Design of novel cholecystokinin-B receptor ligands based on the 'double-ring system' approach.

Abstract A structurally novel series of cholecystokinin-B (CCK-B) receptor ligands has been designed and synthesized based on the ‘double-ring system’ theory of receptor recognition. Compounds 2b- cis and 2g- cis from this 1-amino-2-benzyltetralin series show modest CCK-B receptor affinity, with IC 50 values of 48.5 nM and 39.0 nM, respectively. The results are discussed in the context of ongoing efforts to identify the CCK-B receptor binding site for nonpeptide ligands.