Therapeutic Targets Database
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Target Validation Information
TTD IDTTDC00009
Target Name5-hydroxy-tryptamine 3B receptor    
Type of TargetClinical trial target    
Drug Potency against TargetCilansetronKi = 0.5 nM[1]
MESULERGINEIC50 = 2.13 nM[2]
2-(4-Benzyl-piperazin-1-yl)-benzothiazoleIC50 = 3300 nM[3]
ZACOPRIDEKi = 0.7 nM[4]
2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazoleKi = 0.99 nM[5]
SC-52491Ki = 1.2 nM[6]
QUIPAZINEKi = 1.8 nM[7]
6-(4-Methyl-piperazin-1-yl)-phenanthridineKi = 1.9 nM[7]
SEROTONINKi = 120 nM[7]
3-(2-Amino-ethyl)-2-methyl-1H-indol-5-olKi = 1217 nM[5]
SDZ-205557Ki = 205 nM[4]
2-(4-Methyl-piperazin-1-yl)-quinolineKi = 3 nM[7]
BRL-24682Ki = 41.8 nM[8]
PHA-543613Ki = 511 nM[9]
ML-10302Ki = 782 nM[4]
Action against Disease ModelCilansetronThe 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 (300 ug/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 effects of 5-HT3 receptor antagonists on CRF-induced abnormal defecation partly result from their ameliorating action on colonic water transport.[10]
The Effect of Target Knockout, Knockdown or Genetic Variations5-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 in a 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.[11]
Ref 1Nucleic Acids Res. 2009 Jan;37(Database issue):D680-5. Epub 2008 Oct 23.IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels. To Reference
Ref 2J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. To Reference
Ref 3J 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. To Reference
Ref 4Bioorg. Med. Chem. Lett. 4(12):1433-1436 (1994) To Reference
Ref 5J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. To Reference
Ref 6J Med Chem. 2006 Feb 9;49(3):1125-39.Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. To Reference
Ref 7J 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. To Reference
Ref 8J 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. To Reference
Ref 9J Med Chem. 2006 Jul 13;49(14):4425-36.Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. To Reference
Ref 10Eur J Pharmacol. 2008 Jun 10;587(1-3):281-4. Epub 2008 Mar 30.Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats. To Reference
Ref 11Psychopharmacology (Berl). 1998 Nov;140(2):243-8.5-HT3 receptor over-expression decreases ethanol self administration in transgenic mice. To Reference



 

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