In vitro potency of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate nerve agent-inhibited rat brain acetylcholinesterase

J Toxicol Environ Health A. 2006 Aug;69(15):1431-40. doi: 10.1080/15287390500364283.

Abstract

The efficacy of H oximes (HI-6, HLö-7), the oxime BI-6, and currently used oximes (pralidoxime, obidoxime, trimedoxime) to reactivate acetylcholinesterase inhibited by two nerve agents (tabun, VX agent) was tested in vitro. Both H oximes (HI-6, HLö-7) and the oxime BI-6 were found to be more efficacious reactivators of VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. On the other hand, their potency to reactivate tabun-inhibited acetylcholinesterase was low and did not reach the reactivating efficacy of trimedoxime and obidoxime. Thus, none of these compounds can be considered to be a broad-spectrum reactivator of nerve agent-inhibited acetylcholinesterase in spite of high potency to reactivate acetylcholinesterase inhibited by some nerve agents. More than one oxime may be necessary for the antidotal treatment of nerve agent-exposed individuals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / physiology*
  • Animals
  • Antidotes / pharmacology
  • Brain / drug effects*
  • Chemical Warfare Agents / pharmacology*
  • Cholinesterase Inhibitors / pharmacology
  • Cholinesterase Reactivators / pharmacology*
  • Male
  • Obidoxime Chloride / pharmacology
  • Organophosphates / pharmacology
  • Organothiophosphorus Compounds / pharmacology
  • Oximes / pharmacology*
  • Pralidoxime Compounds / pharmacology
  • Pyridines / pharmacology
  • Pyridinium Compounds / pharmacology
  • Rats
  • Rats, Wistar
  • Trimedoxime / pharmacology

Substances

  • Antidotes
  • BI 6
  • Chemical Warfare Agents
  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Organophosphates
  • Organothiophosphorus Compounds
  • Oximes
  • Pralidoxime Compounds
  • Pyridines
  • Pyridinium Compounds
  • HLo 7
  • Obidoxime Chloride
  • Trimedoxime
  • VX
  • Acetylcholinesterase
  • asoxime chloride
  • pralidoxime
  • tabun