Schopnost nových strukturně odlišných oximů reaktivovat cyclosarinem inhibovanou acetylcholinesterázu z lidského mozku

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F06%3A00001490" target="_blank" >RIV/60162694:G44__/06:00001490 - isvavai.cz</a>

Výsledek na webu

—

DOI - Digital Object Identifier

—

Jazyk výsledku

angličtina

Název v původním jazyce

Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases

Popis výsledku v původním jazyce

Antidotes currently used in the case of organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these compounds worldwide, development of antidotes for the case of the first aid is needed. To select the most promising AChE reactivators is very time consuming process, which is necessary before approval of these compounds to be used as human antidotes. Becauseof ethical reasons, many developing experiments have been conducted on laboratory animals. However, these results could not be often transferred directly to human. Due to this fact, in our work, we have tested five newly developed AChE reactivators # K027, K033, K048, K074 and K075, which achieved promising reactivation activity on rodents, as reactivators of human brain cholinesterases. For this purpose, cyclosarin was used as member of the nerve agent family. H-oxime HI-6 and pralidoxi

Název v anglickém jazyce

Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases

Popis výsledku anglicky

Antidotes currently used in the case of organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these compounds worldwide, development of antidotes for the case of the first aid is needed. To select the most promising AChE reactivators is very time consuming process, which is necessary before approval of these compounds to be used as human antidotes. Becauseof ethical reasons, many developing experiments have been conducted on laboratory animals. However, these results could not be often transferred directly to human. Due to this fact, in our work, we have tested five newly developed AChE reactivators # K027, K033, K048, K074 and K075, which achieved promising reactivation activity on rodents, as reactivators of human brain cholinesterases. For this purpose, cyclosarin was used as member of the nerve agent family. H-oxime HI-6 and pralidoxi

Druh

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

CEP obor

FP - Ostatní lékařské obory

OECD FORD obor

—

Projekt

—

Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2006

Kód důvěrnosti údajů

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

Název periodika

Journal of Enzyme Inhibition and Medicinal Chemistry

ISSN

1475-6366

e-ISSN

—

Svazek periodika

—

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

4

Strana od-do

663-666

Kód UT WoS článku

—

EID výsledku v databázi Scopus

—