Authors: K. Musílek 1; K. Kuča 2; D. Jun 2; Dohnal V.. 3; Kim T-H. 4; Jung Y-S. 4; M. Doležal 1 Authors‘ workplace: Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové, Katedra farmaceutické chemie a kontroly léčiv 1; Fakulta vojenského zdravotnictví Univerzity obrany Hradec Králové, Katedra toxikologie 2; Mendelova zemědělská a lesnická univerzita Brno, Ústav technologie potravin 3; Medicinal Science Division, Korea Research Institute of Chemical Technology, P. O. Box 107, Yusong, Taejon 4; -606, Korea 05 Published in: Čes. slov. Farm., 2006; 55, 115-119 Category: Original Articles
Insecticides (e.g., parathion, chlorpyrifos, methylchlorpyrifos) and nerve agents (e.g., soman, sarin, tabun, VX) belong to the group of organophosphates. They are able to irreversibly inhibit the enzyme acetylcholinesterase (AChE). Three new reactivators with a 3-oxapentane connecting chain were prepared. The ability of the new compounds to reactivate AChE inhibited by pesticides was tested in vitro and compared to known oximes (pralidoxime, methoxime, trimedoxime, obidoxime, HI-6). The results show that the new substances are superior to known reactivators in the case of methylchlorpyrifos-inhibited AChE at a concentration of 10⁻³ M which is unfortunately not applicable to in vivo experiments. All tested compounds are practically ineffective for methylchlorpyrifos-inhibited AChE at the physiological concentration (10⁻⁵ M). On the other hand, the known reactivators surpass new substances in the case of chlorpyrifos-inhibited AChE at both concentrations.
Key words: organophosphate – pesticide – acetylcholinesterase – reactivation – in vitro
Don‘t have an account? Create new account
Enter the email address that you registered with. We will send you instructions on how to set a new password.
