agent N.A. Investigative [37]
[3H]GR65630 DMMHSYA Discovery agent N.A. Investigative [38]
[3H]granisetron DMB9VGW Discovery agent N.A. Investigative [39]
[3H]ramosetron DM21B46 Discovery agent N.A. Investigative [40]
------------------------------------------------------------------------------------
⏷ Show the Full List of 35 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844.
2 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
3 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
4 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
5 Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70.
6 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
7 Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
8 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
9 Effect of serotonin (5-HT)3-receptor antagonists YM060, YM114 (KAE-393), ondansetron and granisetron on 5-HT4 receptors and gastric emptying in rodents. Jpn J Pharmacol. 1995 Nov;69(3):205-14.
10 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
11 Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
12 Pharmacological and regional characterization of [3H]LY278584 binding sites in human brain. J Neurochem. 1993 Feb;60(2):730-7.
13 Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. J Med Chem. 2009 Jun 11;52(11):3548-62.
14 Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors. Neuropharmacology. 2001 Aug;41(2):282-4.
15 Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and... J Med Chem. 2010 Jun 10;53(11):4379-89.
16 Allosteric interactions among agonists and antagonists at 5-hydroxytryptamine3 receptors. J Neurochem. 1995 Jul;65(1):104-10.
17 Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors. Eur J Med Chem. 2009 Jun;44(6):2667-72.
18 Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. J Med Chem. 1990 Jan;33(1):13-6.
19 Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. J Med Chem. 1994 Apr 29;37(9):1320-5.
20 Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
21 Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro. Eur J Pharmacol. 2000 Dec 8;409(2):195-201.
22 Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors. Bioorg Med Chem. 2009 Oct 1;17(19):6872-8.
23 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
24 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
25 Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor ag... J Med Chem. 2010 Feb 11;53(3):1222-37.
26 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
27 The 5-HT3B subunit confers spontaneous channel opening and altered ligand properties of the 5-HT3 receptor. J Biol Chem. 2008 Mar 14;283(11):6826-31.
28 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
29 Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor. Mol Pharmacol. 2011 Jul;80(1):183-90.
30 Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.
31 Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
32 Different efficacy of specific agonists at 5-HT3 receptor splice variants: the role of the extra six amino acid segment. Br J Pharmacol. 1998 Feb;123(4):661-6.
33 Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor:... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5.
34 Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
35 Characterization of interaction of 3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester with Torpedo californica nicotinic acetylcholine receptor and 5-hydroxytryptamine3 receptor. J Pharmacol Exp Ther. 1999 Jul;290(1):129-35.
36 Arginine 246 of the pretransmembrane domain 1 region alters 2,2,2-trichloroethanol action in the 5-hydroxytryptamine3A receptor. J Pharmacol Exp Ther. 2008 Mar;324(3):1011-8.
37 Autoradiographic distribution of [3H]-(S)-zacopride-labelled 5-HT3 receptors in human brain. J Neurol Sci. 1996 Dec;144(1-2):119-27.
38 Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome. J Pharmacol Sci. 2007 Jul;104(3):263-73.
39 Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells. Br J Pharmacol. 1996 Jul;118(5):1237-45.
40 Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species. Mol Pharmacol. 1995 Sep;48(3):407-16.