Russian VX: inhibition and reactivation of acetylcholinesterase compared with VX agent

Basic & Clinical Pharmacology & Toxicology
K KucaVeronika Opletalova

Abstract

Organophosphorus compounds such as nerve agents inhibit, practically irreversibly, cholinesterases by their phosphorylation in the active site of these enzymes. Current antidotal treatment used in the case of acute nerve agent intoxications consists of combined administration of anticholinergic drug (usually atropine) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivator (HI-6, obidoxime, pralidoxime), which from a chemical view is a derivative from the group of pyridinium or bispyridinium aldoximes (commonly called "oxime"). Oximes counteract acetylcholine increase, resulting from AChE inhibition. In the human body environment these compounds are powerful nucleophiles and are able to break down the bond between AChE and nerve agent molecule. This process leads to renewal of enzyme functionality -- to its reactivation. The usefulness of oxime in the reactivation process depends on its chemical structure and on the nerve agent whereby AChE is inhibited. Due to this fact, selection of suitable reactivator in the treatment of intoxications is very important. In our work, we have compared differences in the in vitro inhibition potency of VX and Russian VX on rat, pig and human brain, and subsequently we have tested reactivation o...Continue Reading

References

Jan 1, 1996·Archives of Toxicology·H P van HeldenP L Bruijnzeel
Jul 30, 1997·European Journal of Pharmacology·G CasselA Göransson-Nyberg
Dec 12, 2002·Journal of Toxicology. Clinical Toxicology·J Kassa
Aug 27, 2003·Neurochemical Research·Koichi SakuradaTakehiko Takatori
Sep 24, 2004·Basic & Clinical Pharmacology & Toxicology·Jirí CabalJ Kassa
Nov 20, 2004·Journal of Applied Toxicology : JAT·Georg A PetroianuWolfgang H Maleck
Dec 14, 2004·Toxicology·Lucie SevelováGabriela Krejcová-Kunesová
May 24, 2005·Bioorganic & Medicinal Chemistry Letters·Srinivas Rao ChennamaneniAchaiah Garlapati

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Citations

Aug 31, 2006·International Journal of Toxicology·Jiri KassaKamil Kuca
Apr 26, 2007·Clinical Medicine & Research·Biljana Antonijevic, Milos P Stojiljkovic
Jun 20, 2007·Basic & Clinical Pharmacology & Toxicology·Kamil KucaLucie Musilova
Sep 26, 2008·Basic & Clinical Pharmacology & Toxicology·Jaroslav PejchalJiri Kassa
Aug 7, 2013·Bioorganic & Medicinal Chemistry·Sibelle Feitosa da Cunha Xavier SoaresJosé Daniel Figueroa-Villar
Jan 17, 2015·Annales pharmaceutiques françaises·A-C CuquelP Burnat
Aug 3, 2017·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Keith Candiotti
Feb 15, 2007·Journal of Applied Toxicology : JAT·J BajgarV Blaha
Mar 17, 2020·ACS Omega·Felipe Rodrigues de SouzaTanos Celmar Costa França
Apr 26, 2020·Neuropharmacology·Zrinka Kovarik, Nikolina Maček Hrvat

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