Inactivation of Benzodiazepine Binding Sites by N‐Ethylmaleimide

Abstract
The benzodiazepine receptors of bovine brain membranes were identified by the specific binding of radiolabeled [3H]diazepam [an antianxiety agent]. Pretreatment of membranes with N-ethylmaleimide causes a dose- and time-dependent decrease of 45-60% in the number of binding sites. No decrease occurs when membranes are pretreated with N-ethylmaleimide before administration or in the presence of diazepam. [3H]Diazepam binding to the remaining sites occurs with the same characteristics as binding to the untreated receptor population.