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新型苯二氮䓬受体部分激动剂咪达氮䓬对有机磷中毒惊厥的治疗作用。

Effects of imidazenil, a new benzodiazepine receptor partial agonist, in the treatment of convulsions in organophosphate intoxications.

作者信息

Rump S, Gidynska T, Galecka E, Antkowiak O, Nawrocka M, Kowalczyk M

机构信息

Department of Pharmacology and Toxicology, Military Institute of Hygiene and Epidemiology, Kozielska 4, 01-163 Warsaw, Poland.

出版信息

Neurotox Res. 2000;2(1):17-22. doi: 10.1007/BF03033323.

DOI:10.1007/BF03033323
PMID:15545002
Abstract

Anticonvulsant and antilethal effects of imidazenil, a new imidazobenzodiazepine derivative, in fluostigmine (DFP; diisopropyl phosphorofluoridate) intoxications were studied and compared with the effects of diazepam on mice and rats. Special attention was payed to the myorelaxant effects of both drugs. It was stated that imidazenil (i) significantly decreased convulsion intensity in mice, (ii) quickly inhibited seizure patterns in bioelectrical activity in the rat's brain, (iii) significantly increased antilethal effectiveness of the standard therapy in mice intoxicated with DFP. These effects are comparable to those of diazepam. However, effects of imidazenil in the rota-rod test of the mouse were noted in doses 5-10 times higher than therapeutic ones, when effects of diazepam on motor co-ordination were seen in therapeutic dosage.

摘要

研究了新型咪唑并苯二氮䓬衍生物咪达唑尼在氟斯的明(二异丙基氟磷酸酯,DFP)中毒中的抗惊厥和抗致死作用,并与地西泮对小鼠和大鼠的作用进行了比较。特别关注了两种药物的肌松作用。结果表明,咪达唑尼(i)显著降低了小鼠的惊厥强度,(ii)迅速抑制了大鼠大脑生物电活动中的癫痫发作模式,(iii)显著提高了DFP中毒小鼠标准治疗的抗致死效果。这些作用与地西泮相当。然而,在小鼠转棒试验中,咪达唑尼产生作用的剂量比治疗剂量高5 - 10倍,而地西泮在治疗剂量时就可见对运动协调的作用。

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引用本文的文献

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Proc Natl Acad Sci U S A. 2008 Sep 16;105(37):14169-74. doi: 10.1073/pnas.0807172105. Epub 2008 Sep 10.

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Effects of diazepam on epileptiform patterns of bioelectrical activity of the rabbit's brain induced by fluostigmine.地西泮对毒扁豆碱诱发的兔脑生物电活动癫痫样模式的影响。
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