Abstract
The C 3-substituted benzodiazepines derived from asperlicin, e.g. devazepide (L-364,718, MK-329), constitute the most potent class of cholecystokinin A-type (CCK A) receptor antagonists. In order to gain insight into the prerequisites for binding, we examined the conformational properties of both potent and weak representati3es of this class with computer assisted molecular modelling (CAMM) techniques. The CAMM results indicate that the binding site for C 3-substituents is a planar slot on the CCK A receptor surface and, in addition, allow the proposal of a model which describes the relative binding mode of the less potent R isomers versus that of the S isomers. The latter model illustrates the unique spatial properties of the benzodiazepine moiety, which we suggest functions primarily as an invertible core which assures an optimal arrangement of attached substituents.
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