Potency of Five Structurally Different Acetylcholinesterase Reactivators to Reactivate Human Brain Cholinesterases Inhibited by Cyclosarin

Abstract

Acetylcholinesterase (AChE; EC 3.1.1.7) reactivators are used as a part of the antidotal therapy of organophosphorus pesticide and nerve agent intoxications. Cyclosarin is one member of the nerve agent family. In this article, we compared the reactivation potency of five structurally different AChE reactivators (pralidoxime, trimedoxime, methoxime, HS-6, and BI-6) to reactivate cyclosarin-inhibited cholinesterases of human brain. The results demonstrate that the bisquaternary monooxime reactivator BI-6 seems to be the most potent reactivator of cyclosarin-inhibited cholinesterases. Moreover, according to the results, we can describe basic structural requirements, which are necessary for the efficacious reactivation process.

Keywords :

• Cholinesterase
• Reactivators
• Cyclosarin
• Nerve agent
• Oxime