TRISOXIME - a Bulky Trisquaternary Reactivator of Acetylcholinesterase

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61988987%3A17110%2F16%3AA1701LLI" target="_blank" >RIV/61988987:17110/16:A1701LLI - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00179906:_____/16:10323694 RIV/60162694:G44__/16:43875591 RIV/62690094:18470/16:50004679

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

TRISOXIME - a Bulky Trisquaternary Reactivator of Acetylcholinesterase

Popis výsledku v původním jazyce

Structure of acetylcholinesterase (AChE) reactivators influences their reactivation activity. Monoquaternary or bisquaternary reactivators are generally used for this purpose. In this work, there is discussed in vitro activity of trisquaternary AChE reactivator - Trisoxime (K388). Its reactivation activity is tested on the AChE inhibited by selected nerve agents - tabun, sarin, cyclosarin, soman, VX, Russian VX and diisopropyl fluorophosphates (DFP). As a result, only AChE inhibited by three nerve agents (VX, Russian VX and DFP) was satisfactorily reactivated at tested oxime concentrations (10(-5) M and 10(-3) M). This relatively poor reactivation potency was probably caused by the bulky spherical structure of tested oxime. Although results obtained in this study are not favorable, they are showing that the addition of one more quaternary ring to the reactivator's molecule is not the right way to improve its reactivation potency.

Název v anglickém jazyce

TRISOXIME - a Bulky Trisquaternary Reactivator of Acetylcholinesterase

Popis výsledku anglicky

Structure of acetylcholinesterase (AChE) reactivators influences their reactivation activity. Monoquaternary or bisquaternary reactivators are generally used for this purpose. In this work, there is discussed in vitro activity of trisquaternary AChE reactivator - Trisoxime (K388). Its reactivation activity is tested on the AChE inhibited by selected nerve agents - tabun, sarin, cyclosarin, soman, VX, Russian VX and diisopropyl fluorophosphates (DFP). As a result, only AChE inhibited by three nerve agents (VX, Russian VX and DFP) was satisfactorily reactivated at tested oxime concentrations (10(-5) M and 10(-3) M). This relatively poor reactivation potency was probably caused by the bulky spherical structure of tested oxime. Although results obtained in this study are not favorable, they are showing that the addition of one more quaternary ring to the reactivator's molecule is not the right way to improve its reactivation potency.

Druh

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

CEP obor

FH - Neurologie, neurochirurgie, neurovědy

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

V - Vyzkumna aktivita podporovana z jinych verejnych zdroju

Rok uplatnění

2016

Kód důvěrnosti údajů

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

Název periodika

LETTERS IN DRUG DESIGN & DISCOVERY

ISSN

1570-1808

e-ISSN

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Svazek periodika

13

Číslo periodika v rámci svazku

5

Stát vydavatele periodika

AE - Spojené arabské emiráty

Počet stran výsledku

4

Strana od-do

372-375

Kód UT WoS článku

000374883700003

EID výsledku v databázi Scopus

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