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Safinamide-d4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Safinamide-d4图片
包装:1mg
规格:98%
市场价:4815元
分子量:306.4

产品介绍
C17H15D4FN2O2
货号:ajcx19600
CAS:N/A
分子式:C17H15D4FN2O2
分子量:306.4
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Safinamide-d4 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; IC50 = ~0.1 μM).1 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).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 (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 , picrotoxin , 3-mercaptopropionic acid, and strychnine in mice (ED50s = 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.

参考文献
1. Strolin Benedetti, M.S., Marrari, P., Colombo, M., et al. The anticonvulsant FCE 26743 is a selective and short-acting MAO-B inhibitor devoid of inducing properties towards cytochrome P450-dependent testosterone hydroxylation in mice and rats. J. Pharm. Pharmacol. 46(10), 814-819 (1994).
2. Salvati, P., Maj, R., Caccia, C., et al. Biochemical and electrophysiological studies on the mechanism of action of PNU-151774E, a novel antiepileptic compound. J. Pharmacol. Exp. Ther. 288(3), 1151-1159 (1999).
3. Fariello, R.G., McArthur, R.A., Bonsignori, A., et al. Preclinical evaluation of PNU-151774E as a novel anticonvulsant. J. Pharmacol. Exp. Ther. 285(2), 397-403 (1998).