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Assays & screens

In situ monitoring of dopamine metabolism to identify improved monoamine oxidase (MAO) inhibitors

A method of in situ monitoring of dopamine metabolism could be used to identify improved MAO inhibitors to treat neurological diseases. An isotope-labeled dopamine that could be used with NMR to detect MAO-mediated dopamine metabolism was synthesized. In a mouse liver tissue homogenate, the method identified analogs of an MAO inhibitor that were more potent inhibitors of dopamine metabolism in situ than the parent compound, despite being less potent inhibitors of the enzyme in vitro. Next steps include using the method to screen for additional MAO inhibitors with improved in situ potency.
At least 10 companies have MAO inhibitors in development stages from preclinical to marketed for neurological conditions and other diseases.

SciBX 5(33); doi:10.1038/scibx.2012.876
Published online Aug. 23, 2012

Unpatented; licensing status not applicable

Ueki, R. et al. J. Am. Chem. Soc.;

published online July 19, 2012;
Contact: Shinsuke Sando,

Kyushu University, Fukuoka, Japan