Vortioxetine-d8 hydrobromide(Synonyms: Lu AA21004-d8 hydrobromide)

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Vortioxetine-d8 hydrobromide (Synonyms: Lu AA21004-d8 hydrobromide)

Vortioxetine-d8 (Lu AA21004-d8) hydrobromide 是 Vortioxetine hydrobromide 的氘代物。Vortioxetine hydrobromide 是5-HT1A，5-HT1B，5-HT3A，5-HT7 受体 和5-羟色胺转运体 (SERT) 的抑制剂，其Ki值分别为 15 nM，33 nM，3.7 nM，19 nM 和 1.6 nM。

Vortioxetine-d8 hydrobromide(Synonyms: Lu AA21004-d8 hydrobromide)

Vortioxetine-d8 hydrobromide Chemical Structure

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生物活性

Vortioxetine-d8 (Lu AA21004-d8) hydrobromide is the deuterium labeled Vortioxetine hydrobromide. Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively[1][2].

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

387.41

Formula

C18H15D8BrN2S
中文名称

盐酸沃替西汀 d8 (氢溴酸盐)
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]. Bang-Andersen B, et al. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21.

    [3]. Guilloux JP, et al. Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 May 28;73C:147-159.

    [4]. Theunissen EL, et al. A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013 Jun;93(6):493-501.

    [5]. Rothschild AJ, Mahableshwarkar AR, Jacobsen P, Vortioxetine (Lu AA21004) 5mg in generalized anxiety disorder: results of an 8-week randomized, double-blind, placebo-controlled clinical trial in the United States. Eur Neuropsychopharmacol. 2012 Dec;22(12):858-66.

    [6]. Mork A, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J Pharmacol Exp Ther. 2012 Mar;340(3):666-75.

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