Effective bisquaternary reactivators of tabun-inhibited AChE

J Appl Toxicol. 2005 Nov-Dec;25(6):491-5. doi: 10.1002/jat.1084.

Abstract

Two cholinesterase reactivators (K074 and K075) were synthesized and their reactivation efficacy against tabun-inhibited acetylcholinesterase of the rat brain was tested in vitro. Comparing this efficacy showed that commonly used oximes (pralidoxim, obidoxime and HI-6) were practically without reactivation potency. On the other hand, oximes K074, K075 and trimedoxime were satisfactorily effective. Moreover, K-oximes reactivated tabun-inhibited AChE at lower concentration (10(-4) and 10(-3) m) in comparison with trimedoxime (10(-3) and 10(-2) m). Thus, K-oximes can be considered as the most effective reactivators of tabun-inhibited AChE at present.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / chemistry
  • Acetylcholinesterase / metabolism*
  • Animals
  • Brain / drug effects
  • Brain / enzymology
  • Butanes / chemistry
  • Butanes / pharmacology
  • Cholinesterase Inhibitors / toxicity*
  • Cholinesterase Reactivators / chemical synthesis
  • Cholinesterase Reactivators / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • In Vitro Techniques
  • Kinetics
  • Organophosphates / toxicity*
  • Oximes / chemical synthesis
  • Oximes / pharmacology*
  • Pyridinium Compounds
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship

Substances

  • 1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide
  • Butanes
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Organophosphates
  • Oximes
  • Pyridinium Compounds
  • Pyrimidines
  • Acetylcholinesterase
  • tabun