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刺激和阻断M及N胆碱能受体的药物对大鼠大脑皮层γ-氨基丁酸水平及谷氨酸脱羧酶活性的影响

Effects of drugs stimulating and blocking M and N cholinergic receptors on GABA level and GAD activity in rat cerebral cortex.

作者信息

Sieklucka-Dziuba M

出版信息

Acta Physiol Pol. 1982 Sep-Dec;33(5-6):577-86.

PMID:7186760
Abstract

In the experiments carried out on Wistar rats it was demonstrated that pilocarpine was without effect on the GABA level in the cerebral cortex, while physostigmine raised this level. These changes were prevented by atropine. Lobeline and nicotine exerted a biphasic effect on GABA level: in small doses given 15 min before decapitation they decreased, and in higher doses and after longer time intervals they increased this level. This was due to their biphasic action on the cholinergic receptor N. Changes in GABA level produced by stimulation of the N receptor by lobeline and nicotine were prevented by mecamylamine, d-tubocurarine, and in part also by atropine, phentolamine and propranolol. This suggests an indirect participation of alpha and beta receptors in the transmission of impulses from the cholinergic N receptors to the GABA-ergic system. The effect of the tested substances on GAD activity was not uniform. No close correlation was demonstrated between GAD activity and GABA level.

摘要

在对Wistar大鼠进行的实验中,已证明毛果芸香碱对大脑皮层中的GABA水平无影响,而毒扁豆碱则提高了该水平。这些变化可被阿托品阻止。洛贝林和尼古丁对GABA水平产生双相效应:在断头前15分钟给予小剂量时,它们会降低GABA水平,而在给予较高剂量和更长时间间隔后,它们会提高该水平。这是由于它们对胆碱能受体N的双相作用。洛贝林和尼古丁刺激N受体所产生的GABA水平变化可被美加明、d - 筒箭毒碱部分阻止,阿托品、酚妥拉明和普萘洛尔也能部分阻止。这表明α和β受体间接参与了从胆碱能N受体到GABA能系统的冲动传递。受试物质对谷氨酸脱羧酶(GAD)活性的影响并不一致。未证明GAD活性与GABA水平之间存在密切相关性。

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