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TB5 is a potent and selective monoamine oxidase B (MAO-B) inhibitor with Ki values of 110 and 1,450 nM for MAO-B and MAO-A, respectively.1 It interacts with the catalytic site of human MAO-B in a competitive manner. In an enzyme assay, MAO-B activity increases from 37% to 97% following inhibitor washout, indicating TB5 binding is reversible. TB5 also demonstrates permeability in a parallel artificial membrane permeation assay (PAMPA), a model for the blood-brain barrier, and has minimal cytotoxicity (>84% cell viability) in HepG2 cells at a concentrations up to 25 μM.
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1. Synthesis, biochemistry, and computational studies of brominated thienyl chalcones: A new class of reversible MAO-