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[荷包牡丹碱与氨基硫脲对安定镇静作用的拮抗效应]

[Antagonistic effect of bicuculline and thiosemicarbazide on the tranquilizing effects of diazepam].

作者信息

Ostrovskaia R U, Voronina T A

出版信息

Biull Eksp Biol Med. 1977 Mar;83(3):293-5.

PMID:851632
Abstract

It has been shown that bicuculline--GABA-ergic receptors specific blocking agent in doses of 0.5 and 1.0 mg/kg (subcutaneously), and thiosemicarbazide (inhibiting the brain GABA synthesis) in dose of 5.0 and 8.0 mg/kg (subcutaneously) were capable of antagonizing diazepam effects and of reducing its tranquilizing activity in an experimental test of conflict behavior in rats. Bicuculline exhibited a more pronounced antagonism to diazepam than thiosemicarbazide. The data obtained testified to a possible involvement of the GABA-ergic mechanisms in the realization of the anxiolytic effect of benzodiazepines.

摘要

业已表明,荷包牡丹碱(剂量为0.5和1.0毫克/千克,皮下注射)——一种γ-氨基丁酸能受体特异性阻断剂,以及氨基硫脲(剂量为5.0和8.0毫克/千克,皮下注射,抑制大脑γ-氨基丁酸的合成),在大鼠冲突行为的实验测试中,能够拮抗地西泮的作用并降低其镇静活性。荷包牡丹碱对地西泮的拮抗作用比氨基硫脲更为明显。所获得的数据证明γ-氨基丁酸能机制可能参与了苯二氮䓬类药物抗焦虑作用的实现。

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