Formulation: A solid
Formal Name: 2S-[[[4-[(3-fluorophenyl)methoxy]phenyl-2,3,5,6-d4]methyl]amino]-propanamide
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C17H15D4FN2O2
Formula Weight: 306,4
Shelf life (days): 1460
CAS Number: 2748522-33-8
Notes: Safinamide-d4 is intended for use as an internal standard for the quantification of safinamide (Item No. 21546) by GC- or LC-MS. Safinamide is an inhibitor of monoamine oxidase B (MAO-B; IC50 = ~0.1 μM).{33890} It is selective for MAO-B over MAO-A (IC50 = >10 μM). It also inhibits radioligand binding to sodium channel binding site 2, sigma-1, and sigma-2 receptors in rat brain membranes (IC50s = 8.2, 0.019, and 1.59 μM, respectively).{46371} Safinamide inhibits high voltage-activated calcium currents and depolarization-induced tetrodotoxin-sensitive fast sodium currents in rat hippocampal neurons in a concentration-dependent manner. It inhibits veratrine-induced glutamate release in rat hippocampal slices (IC50 = 56 μM). Safinamide inhibits maximal electroshock-induced tonic extension seizures in mice and rats (ED50s = 8 and 11.8 mg/kg, p.o.) as well as maximal seizures induced by bicuculline (Item No. 11727), picrotoxin (Item No. 20771), 3-mercaptopropionic acid, and strychnine in mice (ED50s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively).{46372} Formulations containing safinamide have been used as adjunctive treatments to levodopa and carbidopa in the treatment of “off” episodes associated with Parkinson’s disease.
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