The synthesis of two ''dipeptoids'' structurally related to the CCK-B antagonist CI-988 (PD134308)(1-2) is described. The 2-and 1-indolyl derivatives 4a,b were prepared in order to define the role of the tryptophan moiety in this series of ''dipeptoids''. They were evaluated as competitors in the binding of [H-3]-CCK8s on guinea pig brain CCK-B receptors.
Synthesis and receptor binding affinity of cholecystokinin receptor ligands: 2- and 1-indolyl derivatives of PD134308
NATALINI, Benedetto;PELLICCIARI, Roberto;
1996
Abstract
The synthesis of two ''dipeptoids'' structurally related to the CCK-B antagonist CI-988 (PD134308)(1-2) is described. The 2-and 1-indolyl derivatives 4a,b were prepared in order to define the role of the tryptophan moiety in this series of ''dipeptoids''. They were evaluated as competitors in the binding of [H-3]-CCK8s on guinea pig brain CCK-B receptors.File in questo prodotto:
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