CCKB selective receptor ligands: novel 1,3,5-trisubstituted benzazepin-2-ones

The novel 3-ureidobenzazepin-2-ones 11 and 12, which incorporate a cationic substituent at the 5-position were designed and synthesised as ligands for the CCKB receptor. These compounds proved to have high affinity for the CCKB receptor and were selective over the CCKA receptor subtype. This work further defines the role of the benzazepine template as a bioisostere for the 1,4-benzodiazepine template of earlier CCK antagonists.