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PMID: 7130973 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

beta-Carbolines as selective monoamine oxidase inhibitors: in vivo implications.

Journal of neural transmission ·Vol. 54 ·No. 3-4 ·1982-00-00 ·Pages 209-18

Glover V, Liebowitz J, Armando I, Sandler M

Abstract

The inhibitory action of a range of beta-carbolines on human and rat monoamine oxidase (MAO) A and B has been studied. Concentrations of 5-hydroxytryptamine and phenylethylamine, approximately at their Km values, were used as substrates for MAO A and B respectively. A wide variation in selectivity was found, with harmaline being 10,000 times more potent an inhibitor of A than B whereas, using tetrahydro-beta-carboline and harmane, the difference was nearer to ten-fold. Of the carbolines which have been found endogenously, tetrahydro-beta-carboline, 6-methoxytetrahydro-beta-carboline and harmane are all sufficiently potent inhibitors of human MAO A, with I50 values of 5 X 10(-6), 10(-6), 5 X 10(-7) M respectively, for this property to be of possible physiological significance. Harmane, with an I50 of 5 X 10(-6) M, might also play a role as an inhibitor of MAO B.

MeSH Terms
Animals Blood Platelets/enzymology Carbolines/pharmacology Female Humans Indoles/pharmacology Liver/enzymology Monoamine Oxidase Monoamine Oxidase Inhibitors Placenta/enzymology Pregnancy Rats
Chemicals
Carbolines Indoles Monoamine Oxidase Inhibitors Monoamine Oxidase
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Glover V
Liebowitz J
Armando I
Sandler M
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30 references, click to expand
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Article Info
Journal
Journal of neural transmission
Abbr.
J Neural Transm
DOI
10.1007/BF01254930
Published
1982-00-00
Pages
209-18
Language
English
Region
Austria
NLM ID
0337042
Subset
IM
External Links
PubMed source DOI: 10.1007/BF01254930
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