RGNCY-0074 (Sembragiline MAO-B inhibitor)

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Sembragiline is a novel selective monoamine oxidase B (MAO-B) inhibitor specifically developed for  the treatment of Alzheimer's disease.  This compound shows potent and log-lasting MAO-B selective inhibition and did not inhibit MAO-A at comparable doses of full MAO-B inhibition.  Sembragiline does not induce serotonin syndrome when administered with the serotonin precursor L-5-hydroxytryptophan in combination with antidepressants such as fluoxetine, nor potentiate the pressor effect of tyramine.  In addition, sembragiline protects against neuronal loss and reduced both ROS formation and reactive astrogliosis in transgenic animal models conditionally over-expressing MAO-B in astroglia.  These data suggest that sembragiline is worthy of further investigation as a potential MAO-B inhibitor therapy in patients with AD and other neurological disorders.  hMAO-B IC50 =5.9+0.62, hMAO-A IC50=3852+597.

SMILE:  FC1=CC=CC(COC2=CC=C(N3C[C@@H](NC(C)=O)CC3=O)C=C2)=C1

Systematic Name:  (S)-N-(1-(4-((3-fluorobenzyl)oxy)phenyl)-5-oxopyrrolidin-3-yl)acetamide 

Molecular Weight:  342.37

Formula:  C19H19FN2O3

PMID:  28642233