荷包牡丹碱对巴氯芬抑制大鼠大脑皮层切片电诱发的[3H]GABA释放的反常拮抗作用。

Paradoxical antagonism by bicuculline of the inhibition by baclofen of the electrically evoked release of [3H]GABA from rat cerebral cortex slices.

作者信息

Maurin Y

机构信息

Department of Biology, Laboratoire d'Etudes et de Recherches Synthélabo, Paris, France.

出版信息

Eur J Pharmacol. 1988 Oct 18;155(3):219-27. doi: 10.1016/0014-2999(88)90507-9.

DOI:10.1016/0014-2999(88)90507-9

PMID:2853062

Abstract

The presynaptic regulation of the electrically evoked release of [3H]GABA was studied in the rat cerebral cortex. Among the GABA receptor agonists tested (GABA, SL 75102, muscimol, THIP, isoguvacine, (+/-)-baclofen), only (+/-)-baclofen inhibited the stimulation-evoked release of [3H]GABA. This effect of baclofen was stereoselective in favor of the (-) enantiomer. The inhibition by (+/-)-baclofen of the electrically evoked release of [3H]GABA was antagonized by bicuculline and picrotoxin. Our results suggest that the release of [3H]GABA in vitro can be modulated by a receptor-mediated mechanism which is sensitive to baclofen, bicuculline and picrotoxin but not to GABA, muscimol or THIP.

摘要

在大鼠大脑皮层中研究了电诱发的[3H]GABA释放的突触前调节。在所测试的GABA受体激动剂（GABA、SL 75102、蝇蕈醇、THIP、异谷氨酰胺、（±）-巴氯芬）中，只有（±）-巴氯芬抑制电刺激诱发的[3H]GABA释放。巴氯芬的这种作用具有立体选择性，有利于（-）对映体。（±）-巴氯芬对电诱发的[3H]GABA释放的抑制作用被荷包牡丹碱和苦味毒拮抗。我们的结果表明，体外[3H]GABA的释放可通过一种受体介导的机制进行调节，该机制对巴氯芬、荷包牡丹碱和苦味毒敏感，但对GABA、蝇蕈醇或THIP不敏感。