Reactivation of VX-inhibited AChE by novel oximes having two oxygen atoms in the linker

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F10%3A00002353" target="_blank" >RIV/60162694:G44__/10:00002353 - 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

Reactivation of VX-inhibited AChE by novel oximes having two oxygen atoms in the linker

Popis výsledku v původním jazyce

Two newly developed AChE reactivators possessing two oxime groups in 4-position of the pyridinium rings with linkers CH2O(CH2)(2)OCH2 and CH2O(CH2)(4)OCH2 were tested for their potency to reactivate VX-inhibited AChE. Their reactivation potency was compared with currently available oximes such as pralidoxime, obidoxime and HI-6. Appropriate constants (affinity towards the intact and inhibited enzyme, reactivation rate) characterizing the reactivation process were determined. According to the data obtained, a new oxime with CH2O(CH2)(2)OCH2 linker reached as high reactivation potency as HI-6. The percentage of reactivation of the oxime with CH2O(CH2)(2)OCH2 linker was comparable to that of obidoxime at a concentration 10 M. Hence, these oximes may be worthy of future development for the treatment of nerve agent intoxications, especially, with lipophilic agents such as soman and cyclosarin.

Název v anglickém jazyce

Reactivation of VX-inhibited AChE by novel oximes having two oxygen atoms in the linker

Popis výsledku anglicky

Two newly developed AChE reactivators possessing two oxime groups in 4-position of the pyridinium rings with linkers CH2O(CH2)(2)OCH2 and CH2O(CH2)(4)OCH2 were tested for their potency to reactivate VX-inhibited AChE. Their reactivation potency was compared with currently available oximes such as pralidoxime, obidoxime and HI-6. Appropriate constants (affinity towards the intact and inhibited enzyme, reactivation rate) characterizing the reactivation process were determined. According to the data obtained, a new oxime with CH2O(CH2)(2)OCH2 linker reached as high reactivation potency as HI-6. The percentage of reactivation of the oxime with CH2O(CH2)(2)OCH2 linker was comparable to that of obidoxime at a concentration 10 M. Hence, these oximes may be worthy of future development for the treatment of nerve agent intoxications, especially, with lipophilic agents such as soman and cyclosarin.

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/OVUOFVZ200801" target="_blank" >OVUOFVZ200801: REAKTIVÁTOR - Robotizovaný systém in vitro evaluace potenciálních reaktivátorů nervově paralytickými látkami inhibované acetylcholinestrázy</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

Environmental Toxicology and Pharmacology

ISSN

1382-6689

e-ISSN

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Svazek periodika

30

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

3

Strana od-do

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Kód UT WoS článku

000279089000014

EID výsledku v databázi Scopus

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