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[每日多次给予芬乙茶碱和地西泮对小鼠脑内γ-氨基丁酸(GABA)和苯二氮䓬受体的影响]

[Effect of multiple daily administration of fenibut and diazepam on GABA and benzodiazepine receptors in the mouse brain].

作者信息

Riago L K, Sarv Kh A, Allikmets L Kh

出版信息

Biull Eksp Biol Med. 1983 Dec;96(12):49-50.

PMID:6140966
Abstract

It was shown in experiments on mice that 25 hours after chronic treatment with fenibut (100 mg/kg, twice daily for 10 days) was discontinued the number of benzodiazepine and GABAA (bicucullin-sensitive) receptor sites was increased and 48 hours after treatment discontinuation the number of GABAB (bicucullin nonsensitive) sites was decreased. The enhanced binding to GABAA and GABAB receptor sites and the decreased binding to benzodiazepine receptors was observed 24 hours after discontinuation of chronic treatment with diazepam (5 mg/kg, twice daily). Forty-eight hours after diazepam chronic treatment was discontinued the number of benzodiazepine receptor sites was increased. The involvement of the increased benzodiazepine receptor sensitivity in the mechanism of therapeutic activity of fenibut is suggested.

摘要

在小鼠实验中发现,长期服用芬尼布(100毫克/千克,每日两次,共10天)停药25小时后,苯二氮䓬和GABAA(荷包牡丹碱敏感型)受体位点数量增加,停药48小时后,GABAB(荷包牡丹碱不敏感型)位点数量减少。停用地西泮(5毫克/千克,每日两次)进行长期治疗24小时后,观察到与GABAA和GABAB受体位点的结合增强,与苯二氮䓬受体的结合减少。地西泮长期治疗停药48小时后,苯二氮䓬受体位点数量增加。提示苯二氮䓬受体敏感性增加参与了芬尼布的治疗活性机制。

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[Pharmacology of benzodiazepine receptors].
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