Optimal Choice of Acetylcholinesterase Reactivators for Antidoral Treatment of Nerve Agent Intoxication

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Strategy for the development of new acetylcholinesterase reactivators - antidotes used for treatment of nerve agent poisonings.

The mechanism of intoxication with organophosphorus compounds, including highly toxic nerve agents, is based on the formation of irreversibly inhibited acetylcholinesterase (AChE; EC 3.1.1.7) that could be followed by a generalized cholinergic crisis. Nerve agent poisoning is conventionally treated using a combination of a cholinolytic drug (atropine mostly) to counteract the accumulation of ac...

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Nicotinic antagonists in the treatment of nerve agent intoxication.

Organophosphorus (OP) nerve agents are potent inhibitors of human acetylcholinesterase and butyrylcholinesterase. Although some OPs may induce delayed toxic effects on muscle and nerve,1 it is the inhibition of acetylcholinesterase that accounts for the acute life-threatening toxicity of soman, sarin, VX, tabun and similar OP compounds. This acute toxicity, which arises from the uncontrolled ac...

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Treatment and Prophylaxis of Nerve Agent/ Organophosphates Intoxication

Basic mechanism of action of organophosphates (OP)/nerve agents is based on acetylcholinesterase (AChE) inhibition and subsequent accumulation of neuromediator acetylcholine at the cholinergic synapses, either peripheral or central, causing cholinergic hyperstimulation and development of symptoms of poisoning, followed by metabolic dysbalance and, without eff ective prophylaxis/treatment leadin...

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Central Acetylcholinesterase Reactivation by Oximes Improves Survival and Terminates Seizures Following Nerve Agent Intoxication

The current treatment regimen for organophosphorus nerve agent intoxication depends on the ability of oximes to rapidly reactivate nerve agent-inhibited acetylcholinesterase (AChE) activity. We have studied the capability of the tertiary oximes monoisonitrosoacetone (MINA) and diacetylmonoxime (DAM), in comparison with the quaternary oximes 2-PAM, HLö7 and MMB-4, to reactivate AChE inhibited by...

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ژورنال

عنوان ژورنال: Acta Medica (Hradec Kralove, Czech Republic)

سال: 2010

ISSN: 1211-4286,1805-9694

DOI: 10.14712/18059694.2016.78