Interaction of anticonvulsants with the barbiturate-benzodiazepine-GABA receptor complex.
Unlike the anesthetic barbiturate pentobarbital and the anxiolytic pyrazolopyridine etazolate, which enhance [3H]diazepam binding to rat brain membranes, the anticonvulsant barbiturates phenobarbital and metharbital, and also chlormethiazole, at therapeutic concentrations (10-1000 muM), do not stimulate [3H]diazepam binding, but instead block the enhancement by both pentobarbital and etazolate. The same anticonvulsants at similar concentrations inhibit [3H]alpha-dihydropicrotoxinin (DHP) binding suggesting that these anticonvulsants compete for the same receptor sites as pentobarbital and etazolate, designated the barbiturate-picrotoxinin receptor component of the benzodiazepine-GABA receptor complex.
D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism*; D001463:Barbiturates / Q000494:pharmacology; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D010852:Picrotoxin / Q000031:analogs & derivatives / Q000378:metabolism; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism*; D011955:Receptors, Drug / Q000187:drug effects / Q000378:metabolism*; D011963:Receptors, GABA-A
D000927:Anticonvulsants; D001463:Barbiturates; D010852:Picrotoxin; D011956:Receptors, Cell Surface; D011955:Receptors, Drug; D011963:Receptors, GABA-A; C030975:barbiturate receptor; C017230:dihydropicrotoxinin