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Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes with IC50 of 9 μM. Safinamide increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals. Safinamide significantly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide has a high oral bioavailability (80–92%), is rapidly absorbed in plasma after reaching the peak within 0.5–2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively. Safinamide is currently in a Phase II clinical trial.
| Molecular Weight | 398.45 |
| Formula | C17H19FN2O2.CH4O3S |
| CAS Number | 202825-46-5 |
| Solubility (25°C) | DMSO 80 mg/mL Water 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Daniel A Hussar, et al. Safinamide mesylate, Brodalumab, Guselkumab, and Abaloparatide
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