In vitro reactivation of tabun-inhibited acetylcholinesterase using new oximes--K027, K005, K033 and K048

Cent Eur J Public Health. 2004 Mar:12 Suppl:S59-61.

Abstract

Four new AChE oximes for reactivation of acetylcholinesterase inhibited with tabun - K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium) propane dibromide], K005 [1,3-bis(2-hydroxyiminomethylpyridinium) propane dibromide], K033 [1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide] and K048 [1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium) butane dibromide] were prepared. Their efficacies to reactivate tabun-inhibited acetylcholinesterase were studied and compared with the currently used acetylcholinesterase reactivators (pralidoxime, obidoxime and HI-6). Reactivator K048 seems to be promising reactivator of tabun-inhibited AChE. Its reactivation potency is significantly higher than the efficacy of HI-6 and pralidoxime, and comparable with the potency of the obidoxime at human relevant doses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / enzymology
  • Cholinesterase Inhibitors / toxicity*
  • Cholinesterase Reactivators / chemical synthesis
  • Cholinesterase Reactivators / pharmacology*
  • In Vitro Techniques
  • Organophosphates / toxicity*
  • Oximes / chemical synthesis
  • Oximes / pharmacology*
  • Oximes / toxicity
  • Pyridinium Compounds / chemical synthesis
  • Pyridinium Compounds / pharmacology*
  • Pyridinium Compounds / toxicity
  • Rats

Substances

  • 1,3-bis(2-hydroxyiminomethylpyridinium)propane
  • 1,4-bis(2-hydroxyiminomethylpyridinium)butane
  • 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Organophosphates
  • Oximes
  • Pyridinium Compounds
  • tabun