Thursday, August 23, 2012
Publication and contact
Assays & screens
In situ monitoring of dopamine
metabolism to identify improved monoamine
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.
Published online Aug. 23, 2012
status not applicable
Ueki, R. et al. J. Am.
published online July 19,
Contact: Shinsuke Sando,
Kyushu University, Fukuoka,
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