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哈尔满的γ-氨基丁酸能效应独立于其对苯二氮䓬受体的影响

[GABA-ergic effects of harman independent of its influence on benzodiazepine receptors].

作者信息

Dolzhenko A T, Komissarov I V

出版信息

Biull Eksp Biol Med. 1984 Oct;98(10):446-8.

PMID:6093910
Abstract

It has been shown in experiments on rat cortex slices preincubated with 3H-GABA that chlorodiazepoxide (10(-6), 3.10(-5) M) does not change basal and electric stimulation-induced release of the label. It has been also shown that it does not eliminate the autoinhibitory effect of GABA on electric stimulation-induced release of 3H-GABA. However, harmane and some other (but not all) derivatives given at the same concentrations increase 3H-GABA release induced by electric stimulation and abolish the inhibitory effect of GABA without changing or slightly raising spontaneous release of 3H-GABA. It is concluded that harmane enhances the electrically stimulated release of the transmitter by GABAergic axons whatever the effect on benzodiazepine-binding areas of GABA receptors.

摘要

在对用3H - GABA预孵育的大鼠皮质切片进行的实验中发现,氯氮卓(10(-6),3×10(-5) M)不会改变基础状态下以及电刺激诱导的放射性标记物释放。还发现它不会消除GABA对电刺激诱导的3H - GABA释放的自身抑制作用。然而,哈尔满和其他一些(但不是全部)相同浓度的衍生物会增加电刺激诱导的3H - GABA释放,并消除GABA的抑制作用,同时不改变或略微提高3H - GABA的自发释放。得出的结论是,无论对GABA受体的苯二氮䓬结合区域有何影响,哈尔满都会增强GABA能轴突电刺激诱导的递质释放。

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Electrically evoked [3H]GABA release from cerebral cortical cultures: an in vitro approach for studying glutamate-induced neurotoxicity.
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