| CAS NO: | 508233-74-7 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| 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 |
| 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 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
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.
| 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 | |||||
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