SYNTHESIS AND RECEPTOR-BINDING AFFINITY OF DIPEPTOID CHOLECYSTOKININ LIGANDS

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