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Safinamide-d4-1(Synonyms: FCE 26743-d4-1; EMD 1195686-d4-1)

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Safinamide-d4-1 (Synonyms: FCE 26743-d4-1; EMD 1195686-d4-1)

Safinamide-d4-1 是 Safinamide 氘代物。Safinamide 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 的抑制剂 (IC50=0.098 µM)，对 MAO-A (IC50=580 µM) 选择性较低。Safinamide 也阻断钠通道和调节谷氨酸 (Glu) 释放，在去极化时 (IC50= 8 µM) 比静息电位 (IC50=262 µM) 时，显示出更大的亲和力。Safinamide 具有神经保护作用，可用于帕金森病、缺血脑卒中等疾病的研究。

Safinamide-d4-1(Synonyms: FCE 26743-d4-1; EMD 1195686-d4-1)

Safinamide-d4-1 Chemical Structure

CAS No. : 2748522-33-8

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生物活性

Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

306.37

Formula

C17H15D4FN2O2
CAS 号

2748522-33-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Leonetti F, et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem, 2007, 50(20), 4909-4916.

    [3]. C Caccia, et al.Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23.

    [4]. Michele Morari, et al. Safinamide Differentially Modulates In Vivo Glutamate and GABA Release in the Rat Hippocampus and Basal Ganglia.J Pharmacol Exp Ther. 2018 Feb;364(2):198-206.

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