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 552814 | Effects 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 525484 | J 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 525484 | J 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 533917 | J 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 532034 | J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. | ||||
Ref 525484 | J 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 532034 | J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. | ||||
Ref 525484 | J 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 534503 | J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. | ||||
Ref 552874 | IUPHAR-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 526544 | J 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. |
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