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[γ-氨基丁酸(GABA)受体激动剂对大鼠中枢和外周苯二氮䓬结合位点的统一调节]

[Uniform regulation of central and peripheral benzodiazepine binding sites by GABA receptor agonists in rats].

作者信息

Riago L K, Kiĭvet R K, Allikmets L Kh

出版信息

Biull Eksp Biol Med. 1987 Dec;104(12):685-7.

PMID:2825839
Abstract

Central and peripheral benzodiazepine binding sites were studied in vitro after the administration of GABAA and GABAB agonists. Cerebral cortex and kidney homogenates were used in this study. Muscimol (1.5 mg/kg, intraperitoneally) pretreatment significantly increased the affinity of benzodiazepine binding sites not only in the cerebral cortex but also in the kidneys. Similar changes were obtained with (-) and (+) baclofen (5 mg/kg, intraperitoneally), with the only exception that (-) baclofen in addition to changes in the affinity caused a marked decrease in the number of binding sites in both structures studied. The mechanism of action of GABA agonists on peripheral benzodiazepine binding sites is discussed.

摘要

在给予GABAA和GABAB激动剂后,对中枢和外周苯二氮䓬结合位点进行了体外研究。本研究使用了大脑皮质和肾脏匀浆。预先腹腔注射蝇蕈醇(1.5mg/kg)不仅显著增加了大脑皮质中苯二氮䓬结合位点的亲和力,也增加了肾脏中该位点的亲和力。给予(-)和(+)巴氯芬(5mg/kg,腹腔注射)后也获得了类似的变化,唯一的例外是(-)巴氯芬除了引起亲和力变化外,还导致所研究的两种组织中的结合位点数量显著减少。文中讨论了GABA激动剂对外周苯二氮䓬结合位点的作用机制。

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