Synthesis and receptor-binding affinity of dipeptoid cholecystokinin ligands

Article abstract of DOI:10.1016/0223-5234(96)89137-9

This paper describes the synthesis of novel derivatives 4a-i, which are structurally related to PD134308 and in which the indole moiety is replaced by other aromatic groups. Cholecystokinin-A and -B (CCK-A and CCK-B) receptor binding affinities of these analogues are described and the contribution of the various rings is discussed. Several of the compounds prepared have CCK-B receptor binding values similar to that reported for PD134308 and are highly selective over the CCK-A receptor. They represent potential therapeutic agents for anxiety.