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  • Title: Tissue levels and some pharmacological properties of an acetylated metabolite of phenelzine in the rat.
    Author: Coutts RT, Mozayani A, Danielson TJ, Baker GB.
    Journal: J Pharm Sci; 1991 Aug; 80(8):765-7. PubMed ID: 1791538.
    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.
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