Mofegiline (hydrochloride)

Mofegiline is an inhibitor of monoamine oxidase B (MAO-B; IC₅₀ = 3.6 nM for the rat brain mitochondrial enzyme).¹ It is selective for MAO-B over MAO-A (IC₅₀ = 680 nM). Mofegiline also inhibits vascular adhesion protein-1 (VAP-1), also known as semicarbazide-sensitive amine oxidase (SSAO), an enzyme that has roles in leukocyte adhesion and transmigration, with an IC₅₀ value of 20 nM for the human enzyme.² It reduces MPTP-induced decreases in striatal levels of dopamine, dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) in mice when administered at a dose of 1.25 mg/kg.¹ Mofegiline (5 mg/kg) also inhibits LPS-induced increases in bronchoalveolar lavage fluid (BALF) levels of TNF-α in transgenic mice overexpressing VAP-1.

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1. Zreika, M., Fozard, J.R., Dudley, M.W., et al. MDL 72,974: A potent and selective enzyme-activated irreversible inhibitor of monoamine oxidase type B with potential for use in Parkinson’s disease. J. Neural Transm. Park. Dis. Dement. Sect. 1(4), 243-254 (1989).

2. Foot, J.S., Deodhar, M., Turner, C.I., et al. The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1). Bioorg. Med. Chem. Lett. 22(12), 3935-3940 (2012).