Dual CCK-A and -B receptor antagonists (I). C9-Methyl-1,4-benzodiazepines

Article abstract of DOI:10.1016/S0960-894X(96)00609-9

A novel series of potent CCK-A and CCK-B dual antagonists has been prepared which incorporate a methyl substituent at the 9 position of a 1,4-benzodiazepine ring system. FR193108 ((+)-11) was selected for further biological evaluation, and is expected to be more efficacious than CCK-A selective antagonists for the treatment of pancreatitis, since it has high and well-balanced affinities for both CCK-A and -B receptors.