Abstract
In the past decades a vast number of oximes have been synthesised in order to identify effective compounds for the reactivation of organophosphorus compound (OP)-inhibited acetylcholinesterase (AChE). Up to now, oxime efficacy has been tested primarily in animal experiments. However, the accretive evidence of substantial species differences regarding kinetic properties of human and animal AChE led to an increasing number of in vitro kinetic studies quantifying the reactivating potency of oximes. These data were shown to provide a basis for the selection of effective oximes and for defining adequate oxime doses in human OP poisoning. This review will discuss experimental and theoretical models for the in vitro assessment of oxime efficacy and will give an overview of the present status in the evaluation of oximes as antidotes against OP poisoning.
Keywords: Oxime, organophosphate, acetylcholinesterase, in vitro study
Current Bioactive Compounds
Title: Kinetic Analysis of Oxime Interactions with Acetylcholinesterase as a Basis for the Evaluation of Oxime Efficacy in Organophosphate Poisoning
Volume: 6 Issue: 1
Author(s): F. Worek, P. Eyer, N. Aurbek and H. Thiermann
Affiliation:
Keywords: Oxime, organophosphate, acetylcholinesterase, in vitro study
Abstract: In the past decades a vast number of oximes have been synthesised in order to identify effective compounds for the reactivation of organophosphorus compound (OP)-inhibited acetylcholinesterase (AChE). Up to now, oxime efficacy has been tested primarily in animal experiments. However, the accretive evidence of substantial species differences regarding kinetic properties of human and animal AChE led to an increasing number of in vitro kinetic studies quantifying the reactivating potency of oximes. These data were shown to provide a basis for the selection of effective oximes and for defining adequate oxime doses in human OP poisoning. This review will discuss experimental and theoretical models for the in vitro assessment of oxime efficacy and will give an overview of the present status in the evaluation of oximes as antidotes against OP poisoning.
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Worek F., Eyer P., Aurbek N. and Thiermann H., Kinetic Analysis of Oxime Interactions with Acetylcholinesterase as a Basis for the Evaluation of Oxime Efficacy in Organophosphate Poisoning, Current Bioactive Compounds 2010; 6 (1) . https://dx.doi.org/10.2174/157340710790711728
DOI https://dx.doi.org/10.2174/157340710790711728 |
Print ISSN 1573-4072 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6646 |
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