The reactivators of acetylcholinesterase (AChE, EC 184.108.40.206) are very important components in the treatment of intoxications caused by organophosphate inhibitors such as nerve agents and pesticides. These inhibitors covalently bind to active site of mentioned enzyme and irreversibly inhibit its activity. The reactivator breaks the inhibitor-enzyme covalent bond and restores its activity. Unfortunately, there is no reactivator applicable for every type of inhibitor; it means that every structural change in the molecule of inhibitor needs a specific structure of the reactivator. K 203 ((E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide) was selectively developed for tabun intoxication of AChE. Its properties exceeded all commercial reactivators in tabun poisoning with valuable activity/toxicity profile.
The work was supported by the Grant Agency of Ministry of Education, Youth and Sports (Czech Republic) – grant no. ME865.