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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Universality of Oxime K203 for Reactivation of Nerve Agent-Inhibited AChE

Author(s): Kamil Kuca, Martina Hrabinova, Daniel Jun, Kamil Musilek, Marek Penhaker, Ondrej Krejcar and Ondrej Soukup

Volume 11 , Issue 7 , 2015

Page: [683 - 686] Pages: 4

DOI: 10.2174/1573406411666150407154204

Price: $65

Abstract

Oxime K203 seems to be the most promising oxime in case of reactivation of tabuninhibited acetylcholinesterase (AChE). Although it was originally developed for treatment of tabun intoxications, it is able to reactivate cholinesterases inhibited by other nerve agents. This study is aimed at the evaluation of its potency in vitro against other nerve agents. For this purpose, sarin, tabun, cyclosarin, soman, VX, Russian VX and DFP were selected as members of the nerve agent family to check its universality. At high concentrations (10-3 M), oxime K203 reached promising reactivation activity. At low concentrations, relevant for human use (10-5 M), promising reactivation potency was obtained only with tabun. In conclusion, oxime K203 reactivates other nerve agents-inhibited cholinesterases, however its broad-spectrum reactivation is limited at high, for human not attainable, concentrations only.

Keywords: Cholinesterase, K203, oxime, nerve agent, antidote, reactivator.


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