Selective inactivation of MAO-B by benzyl-dimethyl-silyl-methanamines in vitro

Biochem Biophys Res Commun. 1989 Apr 28;160(2):540-4. doi: 10.1016/0006-291x(89)92466-2.

Abstract

The alpha-silyl amines benzyl-dimethyl-silyl-methanamine and the p-fluoro and p-chloro derivatives are potent time-dependent inhibitors of rat brain MAO-B. The inhibition exhibits saturation kinetics, takes place in the enzyme active-site and is irreversible. The most potent inhibitor in the series is 4-fluorobenzyl-dimethyl-silyl-methanamine (KI = 11 microM, tau 1/2 = 2.3 min). Its selectivity for the B-form relative to the A-form of rat brain MAO is higher than 10(4). Benzyl-dimethyl-silyl-methanamines may represent a new family of anti-Parkinsonian agents.

MeSH terms

  • Animals
  • Benzylamines / pharmacology
  • Brain / drug effects
  • Brain / enzymology
  • Enzyme Activation / drug effects
  • Kinetics
  • Methylamines / pharmacology*
  • Monoamine Oxidase / metabolism*
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Rats
  • Silicon / pharmacology*
  • Substrate Specificity

Substances

  • Benzylamines
  • Methylamines
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase
  • Silicon