Tetroxime: reactivation potency - in vitro and in silico study
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F17%3A10337258" target="_blank" >RIV/00179906:_____/17:10337258 - isvavai.cz</a>
Nalezeny alternativní kódy
RIV/60162694:G44__/17:43875727 RIV/62690094:18470/17:50005169
Výsledek na webu
<a href="http://dx.doi.org/10.1039/c6ra16499d" target="_blank" >http://dx.doi.org/10.1039/c6ra16499d</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c6ra16499d" target="_blank" >10.1039/c6ra16499d</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Tetroxime: reactivation potency - in vitro and in silico study
Popis výsledku v původním jazyce
Acetylcholinesterase (AChE) reactivators (oximes) are generally used as treatment in cases of nerve agent poisoning. There is no single oxime applicable in every case of nerve agent intoxication. Based on this fact, novel candidates with broader efficacy are still being sought. In this study, tetroxime a bisquaternary compound bearing four oxime groups, was evaluated for its potency to reactivate rat brain AChE inhibited by selected nerve agents (tabun, sarin, cyclosarin and VX agent). Despite the fact that this oxime contains four oxime groups that could be plausibly responsible for reactivation, it did not achieve broader reactivation activity. Satisfactory results were obtained only in the case of VX agent-inhibited AChE. In the cases of sarin-and cyclosarin-inhibited AChE, acceptable results were reached at higher oxime concentration only. Tetroxime was unable to reactivate tabun-inhibited AChE. However, compared with the gold standard pralidoxime, this oxime achieved more promising results.
Název v anglickém jazyce
Tetroxime: reactivation potency - in vitro and in silico study
Popis výsledku anglicky
Acetylcholinesterase (AChE) reactivators (oximes) are generally used as treatment in cases of nerve agent poisoning. There is no single oxime applicable in every case of nerve agent intoxication. Based on this fact, novel candidates with broader efficacy are still being sought. In this study, tetroxime a bisquaternary compound bearing four oxime groups, was evaluated for its potency to reactivate rat brain AChE inhibited by selected nerve agents (tabun, sarin, cyclosarin and VX agent). Despite the fact that this oxime contains four oxime groups that could be plausibly responsible for reactivation, it did not achieve broader reactivation activity. Satisfactory results were obtained only in the case of VX agent-inhibited AChE. In the cases of sarin-and cyclosarin-inhibited AChE, acceptable results were reached at higher oxime concentration only. Tetroxime was unable to reactivate tabun-inhibited AChE. However, compared with the gold standard pralidoxime, this oxime achieved more promising results.
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
30104 - Pharmacology and pharmacy
Návaznosti výsledku
Projekt
<a href="/cs/project/GA15-16701S" target="_blank" >GA15-16701S: Koncept nekvarterních reaktivátorů AChE jakožto antidot otrav organofosfáty - nová naděje či slepá cesta?</a><br>
Návaznosti
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Ostatní
Rok uplatnění
2017
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
RSC Advances
ISSN
2046-2069
e-ISSN
—
Svazek periodika
7
Číslo periodika v rámci svazku
12
Stát vydavatele periodika
GB - Spojené království Velké Británie a Severního Irska
Počet stran výsledku
5
Strana od-do
7041-7045
Kód UT WoS článku
000393756000030
EID výsledku v databázi Scopus
2-s2.0-85010450466