[Anticholinesterase properties of benzo(f)quinolinium derivatives]

Biokhimiia. 1981 Oct;46(10):1764-7.
[Article in Russian]

Abstract

"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.

Publication types

  • English Abstract

MeSH terms

  • Cholinesterase Inhibitors* / pharmacology*
  • Cholinesterases
  • Humans
  • Kinetics
  • Quinolinium Compounds / pharmacology*
  • Structure-Activity Relationship

Substances

  • Cholinesterase Inhibitors
  • Quinolinium Compounds
  • Cholinesterases