Understand if your compound is an inhibitor of MAO-A or MAO-B enzyme.
Monoamine oxidase (MAO) inhibition is a non-CYP mediated metabolism assay within our portfolio of in vitro ADME screening services. Cyprotex deliver consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements.
In human brain the predominant form is MAO-B, expressed at highest levels in astrocytes and serotonergic neurons, while MAO-A is expressed at highest levels in catecholaminergic neurons.
1Hotamisligil GS and Breakefield XO (1991) Am J Hum Genet 49(2); 383–392
Substrate | Kynuramine |
---|---|
Metabolite | 4-hydroxyquinolinol |
Test Article Concentrations | 0, 0.4, 1, 4, 10, 40 and 100 µM (different concentrations available) |
Enzyme Source | hMAO-A and hMAO-B expressed enzymes (Supersomes™) |
Test Article Requirements | 100 μL of a 40 mM DMSO solution (or equivalent amount in solid) |
Positive Control | Clorgyline MAO-A Selegiline MAO-B |
Analysis Method | LC-MS/MS |
Data Delivery | IC50 Standard error of IC50 % Control at each concentration |
1 Hotamisligil GS and Breakefield XO (1991) Human monoamine oxidase A gene determines levels of enzyme activity. Am J Hum Genet 49(2); 383–392
Learn more about drug metabolism in chapter 3 of our popular Everything you need to know about ADME guide.
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