A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase

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Evaluation of oxime k203 as antidote in tabun poisoning.

We studied bispyridinium oxime K203 [(E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide] with tabun-inhibited human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro, and its antidotal effect on tabun-poisoned mice and rats in vivo. We compared it with oximes K048 and TMB-4, which have proven the most efficient oxime antidotes in tabun poiso...

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The Evaluation of the Reactivating and Neuroprotective Efficacy of Two Newly Prepared Bispyridinium Oximes (K305, K307) in Tabun-Poisoned Rats-A Comparison with Trimedoxime and the Oxime K203.

The ability of two newly developed oximes (K305, K307) to protect tabun-poisoned rats from tabun-induced inhibition of brain acetylcholinesterase, acute neurotoxic signs and symptoms and brain damage was compared with that of the oxime K203 and trimedoxime. The reactivating and neuroprotective effects of the oximes studied combined with atropine on rats poisoned with tabun at a sublethal dose w...

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The Length Dependent Activity of Oximes on Reactivation of Tabun Inhibited Acetylcholinesterase; A Theoretical Study

In this work, the effect of ligand's length on interaction energy of six oximes, A [2-(hydroxyimino)-N-((1-(2-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], B [2-(hydroxyimino)-N-((1-(3-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)propyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], C [2-(hydroxyimino)-N-((1-(4-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)but...

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A comparison of the reactivating and therapeutic efficacy of the newly developed bispyridinium oxime K203 with currently available oximes, in sarin poisoned rats and mice

This study compares the abilities of the newly developed bispyridinium oxime K203 with currently available oximes (HI-6, obidoxime, and trimedoxime) in the reactivation of sarin-inhibited acetylcholinesterase and the reduction of the acute toxicity of sarin. The percentage of reactivation of sarin-inhibited rat blood and tissue acetylcholinesterase was determined in vivo and it was shown that t...

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Effects of Oxime K203 and Oxidative Stress in Plasma of Tabun Poisoned Rats

The highly toxic nature of tabun has been known for many years, but there are still serious limitations to antidotal therapy. In this study, we used rats as an experimental model to evaluate the efficiency of bispyridinium para-oxime K203 as therapy against tabun poisoning as well as to examine if induction of oxidative stress is linked to organophosphate toxicity. K203 showed high potency in c...

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ژورنال

عنوان ژورنال: BMC Pharmacology and Toxicology

سال: 2018

ISSN: 2050-6511

DOI: 10.1186/s40360-018-0196-3