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...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
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
Format:	Artikel
Sprache:	eng
Schlagworte:	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
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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).
ISSN:	0724-8741 1573-904X
DOI:	10.1023/A:1018924503552