In vitro Screening of Oxime Reactivators on the Model of Paraoxon-inhibited Acetylcholinesterase-SAR Study

Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10...

Full description

Saved in:
Bibliographic Details
Published inBulletin of the Korean Chemical Society Vol. 31; no. 6; pp. 1609 - 1614
Main Authors Holas, Ondrej, Musilek, Kamil, Pohanka, Miroslav, Kuca, Kamil, Opletalova, Veronika, Jung, Young-Sik
Format Journal Article
LanguageKorean
Published 2010
Subjects
Pesticide
Reactivator
Acetylcholinesterase
Structural requirements
Online AccessGet full text

Cover

More Information
Summary:Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10 ${\mu}M$). Results were compared to established reactivators pralidoxime, methoxime, HI-6, trimedoxime and obidoxime. More than 30 novel reactivators performed equal or better reactivation ability of POX-inhibited AChE compared to currently used reactivators. The structure-activity relationship for reactivators of paraoxon-inhibited AChE was developed.
Bibliography:KISTI1.1003/JNL.JAKO201018037269879
ISSN:0253-2964
1229-5949