BENZODIAZEPINE ANALOGS .12. AN INVESTIGATION OF SUBSTITUENT AND RING-ATOM EFFECTS ON RECEPTOR-BINDING AFFINITIES

The pharmacological activity of benzodiazepine derivatives is well est ablished and a number of these compounds are in clinical use. In the c ourse of our own research we have previously discussed the synthesis a nd spectrometric analysis of various benzodiazepine analogues. In the present study, we have examined the receptor binding affinities of sel ected benzoxazepinones, benzodiazepinones and benzothiazepinones on br ain benzodiazepine receptors in order to probe their medicinal potenti al, Many of the compounds tested are capable of binding specifically t o the benzodiazepine receptor. The question as to whether or not such compounds are likely to elicit an agonistic or antagonistic response, however, must be addressed by means of in vivo studies.