N2-acetylphenelzine: effects on rat brain GABA, alanine and biogenic amines.
Article Details
- CitationCopy to clipboard
McKenna KF, Baker GB, Coutts RT
N2-acetylphenelzine: effects on rat brain GABA, alanine and biogenic amines.
Naunyn Schmiedebergs Arch Pharmacol. 1991 May;343(5):478-82.
- PubMed ID
- 1881457 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Phenelzine 4-aminobutyrate aminotransferase, mitochondrial Protein Humans UnknownInhibitorDetails Phenelzine Alanine aminotransferase 1 Protein Humans UnknownInhibitorDetails Phenelzine Alanine aminotransferase 2 Protein Humans UnknownInhibitorDetails