Reactivators, from classic to a new generation

摘要

The creating of the reactivators of cholinesterase (ChE) activity is an example for a direct synthesis of biochemical antidotes. The major oximes such as 2PAM, 2PAS, TMB-4 and toxogonin are being applied on a wide range and have been examined in detail. The difficulty in reactivation of the ChE actvity and slight antidote effect concerning intoxication with some organophosphorus compounds (OPC), are some of the reasons for continuing the examinations for the creation of new reactivators of ChE. The creation of the so called "H" oximes gives a new stimulus in this direction. During the evaluation of the new compounds in addition to the antidotal effects and the reactivating effect according to the inhibition of ChE by different OPC, we should examine the recovery of the blocked neuromuscular transmission, the cholinergic receptor functions, the anticonvulsive activity after intoxication with OPC. We consider the importance of the evaluation of pharmacokinetics of the reactivators as well as changes on background of intoxications with different kinds of OPC, as well as of the toxicokinetics of OPC after treatment. It is important that before the synthesis of some new compounds, to examine the QSAR not only considering the reactivation of ChE, but also having in mind their ability to reverse neuromuscular blockade.