title: [The mechanism of anticholinesterase action of acetylene organophosphorus inhibitors].
abstract: Introduction of the triple bond in the leaving group of the organophosphorus inhibitor molecule gives a sharp raise of the inhibitor activity but does not change principal characteristics of the cholinesterase inhibition mechanism. The reactivation experiments suggest that inactivation of cholinesterases by these compounds occurs due to phosphorylating of the serine hydroxyl by the corresponding phosphoric acid. A close similarity was shown between acetylenic and saturated organophosphorus inhibitors in altering ka upon change of pH and tetraalkylammonium ions action. It is demonstrated that S-alkynyl esters of thioacetic acid are slowly hydrolyzed by acetylcholinesterase and cholinesterase without irreversible inhibition of the enzymes.
authors.forename: A P
authors.initials: AP
authors.lastname: Brestkin
authors.forename: Iu G
authors.initials: IuG
authors.lastname: Zhukovskiĭ
authors.forename: S N
authors.initials: SN
authors.lastname: Moralev
authors.forename: V I
authors.initials: VI
authors.lastname: Rozengart
authors.forename: E E
authors.initials: EE
authors.lastname: Sochilina
authors.forename: O V
authors.initials: OV
authors.lastname: Iagodina
authors.forename: L A
authors.initials: LA
authors.lastname: Vikhreva
authors.forename: N N
authors.initials: NN
authors.lastname: Godovikov
authors.forename: M I
authors.initials: MI
authors.lastname: Kabachnik
mesh_terms: D000114:Acetylene / Q000633:toxicity*; D002800:Cholinesterase Inhibitors / Q000633:toxicity*; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007700:Kinetics; D009943:Organophosphorus Compounds / Q000633:toxicity*; D010766:Phosphorylation
chemical_list: D002800:Cholinesterase Inhibitors; D009943:Organophosphorus Compounds; D000114:Acetylene
vernacular_title: O mekhanizme antikholinésteraznogo deĭstviia atsetilenovykh fosforororganicheskikh ingibitorov.