Devazepide

Devazepide is a nonpeptide antagonist of the cholecystokinin 1 (CCK1) receptor (Ki = 0.3 nM). It is selective for CCK1 over the CCK2 receptor (Ki = 342 nM). Devazepide inhibits CCK-8-induced amylase release in isolated dispersed rat pancreatic acini (IC50 = 25.4 nM). It reduces CCK-8-induced decreases in gastric emptying and food intake in rats (ED50s = 140 and 321 µg/kg, respectively), as well as CCK-8-induced contractions of colon and gall bladder in rabbits and cats, respectively (ED50s = 34 and 210 µg/kg, respectively). Devazepide (1 mg/kg) enhances morphine-induced increases in tail-flick latency and prevents the development of morphine tolerance, but does not affect morphine dependence, in rats. It also induces apoptosis and cell cycle arrest at the G1/G0 phase in, and inhibits the migration of, 5637 bladder cancer cells when used at a concentration of 25 µM.Formal Name: N-[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide. CAS Number: 103420-77-5. Synonyms: L-364,718, MK-329, ZINC01847292. Molecular Formula: C25H20N4O2. Formula Weight: 408.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 223, 296 nm. SMILES: O=C(C1=CC2=CC=CC=C2N1)N[C@H]3N=C(C4=CC=CC=C4)C5=CC=CC=C5N(C3=O)C. InChi Code: InChI=1S/C25H20N4O2/c1-29-21-14-8-6-12-18(21)22(16-9-3-2-4-10-16)27-23(25(29)31)28-24(30)20-15-17-11-5-7-13-19(17)26-20/h2-15,23,26H,1H3,(H,28,30)/t23-/m1/s1. InChi Key: NFHRQQKPEBFUJK-HSZRJFAPSA-N.