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一种特异性苯二氮䓬拮抗剂Ro 15 - 1788可逆转地西泮而非普罗加比的肌肉松弛作用。

Reversal of the muscle relaxant effect of diazepam but not of progabide by a specific benzodiazepine antagonist: Ro 15-1788.

作者信息

Schwarz M, Turski L, Sontag K H

出版信息

Eur J Pharmacol. 1983 May 20;90(1):139-42. doi: 10.1016/0014-2999(83)90226-1.

DOI:10.1016/0014-2999(83)90226-1
PMID:6409655
Abstract

The muscle relaxant effects of diazepam and progabide were studied in mutant Han-Wistar rats which exhibit spontaneous tonic activity in the electromyogram of the gastrocnemius-soleus muscle. Treatment with diazepam or progabide produced a dose-related reduction of the spontaneous activity measured in the electromyogram. The depressant effect of diazepam, but not that of progabide was antagonized by the specific benzodiazepine antagonist Ro 15-1788. From these data it is apparent that the muscle relaxant effect of progabide is not mediated through an alteration of benzodiazepine receptors.

摘要

在突变的Han-Wistar大鼠中研究了地西泮和普罗加比的肌肉松弛作用,这些大鼠在腓肠肌-比目鱼肌的肌电图中表现出自发性强直活动。用地西泮或普罗加比治疗可使肌电图中测得的自发活动呈剂量依赖性降低。特异性苯二氮䓬拮抗剂Ro 15-1788可拮抗地西泮的抑制作用,但不能拮抗普罗加比的抑制作用。从这些数据可以明显看出,普罗加比的肌肉松弛作用不是通过改变苯二氮䓬受体介导的。

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Reversal of the muscle relaxant effect of diazepam but not of progabide by a specific benzodiazepine antagonist: Ro 15-1788.一种特异性苯二氮䓬拮抗剂Ro 15 - 1788可逆转地西泮而非普罗加比的肌肉松弛作用。
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Is the muscle relaxant effect of diazepam in spastic mutant rats mediated through GABA-independent benzodiazepine receptors?地西泮对痉挛性突变大鼠的肌肉松弛作用是否通过不依赖γ-氨基丁酸(GABA)的苯二氮䓬受体介导?
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CGS 8216, Ro 15-1788 and methyl-beta-carboline-3-carboxylate, but not EMD 41717 antagonize the muscle relaxant effect of diazepam in genetically spastic rats.CGS 8216、Ro 15 - 1788和甲基-β-咔啉-3-羧酸酯,但不是EMD 41717,可拮抗地西泮对遗传性痉挛大鼠的肌肉松弛作用。
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Reversal of the muscle relaxant effect of diazepam by the specific benzodiazepine antagonist Ro 15-1788: an electromyographic study in morphine model of muscular rigidity in rats.特异性苯二氮䓬拮抗剂Ro 15 - 1788对安定肌松作用的逆转:大鼠吗啡诱导肌强直模型的肌电图研究
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Reversal of the antiaversive and anticonvulsant actions of diazepam, but not of progabide, by a selective antagonist of benzodiazepine receptors.苯二氮䓬受体选择性拮抗剂可逆转地西泮的抗厌恶和抗惊厥作用,但不能逆转普罗加比的此类作用。
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Effect of aminophylline on muscle relaxant action of diazepam and phenobarbitone in genetically spastic rats: further evidence for a purinergic mechanism in the action of diazepam.氨茶碱对遗传性痉挛大鼠地西泮和苯巴比妥肌肉松弛作用的影响:地西泮作用中嘌呤能机制的进一步证据。
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