PMID: 1791538Aug 1, 1991

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

Journal of Pharmaceutical Sciences
R T CouttsG B Baker

Abstract

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.

References

Feb 28, 1979·Psychopharmacology·W J TilstoneE C Johnstone
Mar 17, 1973·Lancet·E C Johnstone, W Marsh
Jan 1, 1966·International Journal of Neuropharmacology·A Spinks, B A Whittle
Nov 1, 1983·The American Journal of Medicine·C A Heller, P A Friedman
Mar 1, 1962·Journal of Medicinal and Pharmaceutical Chemistry·F E ANDERSONJ A HART
Dec 1, 1963·Biochemical Pharmacology·R J WURTMAN, J AXELROD

Related Concepts

N-acetylphenelzine
Acetylation
Biogenic Amines
Brain
Chromatography, Gas-Liquid
Dealkylation
Injections, Intraperitoneal
Liver
Monoamine Oxidase
RIMA (Reversible Inhibitor of Monoamine Oxidase A)

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