Cisapride

Cisapride is an agonist of serotonin (5-HT) receptor subtype 5-HT4 (IC50 = 0.483 µM in COS-7 cells expressing the human receptor). It induces relaxation of precontracted isolated rat esophageal thoracic muscularis mucosae preparations (EC50 = 102.33 nM). Cisapride (0.5 mg/kg) increases the rate of gastric emptying in rats. It is also a human ether-a-go-go related gene (hERG) channel blocker that binds to hERG channels with an IC50 value of less than 1 µM in a fluorescence polarization assay. Formulations containing cisapride have previously been used in the treatment of nocturnal heartburn associated with gastroesophageal reflux disease.Formal Name: rel-4-amino-5-chloro-N-[1-[(3R,4S)-3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxy-benzamide. CAS Number: 81098-60-4. Molecular Formula: C23H29ClFN3O4. Formula Weight: 466.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml, Ethanol: slightly soluble. lambdamax: 214, 276, 308 nm. SMILES: NC1=CC(OC)=C(C(N[C@@H]2CCN(CCCOC3=CC=C(F)C=C3)C[C@@H]2OC)=O)C=C1Cl. InChi Code: InChI=1S/C23H29ClFN3O4/c1-30-21-13-19(26)18(24)12-17(21)23(29)27-20-8-10-28(14-22(20)31-2)9-3-11-32-16-6-4-15(25)5-7-16/h4-7,12-13,20,22H,3,8-11,14,26H2,1-2H3,(H,27,29)/t20-,22+/m1/s1. InChi Key: DCSUBABJRXZOMT-IRLDBZIGSA-N.