title: Interaction of pyridinium oximes with acetylcholinesterase and their effect on organophosphate-poisoned mice.
abstract: The progressive inhibition of acetylcholinesterase (AChE [EC 3.1.1.7]) by organophosphates (OPs), such as the nerve agents tabun and soman, is due to phosphorylation of the active center serine characterized by the formation of conjugates and inactivation of this essential enzyme involved in neurotransmission. Presently, a combination of an antimuscarinic agent, e.g., atropine, and an AChE reactivator, oxime, is used for the treatment of organophosphorus compound poisoning. The increased concern about terrorist use of nerve agents prompted us to search for new, more effective oximes against tabun and soman poisoning. We investigated the interactions of five bispyridinium oximes with human erythrocyte AChE and their effects on tabun- and soman-poisoned mice.
authors.affiliation: Institute for Medical Research and Occupational Health, POB 291, HR-10001 Zagreb, Croatia. zkovarik@imi.hr
authors.forename: Zrinka
authors.initials: Z
authors.lastname: Kovarik
authors.forename: Maja
authors.initials: M
authors.lastname: Calić
authors.forename: Ana Lucić
authors.initials: AL
authors.lastname: Vrdoljak
authors.forename: Bozica
authors.initials: B
authors.lastname: Radić
mesh_terms: D000110:Acetylcholinesterase / Q000097:blood / Q000378:metabolism*; D000818:Animals; D000931:Antidotes / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000633:toxicity; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D051379:Mice; D010755:Organophosphates / Q000633:toxicity*; D010091:Oximes / Q000494:pharmacology*; D011726:Pyridinium Compounds / Q000494:pharmacology*; D012999:Soman / Q000633:toxicity
chemical_list: D000931:Antidotes; D002800:Cholinesterase Inhibitors; D010755:Organophosphates; D010091:Oximes; D011726:Pyridinium Compounds; D012999:Soman; D000110:Acetylcholinesterase; C009374:tabun