Safinamide-d
4
is intended for use as an internal standard for the quantification of safinamide  by GC- or LC-MS. Safinamide is an inhibitor of monoamine oxidase B (MAO-B; IC
50
= ~0.1 μM).
1
It is selective for MAO-B over MAO-A (IC
50
= >10 μM). It also inhibits radioligand binding to sodium channel binding site 2, sigma-1, and sigma-2 receptors in rat brain membranes (IC
50
s = 8.2, 0.019, and 1.59 μM, respectively).
2
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 (IC
50
= 56 μM). Safinamide inhibits maximal electroshock-induced tonic extension seizures in mice and rats (ED
50
s = 8 and 11.8 mg/kg, p.o.) as well as maximal seizures induced by bicuculline , picrotoxin , 3-mercaptopropionic acid, and strychnine in mice (ED
50
s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively).
3
Formulations containing safinamide have been used as adjunctive treatments to levodopa and carbidopa in the treatment of “off” episodes associated with Parkinson’s disease.

INDEX NAME NOT YET ASSIGNED

2748522-33-8: Safinamide-d
4
is intended for use as an internal standard for the quantification of safinamide  by GC- or LC-MS. Safinamide is an inhibitor of monoamine oxidase B (MAO-B; IC
50
= ~0.1 μM).
1
It is selective for MAO-B over MAO-A (IC
50
= >10 μM). It also inhibits radioligand binding to sodium channel binding site 2, sigma-1, and sigma-2 receptors in rat brain membranes (IC
50
s = 8.2, 0.019, and 1.59 μM, respectively).
2
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 (IC
50
= 56 μM). Safinamide inhibits maximal electroshock-induced tonic extension seizures in mice and rats (ED
50
s = 8 and 11.8 mg/kg, p.o.) as well as maximal seizures induced by bicuculline , picrotoxin , 3-mercaptopropionic acid, and strychnine in mice (ED
50
s = 26.9, 60.6, 21.5, and 104.1 mg/kg, p.o., respectively).
3
Formulations containing safinamide have been used as adjunctive treatments to levodopa and carbidopa in the treatment of “off” episodes associated with Parkinson’s disease.

CAS 2748522-33-8

INDEX NAME NOT YET ASSIGNED

Safinamide-d4

Ref: 4Z-S-073005