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Monoamine oxidase (MAO) inhibitors act on mitochondrial enzymes that inactivate monoamine neurotransmitters. The two isoforms, MAO-A and MAO-B, are flavin adenine dinucleotide (FAD)-containing enzymes bound to the outer mitochondrial membrane. In 1968, studies with the inhibitor clorgyline revealed two forms of brain MAO, later named MAO-A and MAO-B. MAO-A preferentially oxidizes serotonin, whereas MAO-B prefers phenylethylamine and benzylamine. The 2002 crystal structure of human MAO-B showed an entrance cavity and a substrate cavity, which together reach the flavin cofactor. Inhibitors here include the MAO-A inhibitor moclobemide and the MAO-B inhibitors selegiline hydrochloride and rasagiline mesylate. Safinamide mesylate, a reversible MAO-B inhibitor, is used in Parkinson's disease research.
FCOB02 is a potent monoamine oxidase B (MAO-B) ligand designed for imaging applications. It exhibits high affinity for MAO-B, with an IC50 value of 10.68 nM, making it suitable for in vivo studies. When labeled as [18F]FCOB02, it serves as a valuable probe for specific MAO-B imaging and quantitative analysis, enabling researchers to investigate the role of MAO-B in various biological processes and diseases.
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