N2-acetylphenelzine: effects on rat brain GABA, alanine and biogenic amines

Naunyn Schmiedebergs Arch Pharmacol. 1991 May;343(5):478-82. doi: 10.1007/BF00169549.


The neurochemical properties of N2-acetylphenelzine were compared with those of phenelzine in a rat model. N2-Acetylphenelzine is a relatively potent inhibitor of monoamine oxidase-A and -B and causes increases in whole-brain levels of noradrenaline and 5-hydroxytryptamine, and decreases in homovanillic acid, 5-hydroxyindole-3-acetic acid, and 3,4-dihydroxyphenylacetic acetic after acute i.p. administration of the drug. Phenelzine is a more potent monoamine oxidase inhibitor than is N2-acetylphenelzine. The most marked difference in the profile was that N2-acetylphenelzine had no effect on whole brain levels of the amino acid neurotransmitters alanine and gamma-aminobutyric acid, whereas phenelzine caused dramatic increases. Acetylation of phenelzine at the N2 position presumably interferes with the inhibition of the transaminase enzymes for gamma-aminobutyric acid and alanine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine / analysis*
  • Animals
  • Biogenic Amines / analysis*
  • Brain Chemistry / drug effects*
  • In Vitro Techniques
  • Male
  • Monoamine Oxidase / analysis
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Phenelzine / analogs & derivatives*
  • Phenelzine / pharmacology
  • Rats
  • Rats, Inbred Strains
  • gamma-Aminobutyric Acid / analysis*


  • Biogenic Amines
  • Monoamine Oxidase Inhibitors
  • gamma-Aminobutyric Acid
  • N-acetylphenelzine
  • Monoamine Oxidase
  • Phenelzine
  • Alanine