Journal of APPLIED BIOMEDICINE
ISSN 1214-0287 (on-line)
ISSN 1214-021X (printed)

Volume 2 (2004), No 1, p 51-56




Synthesis of the three monopyridinium oximes and evaluation of their potency to reactivate acetylcholinesterase inhibited by nerve agents

Kamil Kuca, Jan Picha, Jiri Cabal, Frantisek Liska

Address: Kamil Kuca, Purkyne Military Medical Academy, Department of Toxicology, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic
kucakam@pmfhk.cz

Received 23rd May 2003.
Revised 3rd October 2003.
Published online 16th October 2003.

Full text article (pdf)

SUMMARY
Three potential reactivators of nerve agents-inhibited acetylcholinesterase: 2-[(hydroxyimino)phenylmethyl]-1-methylpyridinium iodide 3a, 2-[(hydroxyimino)pyridin-2-ylmethyl]-1-methylpyridinium iodide 3b and 2-[(1-hydroxyimino) ethyl]-1-methylpyridinium iodide 3c were synthesized. Their reactivation potency was examined using a standard in vitro reactivation test. A rat brain homogenate was used as the source of acetylcholinesterase. Their reactivation potency was compared with a currently used acetylcholinesterase reactivator - 2-PAM (pralidoxime) 4. All tested reactivators were less effective acetylcholinesterase reactivators compared to 2-PAM. In this study, we also tested the reactivation potency of the oxime 2-PAM against inhibition of acetylcholinesterase by sarin, cyclosarin, VX and tabun. Satisfactory results are shown only for the reactivation sarin- and VX-inhibited acetylcholinesterase.

KEY WORDS
VX; reactivation; acetylcholinesterase; oximes; sarin; tabun; cyclosarin


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