Safinamide

Catalog No.S5357 Synonyms: EMD-1195686, PNU-15774E

Safinamide Chemical Structure

Molecular Weight(MW): 302.34

Safinamide is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.

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Biological Activity

Description Safinamide is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.
Targets
MAO-B [1]
(Microsomal)
16.7 nM(Ki)
In vitro

The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. Safinamide also blocks sodium and calcium channels[2].

In vivo Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. Safinamide does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. Safinamide is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of safinamide is found excreted in the feces. Safinamide exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days[2].

Protocol

Solubility (25°C)

In vitro DMSO 60 mg/mL (198.45 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 302.34
Formula

C17H19FN2O2

CAS No. 133865-89-1
Storage powder
in solvent
Synonyms EMD-1195686, PNU-15774E

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