Target Validation Information
Target ID T58940
Target Name 5-hydroxy-tryptamine 3B receptor
Target Type
Discontinued
Drug Potency against Target 6-(4-Methyl-piperazin-1-yl)-phenanthridine Drug Info Ki = 1.9 nM [525484]
(R)-zacopride Drug Info Ki = 0.7 nM
QUIPAZINE Drug Info Ki = 1.8 nM [525484]
2-(4-Benzyl-piperazin-1-yl)-benzothiazole Drug Info IC50 = 3300 nM [533917]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole Drug Info Ki = 0.99 nM [532034]
SEROTONIN Drug Info Ki = 120 nM [525484]
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-ol Drug Info Ki = 1217 nM [532034]
2-(4-Methyl-piperazin-1-yl)-quinoline Drug Info Ki = 3 nM [525484]
MESULERGINE Drug Info IC50 = 2.13 nM [534503]
Cilansetron Drug Info Ki = 0.5 nM [552874]
BRL-24682 Drug Info Ki = 41.8 nM [526544]
Action against Disease Model Cilansetron The effects of corticotropin releasing factor (CRF) and serotonin (5-HT)3 receptor antagonists on intestinal water transport were evaluated by a CRF-induced abnormal water transport model in rat colon. Centrally administered CRF (3-30 ug/kg) markedly decreased colonic fluid loss, whereas oral administration of ramosetron (3, 30 ug/kg), alosetron (300 ug/kg), cilansetron (300ug/kg), or loperamide (3 mg/kg) significantly inhibited it. Ramosetron (1-10 ug/kg), alosetron (10-100 ug/kg), cilansetron (10-100 ug/kg), or loperamide (0.3-3 mg/kg) also showed dose-dependent inhibition of CRF-induced defecation in rats. These results suggest that 5-HT3 receptors are involved in both abnormal colonic water transport and defecation induced by CRF, and that the inhibitory effectsof 5-HT3 receptor antagonists on CRF-induced abnormal defecation partly result from their ameliorating action on colonic water transport. [552814] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations 5-HT3 receptor over-expressing mice drank less alcohol than non-transgenic mice in a two-bottle free choice test. Over-expression of the 5-HT3 receptor in these mice resulted ina decrease in ethanol cons uMption. These mice should prove useful in testing hypothesis regarding a common reward pathway for drugs of abuse and the role 5-HT3 receptors play in this pathway. [552814]
References
Ref 552814Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats. Eur J Pharmacol. 2008 Jun 10;587(1-3):281-4. doi: 10.1016/j.ejphar.2008.03.040. Epub 2008 Mar 30.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 533917J Med Chem. 1994 Apr 29;37(9):1320-5.Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
Ref 532034J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 532034J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Ref 525484J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Ref 534503J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
Ref 552874IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels. Nucleic Acids Res. 2009 Jan;37(Database issue):D680-5. doi: 10.1093/nar/gkn728. Epub 2008 Oct 23.
Ref 526544J Med Chem. 2003 Feb 27;46(5):702-15.Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.