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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

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.

作者信息

Turski L, Havemann U, Kuschinsky K

出版信息

Life Sci. 1983;33 Suppl 1:755-8. doi: 10.1016/0024-3205(83)90612-4.

DOI:10.1016/0024-3205(83)90612-4
PMID:6420630
Abstract

The effects of the benzodiazepines diazepam and midazolam on the rigidity produced by systemic administration of morphine (15 mg/kg i.p.) were studied in rats. The rigidity was recorded as a tonic activity from the gastrocnemius-soleus muscle of non-anesthetized rats in the electromyogram. Both diazepam (1-5 mg/kg i.p.) and midazolam (2.5 and 5 mg/kg i.p.), when administered 45 min after morphine, temporarily antagonized the muscular rigidity. When the competitive antagonist Ro 15-1788 (ethyl-8-fluoro-5, 6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5a]-[1,4]benzodiazepine-3 -carboxylate) (5 mg/kg i.p.) was administered together with diazepam (5 mg/kg i.p.), it prevented the effect of diazepam, although by itself it did not affect the morphine-induced muscular rigidity. Our results suggest that diazepam, by acting on benzodiazepine receptors, can antagonize the morphine-induced muscular rigidity. The latter phenomenon might serve as a model for some types of muscular rigidity observed in humans.

摘要

研究了苯二氮䓬类药物地西泮和咪达唑仑对大鼠腹腔注射吗啡(15毫克/千克)所致强直的影响。强直表现为非麻醉大鼠腓肠肌-比目鱼肌在肌电图中的强直活动。吗啡注射45分钟后,腹腔注射地西泮(1-5毫克/千克)和咪达唑仑(2.5和5毫克/千克)均可暂时拮抗肌肉强直。当竞争性拮抗剂Ro 15-1788(8-氟-5,6-二氢-5-甲基-6-氧代-4H-咪唑并[1,5a][1,4]苯二氮䓬-3-羧酸乙酯)(5毫克/千克腹腔注射)与地西泮(5毫克/千克腹腔注射)一起给药时,可阻断地西泮的作用,尽管其本身并不影响吗啡诱导的肌肉强直。我们的结果表明,地西泮通过作用于苯二氮䓬受体,可拮抗吗啡诱导的肌肉强直。后一种现象可能是人类某些类型肌肉强直的模型。

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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 antinociceptive effect of cholecystokinin by benzodiazepines and a benzodiazepine antagonist, Ro 15-1788.
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引用本文的文献

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JA Clin Rep. 2024 Aug 1;10(1):47. doi: 10.1186/s40981-024-00732-1.
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Direct mechanomyographic measurement of the myorelaxant action of baclofen and diazepam in normal and reserpinized rats.在正常大鼠和利血平化大鼠中直接肌动图测量巴氯芬和地西泮的肌松作用。
Naunyn Schmiedebergs Arch Pharmacol. 1992 Feb;345(2):209-12. doi: 10.1007/BF00165738.