Mosapride (citrate)

Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Ki = 69.9 nM). It is selective for 5-HT4 over 5-HT1, 5-HT2, dopamine D2, and alpha1- and alpha2-adrenergic receptors but acts as a partial antagonist at 5-HT3 (Ki = 1,189 nM). It induces relaxation of precontracted rat esophageal thoracic muscularis mucosa preparations and enhances electrically evoked contractions in isolated guinea pig ileum (EC50s = 208.4 and 73.2 nM, respectively). Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs. It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg.Formal Name: 4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]-benzamide, 2-hydroxy-1,2,3-monopropanetricarboxylate. CAS Number: 112885-42-4. Synonyms: AS-4370. Molecular Formula: C21H25ClFN3O3 . C6H8O7. Formula Weight: 614.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 15 mg/ml. lambdamax: 212, 232, 274, 309 nm. SMILES: ClC1=C(N)C=C(OCC)C(C(NCC2OCCN(CC3=CC=C(F)C=C3)C2)=O)=C1.OC(CC(C(O)=O)(O)CC(O)=O)=O. InChi Code: InChI=1S/C21H25ClFN3O3.C6H8O7/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14,7-3(8)1-6(13,5(11)12)2-4(9)10/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27),13H,1-2H2,(H,7,8)(H,9,10)(H,11,12). InChi Key: HUZTYZBFZKRPFG-UHFFFAOYSA-N.