Inhibition of [3H]Diazepam and [3H]3‐Carboethoxy‐β‐Carboline Binding by Irazepine: Evidence for Multiple “Domains” of the Benzodiazepine Receptor
- 4 October 1982
- journal article
- research article
- Published by Wiley in Journal of Neurochemistry
- Vol. 39 (4) , 1142-1146
- https://doi.org/10.1111/j.1471-4159.1982.tb11507.x
Abstract
The binding of [3H]diazepam and [3H]3-carboethoxy-β-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 (max of [3H]3-carboethoxy-β-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.Keywords
This publication has 26 references indexed in Scilit:
- Comparison of the effects of GABA and chloride ion on the affinities of ligands for the benzodiazepine receptorLife Sciences, 1982
- Agonist and antagonist benzodiazepine receptor interaction in vitroNature, 1981
- Binding of [3H]ethyl‐β‐carboline‐3‐carboxylate to brain benzodiazepine receptorsFEBS Letters, 1981
- [3H]ethyl β-carboline-3-carboxylate binding to the benzodiazepine receptors is not affected by GABAEuropean Journal of Pharmacology, 1981
- Ethyl β-carboline carboxylate lowers seizure threshold and antagonizes flurazepam-induced sedation in ratsNature, 1981
- Heterogeneity of Benzodiazepine Receptors in the Central Nervous System Demonstrated with Kenazepine, an Alkylating BenzodiazepineJournal of Neurochemistry, 1980
- Irazepine, a noncompetitive, irreversible inhibitor of 3H-diazepam binding to benzodiazepine receptorsNature, 1979
- Enhancement of the binding of 3H-diazepam to rat brain membranes by SQ 20009, a novel anxiolytic, γ-aminobutyric acid (GABA) and muscimolLife Sciences, 1979
- Is the benzodiazepine receptor coupled to a chloride anion channel?Nature, 1979
- GABAergic modulation of benzodiazepine binding site sensitivityNature, 1978