title: Evaluation of potency of known oximes (pralidoxime, trimedoxime, HI-6, methoxime, obidoxime) to in vitro reactivate acetylcholinesterase inhibited by pesticides (chlorpyrifos and methylchlorpyrifos) and nerve agent (Russian VX).
abstract: Nerve agents and pesticides belong to the group of organophosphates. They are able to inhibit irreversibly the enzyme acetylcholinesterase (AChE). Acetylcholinesterase reactivators were designed for the treatment of nerve agent intoxications. Their potency to reactivate pesticide-inhibited AChE was many times evaluated. In this study, five commonly used AChE reactivators (pralidoxime, methoxime, HI-6, obidoxime, trimedoxime) for the reactivation of AChE inhibited by two pesticides (chlorpyrifos and methylchlorpyrifos) were used. Russian VX (nerve agent) as a member of nerve agents' family was taken for comparison. Obtained results show that oximes developed against nerve agent intoxication are less effective for intoxication with organophosphorus pesticides. Especially, methylchlorpyrifos-inhibited AChE was found to be poorly reactivated by the compounds used.
authors.affiliation: University of Defence, Faculty of Military Health Sciences, Department of Toxicology, Hradec Králové, Czech Republic.
authors.forename: Kamil
authors.initials: K
authors.lastname: Musílek
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuca
authors.forename: Daniel
authors.initials: D
authors.lastname: Jun
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000201:enzymology; D002619:Chemical Warfare Agents / Q000494:pharmacology; D004390:Chlorpyrifos / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D002801:Cholinesterase Reactivators / Q000494:pharmacology*; D066298:In Vitro Techniques; D007306:Insecticides / Q000494:pharmacology*; D009946:Organothiophosphorus Compounds / Q000494:pharmacology*; D010091:Oximes / Q000494:pharmacology*; D051381:Rats
chemical_list: D002619:Chemical Warfare Agents; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D007306:Insecticides; D009946:Organothiophosphorus Compounds; D010091:Oximes; D000110:Acetylcholinesterase; D004390:Chlorpyrifos; C451779:S-(N,N-diethylaminoethyl) isobutyl methylphosphothiolate