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A comparison of reactivating efficacy of newly developed oximes (K074, K075) and currently available oximes (obidoxime, HI-6) in soman, cyclosarin and tabun-poisoned rats.
Due to their reactivating effects, both newly developed K oximes can be considered to be promising oximes for the antidotal treatment of acute tabun poisonings while the oxime HI-6 is still the most promising oxime for thetreatment of acute soman and cyclosarin poisonings. Expand
Oximes: Inhibitors of Human Recombinant Acetylcholinesterase. A Structure-Activity Relationship (SAR) Study
The goal of the present study is to determine how oxime structure influences the inhibition of human recombinant AChE (hrAChE), so 24 structurally different oximes were tested and the results compared to the previous eel A cholinesterase (EeA chE) experiments. Expand
Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma
K027 [1‐(4‐hydroxyiminomethylpyridinium)‐3‐(4‐carbamoylpyridinium)–propane dibromide] is a promising new reactivator of organophosphate‐ or organophosphonate‐inhibited acetylcholinesterase (AChE)Expand
Partition of bispyridinium oximes (trimedoxime and K074) administered in therapeutic doses into different parts of the rat brain.
It was confirmed that oximes are able to penetrate into the brain after injection of therapeutic doses corresponding with 5% of LD(50), and their levels achieved in different brain regions 60 min after the administration were detected. Expand
Effect of five acetylcholinesterase reactivators on tabun‐intoxicated rats: induction of oxidative stress versus reactivation efficacy
The potency of oximes to reactivate brain AChE was lower due to the poor blood–brain barrier penetration of used compounds, and the oxidative stress provoked by HI‐6 and K628 was found to be significant on probability level P = 0.05. Expand
Two possibilities how to increase the efficacy of antidotal treatment of nerve agent poisonings.
The review describes the evaluation of the potency of newly developed oximes or combinations of oximes to reactivate nerve agent-inhibited acetylcholinesterase and to counteract the acute toxicity of nerve agents in comparison with single commonly used oxime. Expand
Changes of rat plasma total low molecular weight antioxidant level after tabun exposure and consequent treatment by acetylcholinesterase reactivators
The principle of oxime reactivator function and a novel insight into AChE activity regulation and oxidative stress is discussed and the sizable modulation of low molecular weight antioxidant (LMWA) levels was determined. Expand
Time-Dependent Changes of Oxime K027 Concentrations in Different Parts of Rat Central Nervous System
This study showed that oxime K027 is able to achieve high concentration level in perfused brain tissue relatively quickly, but also demonstrated rapid clearance from the central nervous system, probably due to low overall uptake of oximes into the brain. Expand
Pharmacokinetics of acetylcholinesterase reactivator K203 and consequent evaluation of low molecular weight antioxidants/markers of oxidative stress
Oxime K203 is a new compound designed to be used as an acetylcholinesterase reactivator for the treatment of intoxication following exposure to tabun and certain pesticides. After intramuscularExpand
Inhibition of blood cholinesterases following intoxication with VX and its derivatives
Nerve agents can be divided into G‐agents (sarin, soman, tabun, cyclosarin etc.) and V‐agents and their properties were studied in rats in vivo. Expand