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Vortioxetine-d8
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。
Vortioxetine-d8图片
CAS NO:2140316-62-5
包装:1mg
市场价:4521元

产品介绍
Vortioxetine-d8 是一种氘标记的 Vortioxetine。
Cas No.2140316-62-5
别名Lu AA 21004 D8
Canonical SMILESCC1=CC(C)=CC=C1SC2=C(N3C([2H])([2H])C([2H])([2H])NC([2H])([2H])C3([2H])[2H])C=CC=C2
分子式C18H14D8N2S
分子量306.5
溶解度Chloroform: soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Vortioxetine-d8is intended for use as an internal standard for the quantification of vortioxetine by GC- or LC-MS. Vortioxetine is a multimodal serotonergic agent that acts as a serotonin reuptake inhibitor (Ki= 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).1It also binds to the β1-adrenergic receptor (Ki= 46 nM). It acts as an antagonist at 5-HT3Aand 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1Areceptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6receptors with Kivalues greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levelsin vivoin rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.2It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.

1.Bang-Andersen, B., Ruhland, T., JØrgensen, M., et al.Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): A novel multimodal compound for the treatment of major depressive disorderJ. Med Chem.54(9)3206-3221(2011) 2.Guilloux, J.P., Mendez-David, I., Pehrson, A., et al.Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in miceNeuropharmacology73147-159(2013)