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Vortioxetine(Lu AA21004)HBr
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(Lu AA21004)HBr图片
CAS NO:960203-27-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
Vortioxetine (Lu AA21004) HBr 是一种多模式 5-羟色胺能剂，抑制 5-HT1A、5-HT1B、5-HT3A、5-HT7 受体和 SERT，Ki 值为 15 nM、33 nM、3.7 nM、19 nM 和 1.6 nM，分别。
Cas No.960203-27-4
别名盐酸沃替西汀; Lu AA21004 hydrobromide
化学名1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;hydrobromide
Canonical SMILESCC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.Br
分子式C18H22N2S.HBr
分子量379.36
溶解度≥ 18.968mg/mL in DMSO
储存条件Store at 2-8℃
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 (Lu AA21004) HBr (vortioxetine) is an antidepressant, [1] [2] and a serotonin (5-HT) receptor modulator [1] [3] with Ki values of 3.7 nM, 19 nM, 200 nM, 33 nM, 15 nM, and 1.6 nM, to human (h) 5-HT3A receptor, h5-HT7 receptor, rat (r) 5-HT7 receptor, h5-HT1B receptor, h5-HT1A receptor and h5-HT transporter (hSERT), respectively, with an IC50 value of 2080 nM to r5-HT7 receptor, and with an EC50 value of 460 nM to h5-HT1B receptor [3].

5-HT is important in brain, acting as a neurotransmitter in neuromodulation [4].

In HELA cells expressing h5-HT1B receptors stably, Lu AA21004 displayed a partial agonistic response with an EC50 value of 460±110 nM and an IA of 22%. In a polyclonal HEK-293 cell line expressing the r5-HT7 receptor, Lu AA21004 bound to the r5-HT7 receptor with a Ki value of 200±27 nM and was a functional antagonist at the r5-HT7 receptor with an IC50 value of 2080±18 nM [3].

In rats, subcutaneous (sc) administration of Lu AA21004 resulted in ED50 values of 0.4 mg/kg and 3.2 mg/kg to the rSERT and the r5-HT1B receptor, respectively. Lu AA21004 acted as an antagonist of 5-HT3 receptor with an ED50 value of 0.11 mg/kg sc [3]. Treatment with vortioxetine at doses of 2.5 and 5 mg/kg prior to the acquisition of novel objects made rats show 29 and 33 s, respectively, as average exploration values [5].

References:
[1].  Connie Sanchez, Karen E. Asin, Francesc Artigas, et al. Vortioxetine, a novel antidepressant with multimodal activity: Review of preclinical and clinical data. Pharmacology & Therapeutics, 2015, 145:43-57.
[2].  Er-min Gu, Chengke Huang, Bingqing Liang, et al. An UPLC–MS/MS method for the quantitation of vortioxetine in rat plasma: Application to a pharmacokinetic study. J. Chromatogr. B, 2015, 997:70-74.
[3].  A. Mork, A. Pehrson, L.T. Brennum, S. Moller Nielsen, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J. Pharmacol. Exp. Ther., 2012, 340:666-675.
[4].  David M. Lovinger. Serotonin’s Role in Alcohol’s Effects on the Brain. Alcohol Health & Research World, 1997, 21(2):114-120.
[5].  Arne Mork, Liliana P. Montezinho, Silke Miller, et al. Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacology, Biochemistry and Behavior, 2013, 105:41-50.