For research use only. Not for therapeutic Use.
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders[1].
Devazepide (oral gavage; 4 mg/kg; twice per day) significantly accelerates cholesterol crystallization and crystal growth to microlithiasis, and the formation of gallstones in mice[2].Devazepide (intraperitoneal injection; 0.1-1 mg/kg) has opposite effects on spontaneous locomotor activity, and on caerulein- and apomorphine-induced hypomotility in the mouse[3].
| Catalog Number | M011517 |
| CAS Number | 103420-77-5 |
| Synonyms | N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide |
| Molecular Formula | C25H20N4O2 |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | NFHRQQKPEBFUJK-HSZRJFAPSA-N |
| SMILES | CN1C2=CC=CC=C2C(=NC(C1=O)NC(=O)C3=CC4=CC=CC=C4N3)C5=CC=CC=C5 |
| Reference | [1]. Chang RS, et al. Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6. [2]. Helen H Wang, et al. The cholecystokinin-1 receptor antagonist devazepide increases cholesterol cholelithogenesis in mice. Eur J Clin Invest [3]. E Vasar, et al. Differential involvement of CCK-A and CCK-B receptors in the regulation of locomotor activity in the mouse. Psychopharmacology (Berl). 1991;105(3):393-9 |
