The antidotal efficacy of the bispyridinum oximes K027 and TMB-4 against tabun poisoning in mice

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F10%3A00002237" target="_blank" >RIV/60162694:G44__/10:00002237 - 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

The antidotal efficacy of the bispyridinum oximes K027 and TMB-4 against tabun poisoning in mice

Popis výsledku v původním jazyce

A toxic effect of highly toxic nervous agents is irreversible inhibition of vitally important enzyme acethylcholinesterase (AChE). Inhibition of AChE results in accumulation of acetylcholine (ACh) at the synaptic cleft of the cholinergic neurons, leadingto overstimulation of cholinergic receptors. The highly toxic nature of tabun has been known for many years, but there are still serious limitations to the antidotal therapy. In this paper a bispyridinium compound K027 [1-(4-hydroxyiminomethylpyridinium)-3-(-4-carbamoylpyridinium) propane dibromide] was tested as potential antidote in tabun poisoned mice. Oxime TMB-4 was included for comparison. The therapeutic efficacy of applied antidotal regimens was tested as pretreatment given 15 min before tabunpoisoning and/or as therapy given 1 min after tabun poisoning. Using oxime K027 (25% of its LD(50)) plus atropine as both, pretreatment and therapy, we showed that this combination can protect mice 8 times better than the therapy alone. U

Název v anglickém jazyce

The antidotal efficacy of the bispyridinum oximes K027 and TMB-4 against tabun poisoning in mice

Popis výsledku anglicky

A toxic effect of highly toxic nervous agents is irreversible inhibition of vitally important enzyme acethylcholinesterase (AChE). Inhibition of AChE results in accumulation of acetylcholine (ACh) at the synaptic cleft of the cholinergic neurons, leadingto overstimulation of cholinergic receptors. The highly toxic nature of tabun has been known for many years, but there are still serious limitations to the antidotal therapy. In this paper a bispyridinium compound K027 [1-(4-hydroxyiminomethylpyridinium)-3-(-4-carbamoylpyridinium) propane dibromide] was tested as potential antidote in tabun poisoned mice. Oxime TMB-4 was included for comparison. The therapeutic efficacy of applied antidotal regimens was tested as pretreatment given 15 min before tabunpoisoning and/or as therapy given 1 min after tabun poisoning. Using oxime K027 (25% of its LD(50)) plus atropine as both, pretreatment and therapy, we showed that this combination can protect mice 8 times better than the therapy alone. U

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

<a href="/cs/project/GP305%2F07%2FP162" target="_blank" >GP305/07/P162: Vztah mezi strukturou reaktivátorů acetylcholinesterázy a jejich reaktivační účinností</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2010

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

2010

Číslo periodika v rámci svazku

187

Stát vydavatele periodika

IE - Irsko

Počet stran výsledku

4

Strana od-do

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Kód UT WoS článku

000281108600052

EID výsledku v databázi Scopus

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