title: Reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro.
abstract: We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a toxic metabolite of the pesticide leptophos. Compounds were assayed in concentrations of 10 and 100 μM. In case of leptophos-oxon inhibited AChE, the best reactivation potency was achieved with methoxime, trimedoxime, obidoxime and oxime K027. The most potent reactivators of inhibited BChE were K033, obidoxime, K117, bis-3-PA, K075, K074 and K127. The reactivation efficacy of tested oximes was lower in case of leptophos-oxon inhibited BChE.
authors.affiliation: Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.
authors.forename: Daniel
authors.initials: D
authors.lastname: Jun
authors.forename: Lucie
authors.initials: L
authors.lastname: Musilova
authors.forename: Miroslav
authors.initials: M
authors.lastname: Pohanka
authors.forename: Young-Sik
authors.initials: YS
authors.lastname: Jung
authors.forename: Pavel
authors.initials: P
authors.lastname: Bostik
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuca
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry*; D002091:Butyrylcholinesterase / Q000737:chemistry*; D004912:Erythrocytes / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D010773:Leptophos / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010091:Oximes / Q000737:chemistry*; D010575:Pesticides / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D010091:Oximes; D010575:Pesticides; C008265:leptophos oxon; D010773:Leptophos; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase