In vitro reactivation of acetylcholinesterase using the oxime K027

Vet Hum Toxicol. 2004 Feb;46(1):15-8.

Abstract

The ability of a new bisquaternary oxime, K027 (1-[4-hydroxyiminomethylpyridinium]-3-[carbamoylpyridinium] propane dibromide), to reactivate the enzyme acetylcholinesterase (AChE) inhibited by the nerve agents Tabun, sarin and VX was evaluated. Its reactivation potency was compared to the AChE reactivators pralidoxime (2-PAM), obidoxime and HI-6; K027 seems a good reactivator of organophosphates-inhibited AChE. Its reactivation potency is lower compared to the other oximes for reactivation of sarin-inhibited AChE, but it is sufficient to significantly increase the activity of sarin-inhibited AChE. Its reactivation ability is comparable to obidoxime for reactivation of VX- and tabun-inhibited AChE and is higher than the reactivation potency of HI-6, for tabun-inhibited AChE. HI-6 is currently regarded the most promising reactivator of organophosphates-inhibited AChE.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / chemistry*
  • Animals
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators / chemistry*
  • Dose-Response Relationship, Drug
  • Obidoxime Chloride / chemistry
  • Organophosphates
  • Organothiophosphorus Compounds
  • Oximes / chemistry*
  • Pralidoxime Compounds / chemistry
  • Pyridinium Compounds / chemistry
  • Sarin
  • Structure-Activity Relationship

Substances

  • 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Organophosphates
  • Organothiophosphorus Compounds
  • Oximes
  • Pralidoxime Compounds
  • Pyridinium Compounds
  • Obidoxime Chloride
  • VX
  • Sarin
  • Acetylcholinesterase
  • asoxime chloride
  • pralidoxime
  • tabun