Inhibition of human benzylamine oxidase (BzAO) by analogues of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)

Toxicol Lett. 1990 Dec;54(2-3):135-42. doi: 10.1016/0378-4274(90)90176-m.

Abstract

A sensitive assay for human plasma BzAO, involving the conversion of 14C-benzylamine to 14C-benzaldehyde, was developed. MPTP and several of its analogues were found to be competitive inhibitors of the enzyme. Ki values for the MPTP analogues in the presence of human plasma BzAO were determined. The analogues had a different rank order of inhibition of human plasma BzAO compared with the rank order of inhibition of bovine plasma BzAO found previously. MPTP and 1-methyl-4-(2-methylphenyl)-1,2,3,6-tetrahydropyridine (2'-CH3-MPTP), which are potent nigrostriatal toxins, were weak inhibitors of human plasma BzAO.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / analogs & derivatives*
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine / pharmacology*
  • Benzylamine Oxidase / antagonists & inhibitors*
  • Benzylamine Oxidase / blood
  • Carbidopa / pharmacology
  • Dopamine Agents / pharmacology*
  • Humans
  • Kinetics
  • Parkinson Disease / blood
  • Parkinson Disease / enzymology*
  • Selegiline / pharmacology

Substances

  • Dopamine Agents
  • 1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine
  • Selegiline
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine
  • Benzylamine Oxidase
  • Carbidopa