An inhibitor of MAO-B (IC50 = ~0.1 μM); selective for MAO-B over MAO-A (IC50 = >10 μM); inhibits radioligand binding to sodium channel binding site 2

Safinamide (mesylate) – 5 mg

Brand:
Cayman
CAS:
202825-46-5
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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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Description

An inhibitor of MAO-B (IC50 = ~0.1 μM); selective for MAO-B over MAO-A (IC50 = >10 μM); 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); inhibits high voltage-activated calcium currents and depolarization-induced tetrodotoxin-sensitive fast sodium currents in rat hippocampal neurons; inhibits veratrine-induced glutamate release in rat hippocampal slices (IC50 = 56 μM); 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, picrotoxin, 3-mercaptopropionic acid, and strychnine in mice (ED50s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively)

Formal name: 2S-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-propanamide, monomethanesulfonate

Synonyms:  EMD 1195686|FCE 26743|NW-1015|PNU-151774E

Molecular weight: 398.4

CAS: 202825-46-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease||Research Area|Neuroscience|Seizure Disorders

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