Safinamide Mesylate 202825-46-5

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Molecular Weight:

398.45 Safinamide Mesylate is mesylate salt of Safinamide, selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A. Phase 3.






Biological Activity


Safinamide is a highly selective MAO-B inhibitor in rat brain
mitochondria, with an IC50 of 98 nM. safinamide inhibits MAO-B in human
brain with an IC50 of 9 nM. Safinamide has high affinity for the Na+ channel-binding site II in rat cortical membranes, with an IC50 of 8 μM. Safinamide inhibits the fast Na+ currents in a concentration- and state-dependent manner in rat cortical neurons.


Safinamide blocks N-Type Ca2+ currents in rat cortical neurons with IC50 23 μM. Safinamide inhibits
glutamate release induced by depolarizing conditions in rat hippocampal
synaptosomes with IC50 of 9 μM. Safinamide incubated 1 hour before
veratridine reduces the neuron damage with an IC50 1.4 μM through
blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. Safinamide binds to human MAO B with a Ki of 0.5 μM. Safinamide binds
to human MAO B in an extended conformation occupying both flavin and
entrance cavity.


Safinamide orally administrated dose-dependently inhibits mouse brain
MAO-B with IC50 of 0.6 mg/kg, and MAO-B activity recovers quickly,
starting from 8 hours. Safinamide significantly inhibits cell body
degeneration in the substantia nigra pars compacta.


Safinamide
intraperitoneally administered 15 minutes before kainic acid protects
against hippocampal neuron loss, starting at 10 mg/kg showing
neuroprotective properties. Safinamide intraperitoneally administrated
at dose of 100 mg/kg shows a relevant neurorescuing effect on
hippocampal neurons when given 3 hours after ischemia. 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.

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Product Categories : Metabolism > MAO Inhibitor