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. 2006 Dec;2(4):141–146. doi: 10.1007/BF03161181

Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes

Kamil Kuca 1,✉, Daniel Jun 1
PMCID: PMC3550075  PMID: 18072133

Abstract

Introduction

Organophosphorus nerve agents inhibit the enzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators (also known as oximes) are generally used for the reactivation of an inhibited enzyme.

Methods

Two new AChE reactivators—K033 and K027—were tested for theirin vitro reactivation of sarin-inhibited pig-brain AChE. Their reactivation potencies were compared with the commercially available AChE reactivators, pralidoxime, obidoxime, and HI-6.

Results

Of the oximes tested, the newly developed oxime K027 achieved the highest reactivation potency (100%; concentration of the oxime −10−2 M). However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10−4 M and lower).

Conclusion

For human relevant doses, newly developed oximes (K027 and K033) do not surpass the reactivation potency of the most promising oxime, HI-6.

Keywords: acetylcholinesterase, reactivation, sarin, nerve agents, inhibition, pig brain homogenate

Full Text

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Footnotes

There was no outside funding of any kind used for this study.

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