Nové bispyridiniové oximy: in vitro zhodnocení jejich biochemických parametrů

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F08%3A00001923" target="_blank" >RIV/60162694:G44__/08:00001923 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

New bispyridinium oximes: in vitro evaluation of their biochemical parameters

Popis výsledku v původním jazyce

Improving the efficacy of antidotal treatment of poisonings with nerve agents is still a challenge for the scientific community. This study investigated the interactions of four bispyridinium oximes with human erythrocyte acetylcholinesterase (AChE) andtheir effects on soman- and tabun-poisoned mice. Oximes HI-6 and TMB-4 were used for comparison.These oximes inhibited AchE with inhibitory potency (IC50) ranging from 0.02 to 1.0 mM. The best reactivating potency (%R) was obtained with K074, when AChE was inhibited by tabun.The protective potency (P50) of all oximes in human erythrocyte AChE inhibited by soman and tabun could not be determined. In tabun-poisoned mice very good antidotal efficacy was obtained with K027, K048, and K074, which makes theminteresting for future investigation. The combination of HI-6 and atropine is the therapy of choice for soman poisoning.

Název v anglickém jazyce

New bispyridinium oximes: in vitro evaluation of their biochemical parameters

Popis výsledku anglicky

Improving the efficacy of antidotal treatment of poisonings with nerve agents is still a challenge for the scientific community. This study investigated the interactions of four bispyridinium oximes with human erythrocyte acetylcholinesterase (AChE) andtheir effects on soman- and tabun-poisoned mice. Oximes HI-6 and TMB-4 were used for comparison.These oximes inhibited AchE with inhibitory potency (IC50) ranging from 0.02 to 1.0 mM. The best reactivating potency (%R) was obtained with K074, when AChE was inhibited by tabun.The protective potency (P50) of all oximes in human erythrocyte AChE inhibited by soman and tabun could not be determined. In tabun-poisoned mice very good antidotal efficacy was obtained with K027, K048, and K074, which makes theminteresting for future investigation. The combination of HI-6 and atropine is the therapy of choice for soman poisoning.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FP - Ostatní lékařské obory

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2008

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Chemico-Biological Interactions

ISSN

0009-2797

e-ISSN

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Svazek periodika

175

Číslo periodika v rámci svazku

1-3

Stát vydavatele periodika

IE - Irsko

Počet stran výsledku

4

Strana od-do

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Kód UT WoS článku

000260110500079

EID výsledku v databázi Scopus

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