Solubilization of convulsant/barbiturate binding activity on the gamma-aminobutyric acid/benzodiazepine receptor complex |
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Authors: | R G King R W Olsen |
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Institution: | 1. Department of Biochemistry and Division of Biomedical Sciences, University of California, Riverside, CA 92521, USA;2. Department of Pharmacology, School of Medicine, and Brain Research Institute, University of California, Los Angeles, CA 90024, USA |
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Abstract: | 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. |
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