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Solubilization of convulsant/barbiturate binding activity on the gamma-aminobutyric acid/benzodiazepine receptor complex.

作者信息

King R G, Olsen R W

出版信息

Biochem Biophys Res Commun. 1984 Mar 15;119(2):530-6. doi: 10.1016/s0006-291x(84)80280-6.

DOI:10.1016/s0006-291x(84)80280-6
PMID:6324766
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.

摘要

相似文献

1
Solubilization of convulsant/barbiturate binding activity on the gamma-aminobutyric acid/benzodiazepine receptor complex.
Biochem Biophys Res Commun. 1984 Mar 15;119(2):530-6. doi: 10.1016/s0006-291x(84)80280-6.
2
Convulsant/barbiturate activity on the soluble gamma-aminobutyric acid-benzodiazepine receptor complex.惊厥剂/巴比妥类药物对可溶性γ-氨基丁酸-苯二氮䓬受体复合物的作用。
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Binding characteristics and interactions of depressant drugs with [35S]t-butylbicyclophosphorothionate, a ligand that binds to the picrotoxinin site.
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Barbiturate recognition site on the GABA/benzodiazepine receptor complex is distinct from the picrotoxinin/TBPS recognition site.
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CNS depressants accelerate the dissociation of 35S-TBPS binding and GABA enhances their displacing potencies.中枢神经系统抑制剂加速35S - TBPS结合的解离，而γ-氨基丁酸（GABA）增强它们的置换效力。
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Anxiolytic cyclopyrrolone drugs allosterically modulate the binding of [35S]t-butylbicyclophosphorothionate to the benzodiazepine/gamma-aminobutyric acid-A receptor/chloride anionophore complex.抗焦虑环吡咯酮类药物可别构调节[35S]叔丁基双环磷硫代酸盐与苯二氮䓬/γ-氨基丁酸-A受体/氯化物阴离子载体复合物的结合。
Mol Pharmacol. 1984 Nov;26(3):470-6.

引用本文的文献

1
Understanding the GABAA receptor: a chemically gated ion channel.了解γ-氨基丁酸A型受体：一种化学门控离子通道。
Biochem J. 1988 Jan 1;249(1):21-32. doi: 10.1042/bj2490021.