Safinamide (mesylate)

Safinamide is an inhibitor of monoamine oxidase B (MAO-B, IC50 = ~0.1 µM). 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). 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 (Cay-11727), picrotoxin (Cay-20771), 3-mercaptopropionic acid, and strychnine in mice (ED50s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively). Formulations containing safinamide have been used as adjunctive treatments to levodopa and carbidopa in the treatment of "off" episodes associated with Parkinson's disease.Formal Name: 2S-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-propanamide, monomethanesulfonate. CAS Number: 202825-46-5. Synonyms: EMD 1195686, FCE 26743, NW-1015, PNU-151774E. Molecular Formula: C17H19FN2O2 . CH3SO3H. Formula Weight: 398.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): slightly soluble. lambdamax: 228, 263, 269 nm. SMILES: FC1=CC(COC2=CC=C(CN[C@@H](C)C(N)=O)C=C2)=CC=C1.O=S(O)(C)=O. InChi Code: InChI=1S/C17H19FN2O2.CH4O3S/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14,1-5(2,3)4/h2-9,12,20H,10-11H2,1H3,(H2,19,21),1H3,(H,2,3,4)/t12-,/m0./s1. InChi Key: YKOCHIUQOBQIAC-YDALLXLXSA-N.