Vortioxetine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
沃替西汀是一种新型的多模式抗抑郁药,目前正处于抑郁症治疗的研发阶段.5-羟色胺能系统通过不同的5-HT受体,在认知功能方面发挥着重要作用.
体外实验:沃替西汀(Lu AA21004)是先导化合物,对重组人5-HT1A(Ki = 15 nM)\5-HT1B (Ki = 33 nM)\5-HT3A (Ki = 3.7 nM)\5-HT7 (Ki = 19 nM)\去甲肾上腺素能β1受体(Ki = 46 nM)及SERT (Ki = 1.6 nM)有高亲和力.沃替西汀对5-HT3A 和5-HT7受体有拮抗特性,对5-HT1B受体有部分激动剂特性,对5-HT1A受体有激动性,强效抑制SERT[1].
体内实验:在意识清醒的大鼠中,沃替西汀急性治疗3天后,可显著提升大脑内的胞外5-HT水平.治疗3天后(每天5或10 mg/kg),SERT占有率仅分别为43%和57% [1].
临床实验:连续15天晚上用药,沃替西汀不会引发认知或精神运动障碍.然而,第2天米氮平损伤认知和精神运动性行为.服用多次剂量的米氮平后,大多数此类影响消失[2].
参考文献：
[1] Bang-Andersen B, Ruhland T, Jrgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mrk A, Stensbl 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, Hjer 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 298.45 |
| Cas No. | 508233-74-7 |
| Formula | C18H22N2S |
| Synonyms | Lu AA 21004;Lu AA21004 |
| Solubility | insoluble in H2O; ≥14.92 mg/mL in DMSO; ≥4.31 mg/mL in EtOH with ultrasonic |
| Chemical Name | 1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | 沃替西汀(Vortioxetine)是一种5-HT3受体拮抗剂,IC50值为12 nM. | |||||
| 靶点 | 5-HT3 receptor | |||||
| IC50 | 12 nM | |||||
质量控制和MSDS
- 批次:
化学结构
