G. Araldi et al., SYNTHESIS AND RECEPTOR-BINDING AFFINITY OF CHOLECYSTOKININ RECEPTOR LIGANDS - 2-INDOLYL AND 1-INDOLYL DERIVATIVES OF PD134308, Il Farmaco, 51(7), 1996, pp. 471-476
The synthesis of two ''dipeptoids'' structurally related to the CCK-B
antagonist CI-988 (PD134308)(1-2) is described. The 2-and 1-indolyl de
rivatives 4a,b were prepared in order to define the role of the trypto
phan moiety in this series of ''dipeptoids''. They were evaluated as c
ompetitors in the binding of [H-3]-CCK8s on guinea pig brain CCK-B rec
eptors.