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°C before assay. Irreversibility and time-dependence of the inhibiton 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.
KeywordsMonoamine Oxidase Heterocyclic Ring Acetylenic Group Mitochondrial Monoamine Oxidase Reaction Progress Curve
Unable to display preview. Download preview PDF.
- Fowler CJ, Tipton KF (1982) Deamination of 5-hydroxytryptamine by both forms of monoamine oxidase in rat brain. J Neurochem 38:733–736 Fowler CJ, Mantle JT, Tipton KF (1982) The nature of inhibition of rat liver monoamine oxidase types A and B by the acetylenic inhibitors clorgyline, 1-deprenyl and pargyline. Biochem Pharmacol 31:3555-3561.PubMedCrossRefGoogle Scholar