Inhibition of [3H]Diazepam and [3H]3-Carboethoxy-β-Carboline Binding by Irazepine: Evidence for Multiple "Domains" of the Benzodiazepine Receptor |
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| Authors: | Phil Skolnick Margaret Schweri Eberhard Kutter Evan Williams Steven Paul |
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| Affiliation: | Laboratory of Bioorgarzic Chemistry, NIADDK, National Institutes of Health, Bethesda, Maryland, U.S.A.;Neuroscience Branch, NIMH, National Institutes of Health, Bethesda, Maryland, U.S.A. |
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| Abstract: | 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. |
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| Keywords: | Diazepam 3-Carboethoxy β-carboline Irazepine Domain Benzodiazepine receptor |
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