Abstract
In this work, two oximes for the treatment of tabun-inhibited acetylcholinesterase (AChE; EC 3.1.1.7), K074 (1,4-bis(4-hydroxyiminomethyl-pyridinium) butane dibromide) and K075 ((E)-1,4-bis(4-hydroxyiminomethylpyridinium)but-2-en dibromide), were testedin vitro as reactivators of AChE. Comparison was made with currently used AChE reactivators (pralidoxime, HI-6, methoxime and obidoxime). Human brain homogenate was taken as an appropriate source of the cholinesterases. As resulted, oxime K074 appears to be the most potent reactivator of tabun-inhibited AChE, with reactivation potency comparable to that of obidoxime. A second AChE reactivator, K075, does not attain as great a reactivation potency as K074, although its maximal reactivation (17%) was achieved at relevant concentrations for humans.
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Kuca, K., Cabal, J., Jun, D. et al. In vitro reactivation potency of acetylcholinesterase reactivators — K074 and K075 — to reactivate tabun-inhibited human brain cholinesterases. neurotox res 11, 101–106 (2007). https://doi.org/10.1007/BF03033389
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DOI: https://doi.org/10.1007/BF03033389