Target Validation Information
TTD ID	T58940
Target Name	5-HT 3B receptor (HTR3B)
Type of Target	Discontinued
Drug Potency against Target	Cilansetron	Drug Info	Ki = 0.5 nM	[7]
		Drug Info	Ki = 1217 nM	[3]
	(R)-zacopride	Drug Info	Ki = 0.7 nM
	2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole	Drug Info	Ki = 0.99 nM	[3]
	2-(4-Benzyl-piperazin-1-yl)-benzothiazole	Drug Info	IC50 = 3300 nM	[4]
	2-(4-Methyl-piperazin-1-yl)-quinoline	Drug Info	Ki = 3 nM	[1]
	6-(4-Methyl-piperazin-1-yl)-phenanthridine	Drug Info	Ki = 1.9 nM	[1]
	BRL-24682	Drug Info	Ki = 41.8 nM	[2]
	MESULERGINE	Drug Info	IC50 = 2.13 nM	[5]
	QUIPAZINE	Drug Info	Ki = 1.8 nM	[1]
	SEROTONIN	Drug Info	Ki = 120 nM	[1]
Action against Disease Model	Cilansetron	Drug Info	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.	[6]
References
REF 1	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.
REF 2	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.
REF 3	Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. J Med Chem. 1990 Jan;33(1):13-6.
REF 4	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.
REF 5	Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
REF 6	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.
REF 7	IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels. Nucleic Acids Res. 2009 Jan;37(Database issue):D680-5.

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