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肟类化合物(解磷定、双复磷、HI-6)对猪脑不同部位中被沙林抑制的乙酰胆碱酯酶的体外重新激活效力比较。

Comparison of in vitro potency of oximes (pralidoxime, obidoxime, HI-6) to reactivate sarin-inhibited acetylcholinesterase in various parts of pig brain.

作者信息

Kuca Kamil, Cabal Jiri, Kassa Jiri, Jun Daniel, Hrabinová Martina

机构信息

Department of Toxicology, Faculty of Military Health Sciences, PO Box 35/T, 500 01, Hradec Králové, Czech Republic.

出版信息

J Appl Toxicol. 2005 Jul-Aug;25(4):271-6. doi: 10.1002/jat.1053.

Abstract

The potency of currently used oximes to reactivate sarin-inhibited acetylcholinesterase (AChE) in various parts of pig brain and whole pig brain was evaluated using in vitro methods. Significant differences in reactivation potency among all tested oximes were observed. At concentrations (10(-4) M) corresponding to recommended doses in vivo, the oxime HI-6 seems to be a more efficacious reactivator of sarin-inhibited AChE in whole pig brain as well as in cerebral hemispheres and cerebellum compared with the other oximes studied. Nevertheless, there are not any differences in the potency of oximes tested to reactivate sarin-inhibited AChE in medulla oblongata. Thus, the oxime HI-6 appears to be the most promising oxime among currently available oximes for the antidotal treatment of acute sarin poisoning, although it is not more efficacious than other currently used oximes in medulla oblongata, whose function is necessary for the vital functions of respiration and circulation.

摘要

采用体外方法评估了当前使用的肟类化合物对猪脑各部分及全猪脑中沙林抑制的乙酰胆碱酯酶(AChE)的重活化能力。观察到所有测试肟类化合物的重活化能力存在显著差异。在与体内推荐剂量相对应的浓度(10⁻⁴ M)下,与其他研究的肟类化合物相比,肟类化合物HI - 6似乎是全猪脑以及大脑半球和小脑中沙林抑制的AChE更有效的重活化剂。然而,所测试的肟类化合物对延髓中沙林抑制的AChE的重活化能力没有差异。因此,肟类化合物HI - 6似乎是目前可用肟类化合物中用于急性沙林中毒解毒治疗最有前景的肟类化合物,尽管它在延髓中的效果并不比其他目前使用的肟类化合物更有效,而延髓的功能对于呼吸和循环的 vital functions 是必需的。 (注:vital functions 直译为“重要功能”,此处表述不太准确,结合上下文推测可能是指维持生命的基本功能,但按要求未做修改。)

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