A QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF LIGANDS EXHIBITING AGONIST AND ANTAGONIST ACTIONS WITH CHOLECYSTOKININ-RECEPTORS

Observed biological activities of substituted phenyl urea/thiourea tet rapeptides as agonists with the cholecystokinin-alimentary canal (CCK- A) receptor, and (R)-4-benzamido-5-oxopentanoic acid derivatives with both peripheral (CCK-A) and the central (CCK-B) (brain) receptors have been shown to be correlated with various physicochemical, e.g. pi, si gma, and structural, e.g. V(w) and dummy, I, parameters. These results were, then interpreted to predict promising criteria for having ligan ds with better affinity with the CCK receptors.