Currently Used Cholinesterase Reactivators Against Nerve Agent Intoxication: Comparison of Their Effectivity in Vitro

Abstract

In vitro comparison of reactivation efficacy of five currently used oximes—pralidoxime, obidoxime, trimedoxime, methoxime, and HI-6 (at two concentrations: 10⁻⁵ and 10⁻³ M)—against acetylcholinesterase (AChE; E.C. 3.1.1.7) inhibited by six different nerve agents (VX, Russian VX, sarin, cyclosarin, tabun, soman) and organophosphorus insecticide chlorpyrifos was the aim of this study. As a source of AChE in the experiments, rat brain homogenate was used. According to the results obtained, no AChE reactivator was able to reach sufficient potency for AChE inhibited by all nerve agents used. Moreover, oxime HI-6 (the most effective one) was not able to reactivate tabun- and soman-inhibited AChE. Due to this fact, it could be designated as a partially broad-spectrum reactivator.

Key Words: :

• Acetylcholinesterase
• Antidote
• Nerve agents
• Oxime
• Reactivation