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两种提高神经毒剂中毒解毒治疗效果的可能性。

Two possibilities how to increase the efficacy of antidotal treatment of nerve agent poisonings.

机构信息

Trebesska, Hradec Kralove, Czech Republic.

出版信息

Mini Rev Med Chem. 2012 Jan;12(1):24-34. doi: 10.2174/138955712798869011.

Abstract

Highly toxic organophosphorus inhibitors of acetylcholinesterase referred as nerve agents are considered to be among the most dangerous chemical warfare agents. The oximes represent very important part of medical countermeasures of nerve agent poisonings. They are used to reactivate the nerve agent-inhibited acetylcholinesterase. Despite long-term research activities, there is no single, broad-spectrum oxime suitable for the antidotal treatment of poisoning with all organophosphorus agents. There are two approaches how to increase and broaden the effectiveness of antidotal treatment of poisoning with nerve agents - to develop new structural analogues of currently available oximes and/or to combine currently available or newly developed oximes. The review describes the evaluation of the potency of newly developed oximes (especially the oxime K203) or combinations of oximes to reactivate nerve agent-inhibited acetylcholinesterase and to counteract the acute toxicity of nerve agents in comparison with single commonly used oxime (obidoxime, trimedoxime or HI-6).

摘要

高度有毒的乙酰胆碱酯酶有机磷抑制剂,被称为神经毒剂,被认为是最危险的化学战剂之一。肟类化合物是神经毒剂中毒医疗对策的重要组成部分。它们用于使神经毒剂抑制的乙酰胆碱酯酶重新活化。尽管进行了长期的研究活动,但没有一种单一的、广谱的肟类化合物适合解毒所有有机磷毒剂的中毒治疗。有两种方法可以提高和拓宽神经毒剂中毒解毒治疗的效果 - 开发现有肟类化合物的新结构类似物和/或组合现有的或新开发的肟类化合物。本综述描述了新开发的肟类化合物(特别是肟 K203)或肟类化合物组合的效力评估,以重新激活神经毒剂抑制的乙酰胆碱酯酶,并与单一常用肟类化合物(obidoxime、trimedoxime 或 HI-6)相比,对抗神经毒剂的急性毒性。

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