Solubilization of convulsant/barbiturate binding activity on the gamma-aminobutyric acid/benzodiazepine receptor complex.
Binding activity of the radioactive cage convulsant [35S]t-butylbicyclophosphorothionate was solubilized from rat brain membranes using the zwitterionic detergent 3-[(3-cholamidopropyl)-dimethylammonio] propanesulfonate. Binding (KD = 26 nM, Bmax = 0.4 pmol/mg protein) was inhibited by picrotoxin and related convulsants and by barbiturates and related depressants that interact with gamma-aminobutyric acid and benzodiazepine receptors via the picrotoxinin binding site. The convulsant/barbiturate binding activity chromatographed on gel filtration as a single peak coinciding with the benzodiazepine/gamma-aminobutyric acid receptor protein complex.
D000818:Animals; D001463:Barbiturates / Q000378:metabolism*; D001569:Benzodiazepines / Q000378:metabolism*; D001667:Binding, Competitive; D001643:Bridged Bicyclo Compounds / Q000378:metabolism*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism*; D003292:Convulsants / Q000378:metabolism*; D007425:Intracellular Membranes / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000302:isolation & purification / Q000378:metabolism*; D011963:Receptors, GABA-A; D017981:Receptors, Neurotransmitter / Q000302:isolation & purification / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D001463:Barbiturates; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D001952:Bridged-Ring Compounds; D003292:Convulsants; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D017981:Receptors, Neurotransmitter; C030975:barbiturate receptor; D001569:Benzodiazepines; D005680:gamma-Aminobutyric Acid; C037476:tert-butylbicyclophosphorothionate