Effect of the new selective COMT inhibitor CGP 28014 A on the formation of 3-O-methyldopa (3OMD) in plasma of healthy subjects

J Neural Transm Suppl. 1990;32:387-91. doi: 10.1007/978-3-7091-9113-2_53.

Abstract

CGP 28014 A is a specific inhibitor of catechol-O-methyl transferase (COMT). The effect on COMT was assessed with the levodopa test in 5 unmedicated subjects and after pretreatment with 200-600 mg CGP 28014 p.o. Plasma concentrations of DOPA, 3-O-methyldopa (3OMD), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid were measured. CGP 28014 A decreased 3OMD not dose-related by 67% (p less than 0.05). This, and an increase of DOPAC shows COMT inhibition by this compound in humans.

MeSH terms

  • 3,4-Dihydroxyphenylacetic Acid / metabolism
  • Amidines / pharmacology*
  • Catechol O-Methyltransferase Inhibitors*
  • Dihydroxyphenylalanine / metabolism
  • Homovanillic Acid / metabolism
  • Humans
  • Male
  • Pyridones / pharmacology*
  • Tyrosine / analogs & derivatives*
  • Tyrosine / biosynthesis
  • Tyrosine / blood
  • Tyrosine / pharmacokinetics

Substances

  • Amidines
  • Catechol O-Methyltransferase Inhibitors
  • Pyridones
  • 3,4-Dihydroxyphenylacetic Acid
  • N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine
  • Tyrosine
  • Dihydroxyphenylalanine
  • 3-methoxytyrosine
  • Homovanillic Acid