engleski

Antidotal treatment of soman intoxication in mice with bispyridinium oximes

Like organophosphosphate insecticides, nerve agents phosphorylate and inactivate acetylcholinesterase (AChE), leading to accumulation of acetylcholine at nicotinic and muscarinic receptors, and other receptors in the central nervous system (CNS). Together with atropine, pyridinium oximes are known to be successfully used to treat poisoning with many OPs. The aim of this study was to evalute the efficacy of three new bis-pyridinium compounds: [1-(4-hydroxyiminomethyl pyridinium)-3-(4-carbamoyl pyridinium)] propane dibromide ( K 027), [1-(4- hydroxyiminomethyl pyridinium)-4-(4-carbamoylpyridinium)] butane dibromide (K 048) and [1, 4-bis (2-hydroxyiminomethyl pyridinium)] butane dibromide (K 033), in combination with atropine in the therapy of soman intoxication in mice in vivo. Their acute intraperitoneal (i.p.) toxicity (LD50 with 95% confidence limits) was tested and observed for 24 hours. The therapeutic effect was expressed as the therapeutic factor (TF) with 95% confidence limits and as the therapeutic dose (TD). In vivo results show that the tested compounds are relatively toxic (their LD50 was from 33.4 to 672.8 mg/kg body weight). Generally, in vivo toxicity of these compounds and their antidotal efficacy expressed as the TF, TD and the ratio between dead and injected experimental animals were depended of type of the substituent in the pyridinium ring, and chains between pyridinium moieties.

Bispyridinium oximes; Soman; AChE

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