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

Bulletin of the Korean chemical society

Young Sik Jung¹  Ondrej Holas¹  Veronika Opletalova¹  Kamil Musilek Miroslav Pohanka¹  Kamil Kuca¹ 

关键词: Acetylcholinesterase;    Pesticide;    Reactivator;    Structural requirements;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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 レM and 10 レ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.

【 授权许可】

Unknown