Protective action of series of new mono-pyridinium salts and their effect on "aging" of acetylcholine esterase inhibited by fluostigmine.
The protection of acetylcholine esterase (AChE) and the influence on "aging" of AChE--inhibitor complex of several new methylpyridinium derivatives was studied in human blood cells and in mice poisoned with diisopropyl phosphorofluoridate (fluostigmine, DFP). A correlation between the chemical structure of the compounds and their biological activity has been found. The most potent was compound PAN-W-24, having 4-N(CH3)3 substitutent, which markedly prolonged the half-life of "aging" of the AChE-fluostigmine complex.
D000110:Acetylcholinesterase / Q000378:metabolism*; D002800:Cholinesterase Inhibitors; D004912:Erythrocytes / Q000201:enzymology; D006207:Half-Life; D006801:Humans; D066298:In Vitro Techniques; D007531:Isoflurophate / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D007928:Lethal Dose 50; D011726:Pyridinium Compounds / Q000494:pharmacology*; D013997:Time Factors
D002800:Cholinesterase Inhibitors; D011726:Pyridinium Compounds; D007531:Isoflurophate; D000110:Acetylcholinesterase