Differential modulation of etazolate or pentobarbital enhanced [3H] muscimol binding by benzodiazepine agonists and inverse agonists.
Flunitrazepam, a benzodiazepine agonist increases, and DMCM, an inverse agonist decreases the stimulation by etazolate or pentobarbital of [3H] muscimol binding to membranes of rat cerebral cortex. Ro 15-1788 has no marked effects but antagonizes the action of both flunitrazepam and DMCM. The investigation of several drugs acting on benzodiazepine receptors on etazolate enhancement of [3H] muscimol binding suggests that their receptor interaction reflects a spectrum from agonists to inverse agonists.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001569:Benzodiazepines / Q000037:antagonists & inhibitors; D001570:Benzodiazepinones / Q000494:pharmacology; D001667:Binding, Competitive; D002243:Carbolines / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism*; D003292:Convulsants / Q000494:pharmacology; D004974:Etazolate / Q000494:pharmacology*; D005442:Flumazenil; D005445:Flunitrazepam / Q000494:pharmacology; D007700:Kinetics; D009118:Muscimol / Q000378:metabolism*; D009539:Nicotinic Acids / Q000494:pharmacology*; D010080:Oxazoles / Q000378:metabolism*; D010424:Pentobarbital / Q000494:pharmacology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D011963:Receptors, GABA-A
D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D002243:Carbolines; D003292:Convulsants; D009539:Nicotinic Acids; D010080:Oxazoles; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D001569:Benzodiazepines; C034818:methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate; D009118:Muscimol; D005442:Flumazenil; D005445:Flunitrazepam; D010424:Pentobarbital; D004974:Etazolate