Catalog No.: PC-22021Not For Human Use, Lab Use Only.
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of peripheral cholecystokinin (CCK) receptor with IC50 of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors.
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of peripheral cholecystokinin (CCK) receptor with IC50 of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors. Devazepide is a competitive CCK antagonist, which lacks agonist activity. Devazepide exhibits a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays. Devazepide (0.1 mg/kg) markedly antagonized the contractions of the guinea pig gallbladder produced by intravenous administration of CCK for at least 2 hr. Devazepide (ED50, 0.04 mg/kg, oral) is highly effective as an antagonist of CCK-induced inhibition of gastric emptying in mice.
