Literature DB >> 21981462

A comparison of the efficacy of newly developed reversible inhibitors of acetylcholinesterase with commonly used pyridostigmine as pharmacological pre-treatment of soman-poisoned mice.

Jiri Kassa1, Kamil Musilek, Marketa Koomlova, Jiri Bajgar.   

Abstract

The ability of three newly developed reversible inhibitors of acetylcholinesterase (AChE) (K298, K344 and K474) and currently available carbamate pyridostigmine to increase the resistance of mice against soman and the efficacy of antidotal treatment of soman-poisoned mice was compared. Neither pyridostigmine nor new reversible inhibitors of AChE were able to increase the LD(50) value of soman. Thus, the pharmacological pre-treatment with pyridostigmine or newly synthesized inhibitors of AChE was not able to protect mice against soman-induced lethal acute toxicity. The pharmacological pre-treatment with pyridostigmine alone or with K474 was able to slightly increase the efficacy of antidotal treatment (the oxime HI-6 in combination with atropine) of soman-poisoned mice, but the increase in the efficacy of antidotal treatment was not significant. The other newly developed reversible inhibitors of AChF (K298, K344) were completely ineffective. These findings demonstrate that pharmacological pre-treatment of soman-poisoned mice with tested reversible inhibitors of AChF is not promising.
© 2011 The Authors. Basic & Clinical Pharmacology & Toxicology © 2011 Nordic Pharmacological Society.

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Year:  2011        PMID: 21981462     DOI: 10.1111/j.1742-7843.2011.00808.x

Source DB:  PubMed          Journal:  Basic Clin Pharmacol Toxicol        ISSN: 1742-7835            Impact factor:   4.080


  1 in total

1.  Development of small bisquaternary cholinesterase inhibitors as drugs for pre-treatment of nerve agent poisonings.

Authors:  Kamil Kuca; Jana Zdarova Karasova; Ondrej Soukup; Jiri Kassa; Eva Novotna; Vendula Sepsova; Anna Horova; Jaroslav Pejchal; Martina Hrabinova; Eva Vodakova; Daniel Jun; Eugenie Nepovimova; Martin Valis; Kamil Musilek
Journal:  Drug Des Devel Ther       Date:  2018-03-09       Impact factor: 4.162

  1 in total

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