Original Article

Benzodiazepine derivatives: relationship between anti-convulsant activity and affinity to rabbit frontal cortical receptors

Guang-mei YAN, Ben-rong HU


The correlation between benzodiazepine receptor affinity of 15 benzodiazepine derivatives an d their anti-conculsant activity was studied by reversible radioactive ligand binding and photoaffinity labeling methods. The binding characteristics of benzodiazepine receptor exhibited apparent heterogenecity with two dissociation constants (KD), ie, 0.276 and 5.960 nmol/L, respectively. They showed a good parallel between binding to receptor and anti-convulsant potency of benzodiazepine derivatives (r=0.958 for reversible binding and r=0.960 for photoaffinity labeling). The analysis of structure-activity relationship suggested that the affinity to BZ receptor of benzodiazepine derivatives and their pharmacological effects seemed to be dependent on the replacement of H atom by electrophilic groups at C7 in ring A, C2, in ring C and lactam structure of ring B. The BZ receptor seemed to have three positive electronic sites at least for binding to benzodiazepines.

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