Tissue levels and some pharmacological properties of an acetylated metabolite of phenelzine in the rat

J Pharm Sci. 1991 Aug;80(8):765-7. doi: 10.1002/jps.2600800812.


The metabolic generation of N2-acetylphenelzine by rats treated with phenelzine, and the activity of this metabolite as an inhibitor of monoamine oxidase enzymes in vivo were confirmed. The isomeric amide N1-acetylphenelzine was not a metabolic product of phenelzine and also did not inhibit monoamine oxidase enzymes. Levels of N2-acetylphenelzine in rat blood, after treatment with a dose (0.1 mmol.kg-1) of N2-acetylphenelzine sufficient to inhibit monoamine oxidase enzymes but not to increase brain levels of dopamine or noradrenaline, were higher than those generated metabolically from a higher dose (0.38 mmol.kg-1) of phenelzine which did increase brain levels of these biogenic amines. Metabolically derived N2-acetylphenelzine, therefore, probably does not contribute in any significant way to monoamine oxidase inhibition by phenelzine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation
  • Animals
  • Biogenic Amines / metabolism
  • Brain / drug effects
  • Brain / enzymology
  • Brain / metabolism
  • Chromatography, Gas
  • Dealkylation
  • Injections, Intraperitoneal
  • Liver / metabolism
  • Male
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / pharmacology
  • Phenelzine / analogs & derivatives*
  • Phenelzine / metabolism*
  • Phenelzine / pharmacokinetics
  • Phenelzine / pharmacology
  • Rats
  • Rats, Inbred Strains


  • Biogenic Amines
  • Monoamine Oxidase Inhibitors
  • N-acetylphenelzine
  • Monoamine Oxidase
  • Phenelzine