[The mechanism of anticholinesterase action of acetylene organophosphorus inhibitors]. / O mekhanizme antikholinésteraznogo deistviia atsetilenovykh fosforororganicheskikh ingibitorov.
Bioorg Khim
; 18(8): 1067-72, 1992 Aug.
Article
em Ru
| MEDLINE
| ID: mdl-1445434
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.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Organofosforados
/
Acetileno
/
Inibidores da Colinesterase
Limite:
Humans
Idioma:
Ru
Revista:
Bioorg Khim
Ano de publicação:
1992
Tipo de documento:
Article
País de publicação:
FEDERAÇÃO RUSSA
/
RU
/
RUSIA
/
RUSSIA