产品描述:
SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).