ABSTRACT
The mechanism of action of diazepam and related benzodiazepine (BZ) anxiolytics seems to involve central BZ binding sites (Hommer et al., 1987). In animals, diazepam serves as a discriminative stimulus and the diazepam–stimulus generalizes to other BZs in a dose–dependant and stereoselective manner; the diazepam–stimulus can also be antagonized by the BZ antagonist flumazepil (Ro 15,1788). There exists, for a fairly large series of BZ derivatives, a significant correlation between their ED50 values for stimulus generalization in diazepam–trained animals and both their affinities for BZ binding sites and their human anxiolytic potencies (for a review see Young & Glennon, 1988).
