Effect of picrotoxinin on benzodiazepine receptor binding.
The effect of picrotoxinin on [3H]flunitrazepam binding to benzodiazepine receptors was investigated. In mouse forebrain membranes, picrotoxinin inhibited basal, GABA- and pentobarbital-stimulated [3H]flunitrazepam binding; this inhibitory activity was temperature- and chloride ion-dependent. Scatchard analysis of the data indicates that picrotoxinin decreases the number of binding sites without altering binding affinity. In cerebellar membranes, picrotoxinin did not alter [3H]flunitrazepam receptor binding.
D000818:Animals; D001921:Brain / Q000378:metabolism; D002531:Cerebellum / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D051379:Mice; D010424:Pentobarbital / Q000494:pharmacology; D010852:Picrotoxin / Q000031:analogs & derivatives* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D054830:Sesterterpenes; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D005445:Flunitrazepam; D010424:Pentobarbital; D010852:Picrotoxin; D011963:Receptors, GABA-A; D054830:Sesterterpenes; D005680:gamma-Aminobutyric Acid; C022961:picrotoxinin