Inactivation of benzodiazepine binding sites by N-ethylmaleimide.
The benzodiazepine receptors of bovine brain membranes have been identified by the specific binding of radiolabeled [3H]diazepam. Pretreatment of membranes with N-ethylmaleimide causes a dose- and time-dependent decrease of 45 to 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. Binding of [3H]diazepam to the remaining sites occurs with the same characteristics as binding to the untreated receptor population.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism / Q000494:pharmacology; D005033:Ethylmaleimide / Q000494:pharmacology*; D007700:Kinetics; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism*; D011963:Receptors, GABA-A; D017981:Receptors, Neurotransmitter / Q000378:metabolism*
D011955:Receptors, Drug; D011963:Receptors, GABA-A; D017981:Receptors, Neurotransmitter; D005033:Ethylmaleimide; D003975:Diazepam