[Anticholinesterase properties of benzo(f)quinolinium derivatives].
"In vitro" studies have demonstrated that methyl-p-toluene sulfonates of 1-methyl-(ethyl)-3-aryl-benzo(f)quinolinium are highly efficient inhibitors of cholinesterases, the inhibition constants (Ki) for acetylcholinesterase and butyrylcholinesterase being equal to 2.20 +/- 0.49 and 9.43 +/- 0.39 mkM, respectively. The effect of these inhibitors on the enzyme is of competitive - non-competitive type. A certain role in benzo(f)quinoline binding to acetylcholinesterase apparently belongs to the interaction of substituents in the phenyl nucleus with the anionic sites located outside the active surface of the enzyme.
D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D002802:Cholinesterases; D006801:Humans; D007700:Kinetics; D011806:Quinolinium Compounds / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D011806:Quinolinium Compounds; D002802:Cholinesterases
Antikholinésteraznye svoĭstva proizvodnykh benzo[f]khinoliniia.