Effect of GABA and benzodiazepine antagonists on [3H]flunitrazepam binding to cerebral cortical membrane.
The effects of GABA on the binding of [3H]flunitrazepam to bovine cerebral cortical membranes was investigated in presence and in absence of benzodiazepine antagonists. The percentage stimulation of [3H]flunitrazepam binding by GABA is higher when approximately 50% of the binding is displaced by benzodiazepine antagonists. The observed increase in percent stimulation of [3H]flunitrazepam binding by GABA might reflect the preferential displacement of the ligand by benzodiazepine antagonists from a GABA-insensitive conformational state or site of the receptor.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D001569:Benzodiazepines / Q000037:antagonists & inhibitors*; D001667:Binding, Competitive; D002417:Cattle; D002540:Cerebral Cortex / Q000378:metabolism*; D005445:Flunitrazepam / Q000378:metabolism*; D007700:Kinetics; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology*
D014151:Anti-Anxiety Agents; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D001569:Benzodiazepines; D005680:gamma-Aminobutyric Acid; D005445:Flunitrazepam