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G蛋白偶联受体/G蛋白
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5-羟色胺受体
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/ Vilazodone/维拉佐酮

Vilazodone/维拉佐酮 {[allProObj[0].p_purity_real_show]}

货号：A913265 同义名： EMD 68843; SB659746A

Vilazodone 是一种选择性 5-HT 再摄取抑制剂（SSRI）和 5-HT1A 受体部分激动剂，适用于重度抑郁症相关神经递质机制的研究。

Vilazodone/维拉佐酮 化学结构 CAS号：163521-12-8
Vilazodone/维拉佐酮 化学结构
CAS号：163521-12-8
Vilazodone/维拉佐酮 3D分子结构
CAS号：163521-12-8
Vilazodone/维拉佐酮 化学结构 CAS号：163521-12-8
Vilazodone/维拉佐酮 3D分子结构 CAS号：163521-12-8
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Vilazodone/维拉佐酮 纯度/质量文件 产品仅供科研

货号：A913265 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

 		98%
Tropisetron ✔ 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Vilazodone/维拉佐酮 生物活性

描述 Vilazodone is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone (intraperitoneal injection; 3 mg/kg ; single dose) produces increases in extracellular levels of 5‐HT in both the frontal cortex (FC) and ventral hippocampus (vHipp) of rats in vivo microdialysis studies. Maximum increases are observed at 3 mg/kg and reaches 527% and 558% of preinjection baseline values in the FC and vHipp, respectively. Vilazodone (oral gavage ;55 mg/kg ; single dose) inhibits stress‐induced vocalizations in the rat ultrasonic vocalizations test at 120 and 210 min post dose[3]. Chronic vilazodone treatment markedly decreased 5-HT1A receptor levels in cortical and hippocampal regions, while the SSRIs increased levels of this receptor in similar regions[4]. Using in vivo microdialysis, vilazodone (10 mg/kg p.o.) was demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. Vilazodone behaved as a high efficacy partial agonist at the rat hippocampal 5-HT1A receptors in vitro and occupied 5-HT transporters in vivo[5]. Vilazodone inhibited L-DOPA(Levodopa)-induced gene regulation selectively in the direct pathway of the dopamine-depleted striatum[6]. Vilazodone was generally well tolerated in the short- and long-term treatment of MDD(major depressive disorder), with diarrhoea and nausea being the most frequently occurring treatment-emergent adverse events[7].

Vilazodone/维拉佐酮 细胞实验

Cell Line
Concentration Treated Time Description References
Meg-01 cells Meg-01 cells VLZ significantly increased the percentage of CD41+/CD42b+ cells in Meg-01 cells and promoted polyploidization. Elife. 2024 Apr 4;13:RP94765.
HEL cells HEL cells VLZ significantly increased the percentage of CD41+/CD42b+ cells in HEL cells and promoted polyploidization. Elife. 2024 Apr 4;13:RP94765.
COS-7 cells COS-7 cells To evaluate the inhibitory effect of Vilazodone on S-CIT binding, showing a Ki value of 0.7 nM Nat Commun. 2021 Aug 20;12(1):5063.
COS-7 cells COS-7 cells To evaluate the inhibitory effect of Vilazodone on 5-HT transport, showing a Ki value of 1.1 nM Nat Commun. 2021 Aug 20;12(1):5063.

