3-[2-(N-PHENYLACETAMIDE)]-1,5-BENZODIAZEPINES - ORALLY-ACTIVE, BINDING SELECTIVE CCK-A AGONISTS

A series of modifications were made to the C-3 substituent of the 1,5- benzodiazepine CCK-A agonist 1. Replacement of the inner urea NH and a ddition of a methyl group to generate a C-3 quaternary carbon resulted in acetamide 6, which showed CCK-A receptor binding selectivity and s ub-micromolar agonist activity in vitro. Benzodiazepine 6 was active i n an in. vivo mouse gallbladder emptying assay and represents a novel orally active, binding selective CCK-A agonist.