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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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