Reactivation potency of new group of acetylcholinesterase reactivators and their comparison with currently available oximes

Acta Medica (Hradec Kralove). 2006;49(4):233-5. doi: 10.14712/18059694.2017.138.

Abstract

In this work, in vitro potency of novel serie of monoquaternary pyridinium oximes to reactivate cyclosarin-inhibited acetylcholinesterase (AChE) was tested. Currently available oximes (pralidoxime, obidoxime, trimedoxime, HI-6 and BI-6) were used as oximes for comparison. As resulted, none of tested new reactivators was able to reactivate AChE inhibited by cyclosarin. Also pralidoxime, obidoxime and trimedoxime did not reach good reactivation results. Only oximes HI-6 and BI-6 achieved sufficient reactivation potency. From obtained results, it can be deduced, that only reactivators with oxime group in position two are able to reactivate cyclosarin-inhibited AChE.

Publication types

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

MeSH terms

  • Acetylcholinesterase / metabolism*
  • Animals
  • Brain / drug effects*
  • Brain / metabolism
  • Cholinesterase Inhibitors / pharmacology*
  • Cholinesterase Reactivators / chemistry
  • Cholinesterase Reactivators / pharmacology*
  • In Vitro Techniques
  • Organophosphorus Compounds / pharmacology
  • Oximes / chemistry
  • Oximes / pharmacology*
  • Rats

Substances

  • Cholinesterase Inhibitors
  • Cholinesterase Reactivators
  • Organophosphorus Compounds
  • Oximes
  • Acetylcholinesterase
  • cyclohexyl methylphosphonofluoridate