Inhibition of [3H]diazepam and [3H]3-carboethoxy-beta-carboline binding by irazepine: evidence for multiple "domains" of the benzodiazepine receptor.
The binding of [3H]diazepam and [3H]3-carboethoxy-beta-carboline was examined in rat brain synaptosomal membranes treated with irazepine, an alkylating benzodiazepine. Under incubation conditions that resulted in a 25-33% reduction in the Bmax of [3H]diazepam binding, only modest (less than 8.5%) reductions in the Bmax of [3H]3-carboethoxy-beta-carboline were observed. The differential effects of irazepine on the binding of these two compounds may be explained by the presence of multiple areas or "domains" on the benzodiazepine receptor.
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology*; D002243:Carbolines / Q000378:metabolism*; D003975:Diazepam / Q000378:metabolism*; D007211:Indoles / Q000378:metabolism*; D046911:Macromolecular Substances; D008297:Male; D008970:Molecular Weight; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug / Q000187:drug effects*; D011963:Receptors, GABA-A
D001570:Benzodiazepinones; D002243:Carbolines; D007211:Indoles; D046911:Macromolecular Substances; D011955:Receptors, Drug; D011963:Receptors, GABA-A; C019439:irazepine; C024915:beta-carboline-3-carboxylic acid ethyl ester; D003975:Diazepam