Substituted xanthones as selective and reversible monoamine oxidase A (MAO-A) inhibitors

1,3-Dihydroxy-2-methylxanthone (X1), its 4-chloro and 4-bromo derivatives (X1-Cl and X1-Br), and 1,3-dihydroxy-4-methylxanthone were investigated for their inhibition activities toward MAO. A hyperbolic function was derived to fit the data and to calculate IC50 values. The compounds proved to be rev...

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Veröffentlicht in:Pharmaceutical research 1993-08, Vol.10 (8), p.1187-1190
Hauptverfasser: THULL, U, KNEUBÜHLER, S, TESTA, B, BORGES, M. F. M, PINTO, M. M. M
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container_end_page 1190
container_issue 8
container_start_page 1187
container_title Pharmaceutical research
container_volume 10
creator THULL, U
KNEUBÜHLER, S
TESTA, B
BORGES, M. F. M
PINTO, M. M. M
description 1,3-Dihydroxy-2-methylxanthone (X1), its 4-chloro and 4-bromo derivatives (X1-Cl and X1-Br), and 1,3-dihydroxy-4-methylxanthone were investigated for their inhibition activities toward MAO. A hyperbolic function was derived to fit the data and to calculate IC50 values. The compounds proved to be reversible and selective inhibitors of MAO-A, with X1 displaying the highest activity (IC50 = 3.7 microM).
doi_str_mv 10.1023/A:1018924503552
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source MEDLINE; SpringerLink Journals - AutoHoldings
subjects Animals
Biological and medical sciences
Brain - ultrastructure
Brain Chemistry - drug effects
In Vitro Techniques
Kinetics
Medical sciences
Mitochondria - drug effects
Mitochondria - enzymology
Monoamine Oxidase - metabolism
Monoamine Oxidase Inhibitors - chemical synthesis
Monoamine Oxidase Inhibitors - pharmacology
Nerve Tissue Proteins - metabolism
Neuropharmacology
Pharmacology. Drug treatments
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Rats
Rats, Sprague-Dawley
Xanthines - chemical synthesis
Xanthines - pharmacology
title Substituted xanthones as selective and reversible monoamine oxidase A (MAO-A) inhibitors
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