N2-acetylphenelzine: effects on rat brain GABA, alanine and biogenic amines.
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.
McKenna
K F
KF
PMHAC Research Unit, Department of Psychiatry, University of Alberta, Edmonton, Canada.
Baker
G B
GB
Coutts
R T
RT
D000409:Alanine / Q000032:analysis*; D000818:Animals; D001679:Biogenic Amines / Q000032:analysis*; D001923:Brain Chemistry / Q000187:drug effects*; D066298:In Vitro Techniques; D008297:Male; D008995:Monoamine Oxidase / Q000032:analysis; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D010624:Phenelzine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D005680:gamma-Aminobutyric Acid / Q000032:analysis*
D001679:Biogenic Amines; D008996:Monoamine Oxidase Inhibitors; D005680:gamma-Aminobutyric Acid; C043198:N-acetylphenelzine; D008995:Monoamine Oxidase; D010624:Phenelzine; D000409:Alanine