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通过体外方法比较肟类化合物HLö-7与目前使用的肟类化合物(HI-6、解磷定、双复磷)对神经毒剂抑制的大鼠脑乙酰胆碱酯酶的重活化能力。

A comparison of the potency of the oxime HLö-7 and currently used oximes (HI-6, pralidoxime, obidoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods.

作者信息

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

机构信息

Department of Toxicology, University of Defence in Brno, Faculty of Military Health Sciences in Hradec Králov'e, Czech Republic.

出版信息

Acta Medica (Hradec Kralove). 2005;48(2):81-6.

Abstract

(1) The efficacy of the oxime HLö7 and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. (2) Both H oximes (HLö-7, HI-6) were found to be more efficacious reactivators of sarin and VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. On the other hand, their potency to reactivate tabun-inhibited acetylcholinesterase is very low and does not reach the reactivating efficacy of obidoxime. In the case of cyclosarin, the oxime HI-6 was only found to be able to sufficiently reactivate cyclosarin-inhibited acetylcholinesterase in vitro. (3) Thus, the oxime HLö-7 does not seem to be more efficacious reactivator of nerve agent-inhibited acetylcholinesterase than HI-6 according to in vitro evaluation of their reactivation potency and, therefore, it is not more suitable to be introduced for antidotal treatment of nerve agent-exposed people than HI-6.

摘要

(1) 采用体外方法测试了肟HLö7与目前使用的肟(解磷定、双复磷、HI - 6)对各种神经毒剂(沙林、塔崩、环沙林、VX)抑制的乙酰胆碱酯酶的重活化效果。(2) 发现两种H型肟(HLö - 7、HI - 6)对沙林和VX抑制的乙酰胆碱酯酶的重活化效果比解磷定和双复磷更好。另一方面,它们对塔崩抑制的乙酰胆碱酯酶的重活化能力非常低,未达到双复磷的重活化效果。对于环沙林,仅发现肟HI - 6在体外能够充分重活化环沙林抑制的乙酰胆碱酯酶。(3) 因此,根据体外对其重活化能力的评估,肟HLö - 7似乎并非比HI - 6对神经毒剂抑制的乙酰胆碱酯酶更有效的重活化剂,所以与HI - 6相比,它并不更适合用于对接触神经毒剂人员的解毒治疗。

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