background: the role and proper dose of pralidoxime in the treatment of organophosphorus (op) compounds poisoning is an unresolved issue .this study was designed to compare the regimen recommended by the world health organization (who) with the commonly used standard regimen of pralidoxime. methods: this was a randomized open labeled prospective study on op poisoned patients admitted to jss hos...

Four novel bisquaternary aldoxime cholinesterase reactivators differing in their chemical structure were prepared. Afterwards, their biological activity was evaluated for their ability to reactivate acetylcholinesterase (AChE; EC 3.1.1.7) and butyrylcholinesterase (BuChE; EC 3.1.1.8) inhibited by paraoxon. Their reactivation activity was compared with standard reactivators--pralidoxime, obidoxi...

1. Reactivation of erythrocyte cholinesterase inhibited by ethyl p-nitrophenyl ethylphosphonate (armine) was studied with NN'-dimethylenebis-(4-hydroxy-iminomethylpyridinium bromide) (C(2)-oxime), NN'-trimethylenebis-(4-hydroxy-iminomethylpyridinium bromide) (C(3)-oxime), NN'-tetramethylene-(4-hydroxy-iminomethylpyridinium bromide) (C(4)-oxime) and NN'-pentamethylenebis-(4-hydroxyiminomethylpyr...

The therapeutical efficacies of eleven oxime-based acetylcholinesterase reactivators were compared in an in vivo (rat model) study of treatment of intoxication caused by tabun. In this group there were some currently available oximes (obidoxime, trimedoxime and HI-6) and the rest were newly synthesized compounds. The best reactivation efficacy for acetylcholinesterase in blood (expressed as per...

Basic mechanism of action of organophosphates (OP)/nerve agents is based on acetylcholinesterase (AChE) inhibition and subsequent accumulation of neuromediator acetylcholine at the cholinergic synapses, either peripheral or central, causing cholinergic hyperstimulation and development of symptoms of poisoning, followed by metabolic dysbalance and, without eff ective prophylaxis/treatment leadin...

This paper describes an in vitro study of three potential acetylcholinesterase (AChE; EC 3.1.1.7) reactivators derived from a monoquaternary reactivator pralidoxime. Compounds used were pyridinium-2-aldoxime-4-carbamoyl-N-methyl iodide (TO231), pyridinium-2-aldoxime-4-ethoxycarbonyl-N-methyl iodide (TO237), and pyridinium-2-aldoxime-5-ethoxycarbonyl-N-methyl iodide (TO238). Pralidoxime and obid...

Oxime cholinesterase reactivators (oximes) are used to counteract organophosphate intoxication. Charged oximes administered via intramuscular or intravenous injection when the majority of dose is unmetabolized and excreted as urine. In this study, effects selected double charged were determined in HK-2 cell line a model for renal toxicity screening. Some on dehydrogenase activity found obidoxim...

Recently, several bis-pyridiniumaldoximes linked by a variable-length alkylene chain were rationally designed in our laboratories as cholinesterase reactivators. Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and ...

Nerve agents belong to the most toxic organophosphates (OP) in the group of cholinesterase inhibitors. They can be used as chemical warfare agents and, they can be (and were) misused by terrorists, as happened in Matsumoto city (1994) and Tokyo subway (1995). Sarin was used in these cases. Medical protection against their effect (i.e. antidotal treatment) is of prime importance (Bajgar 2004, 20...