Inhibition of MAO by substituted tryptamine analogues.
Three different acetylenic analogues of tryptamine, in which the side chain is attached at the 2 position of the heterocyclic ring, were studied as inhibitors of MAO-A and MAO-B. IC50 values were determined after 30 min preincubation of the enzyme and inhibitor, at 37 degrees C before assay. Irreversibility and time-dependence of the inhibition were also established in each case. The kinetic parameters defining non-covalent complex formation and covalent adduct formation were calculated for the mechanism-based inhibition of both MAO-A and MAO-B by these compounds.
Balsa
D
D
Departament de Bioquímica i Biología Molecular, Facultat de Medicina, Universitát Autónoma de Barcelona, Spain.
Fernandez-Alvarez
E
E
Tipton
K F
KF
Unzeta
M
M
D000818:Animals; D066298:In Vitro Techniques; D007700:Kinetics; D008930:Mitochondria, Liver / Q000201:enzymology; D008995:Monoamine Oxidase / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors; D010627:Phenethylamines / Q000378:metabolism; D051381:Rats; D012701:Serotonin / Q000378:metabolism; D014363:Tryptamines / Q000494:pharmacology*
D008996:Monoamine Oxidase Inhibitors; D010627:Phenethylamines; D014363:Tryptamines; C029261:phenethylamine; D012701:Serotonin; D008995:Monoamine Oxidase