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Vortioxetine
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图片
CAS NO:508233-74-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议
100mg电议

产品介绍
Vortioxetine 是 5-HT1A、5-HT1B、5-HT3A、5-HT7 受体和 SERT 的抑制剂，Ki 值分别为 15 nM、33 nM、3.7 nM、19 nM 和 1.6 nM。
Cas No.508233-74-7
别名沃替西汀; Lu AA 21004
化学名1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine
Canonical SMILESCC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C
分子式C18H22N2S
分子量298.45
溶解度≥ 14.9 mg/mL in DMSO, ≥ 4.31 mg/mL in EtOH with ultrasonic
储存条件Store at -20℃
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 is a novel multimodal antidepressant currently under development for the treatment of MDD. The serotonergic system plays an important role in cognitive functions via various 5-HT receptors.

In vitro: Vortioxetine (Lu AA21004) was the lead compound, displaying high affinity for recombinant human 5-HT1A (Ki = 15 nM), 5-HT1B (Ki = 33 nM), 5-HT3A (Ki = 3.7 nM), 5-HT7 (Ki = 19 nM), and noradrenergic β1 (Ki = 46 nM) receptors, and SERT (Ki = 1.6 nM). Vortioxetine displayed antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT [1].

In vivo: In conscious rats, vortioxetine significantly increased extracellular 5-HT levels in the brain after acute and 3 days of treatment. Following the 3-day treatment (5 or 10 mg/kg/day) SERT occupancies were only 43% and 57%, respectively [1].

Clinical trial: Drugs were administered in the evening of 15 consecutive days. Vortioxetine did not cause cognitive or psychomotor impairment. However, mirtazapine impaired cognitive and psychomotor performance on day 2. Most of these effects disappeared after multiple doses of mirtazapine [2].

References:
[1] Bang-Andersen B, Ruhland T, Jorgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mork A, Stensbol TB.  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;54(9):3206-21.
[2] Theunissen EL, Street D, Hojer AM, Vermeeren A, van Oers A, Ramaekers JG.  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;93(6):493-501.