Vilazodone/维拉佐酮 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Tg (itga2b: eGFP) transgenic zebrafish 10–40 µM 3 dpf to 5 dpf VLZ significantly increased the number of GFP+ cells in the tail region of zebrafish, indicating an increase in platelets. Elife. 2024 Apr 4;13:RP94765.
Mice Apcmin/+; KrasG12D; Tp53+/− mice Oral 25 mg/kg Once daily for 14 days To evaluate the effect of combined treatment with Vilazodone and Regorafenib, showing significant tumor growth inhibition Proc Natl Acad Sci U S A. 2024 Oct 15;121(42):e2406936121
Rats Unilateral 6-hydroxydopamine (6-OHDA) lesion model Intraperitoneal injection 10 mg/kg Once daily for 3 weeks To evaluate the effects of Vilazodone on L-DOPA-induced dyskinesia and gene regulation. Results showed that Vilazodone suppressed L-DOPA-induced dyskinesia and gene regulation without interfering with the prokinetic effects of L-DOPA. Cells. 2020 Oct 9;9(10):2265
Rats Methylphenidate-induced gene regulation model Intraperitoneal injection 10-20 mg/kg Single administration To evaluate the effects of vilazodone on methylphenidate-induced gene regulation and behavior in the striatum. Results showed that, in contrast to fluoxetine, vilazodone did not potentiate methylphenidate-induced gene regulation in the striatum, while it enhanced methylphenidate-induced locomotor activity. Mol Neurobiol. 2024 Apr;61(4):1907-1919
Female Wistar Albino rats Chronic unpredictable mild stress (CUMS) model Oral 10 mg/kg Once daily for 2 weeks Vilazodone alleviated CUMS-induced anxiety-like behaviors by modulating Wnt/β-catenin signaling, improving hippocampal histology, and regulating neurogenesis-related protein expression. Mol Neurobiol. 2024 Nov;61(11):9060-9077
Mice 129SvEv mice Gavage 10 mg/kg 8 and 28 days To evaluate the effect of Vilazodone in the NSF test, results showed that in 129SvEv mice, Vilazodone significantly reduced the latency to eat within 8 days. Int J Neuropsychopharmacol. 2016 Jun 28;19(10):pyw057

Vilazodone/维拉佐酮 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01916824 - Completed - -
NCT01916824 Major Depressive Disorder ... 展开 >> Healthy Controls 收起 << Phase 4 Completed - United States, Georgia ... 展开 >> Emory Mood and Anxiety Disorders Program Atlanta, Georgia, United States, 30322 收起 <<
NCT01469377 Major Depressive Disorder Phase 2 Completed - -

Vilazodone/维拉佐酮 参考文献

[1]Cruz MP. Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder. P T. 2012 Jan;37(1):28-31.

[2]Reed CR, Kajdasz DK, Whalen H, Athanasiou MC, Gallipoli S, Thase ME. The efficacy profile of vilazodone, a novel antidepressant for the treatment of major depressive disorder. Curr Med Res Opin. 2012 Jan;28(1):27-39.

[3]Cruz MP. Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder. P T. 2012 Jan;37(1):28-31

[4]Oosting RS, Chan JS, Olivier B, Banerjee P, Choi YK, Tarazi F. Differential effects of vilazodone versus citalopram and paroxetine on sexual behaviors and serotonin transporter and receptors in male rats. Psychopharmacology (Berl). 2016 Mar;233(6):1025-34

[5]Hughes ZA, Starr KR, Langmead CJ, Hill M, Bartoszyk GD, Hagan JJ, Middlemiss DN, Dawson LA. Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone. Eur J Pharmacol. 2005 Mar 7;510(1-2):49-57

[6]Altwal F, Moon C, West AR, Steiner H. The Multimodal Serotonergic Agent Vilazodone Inhibits L-DOPA-Induced Gene Regulation in Striatal Projection Neurons and Associated Dyskinesia in an Animal Model of Parkinson's Disease. Cells. 2020 Oct 9;9(10):2265

[7]Frampton JE. Vilazodone: in major depressive disorder. CNS Drugs. 2011 Jul;25(7):615-27

Vilazodone/维拉佐酮 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.32mL

2.26mL

1.13mL

22.65mL

4.53mL

2.26mL

Vilazodone/维拉佐酮 技术信息

CAS号163521-12-8
分子式C26H27N5O2
分子量 441.52
SMILES Code O=C(C1=CC2=CC(N3CCN(CCCCC4=CNC5=C4C=C(C#N)C=C5)CC3)=CC=C2O1)N
MDL No. MFCD09838919
别名 EMD 68843; SB659746A
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 80 mg/mL(181.19 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Vilazodone | 163521-12-8 | EMD 68843 | SB659746A | EMD68843 | EMD-68843 | Serotonin Reuptake Inhibitor | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | Serotonin Transporter | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Vilazodone/维拉佐酮 纯度/质量文件 | Vilazodone/维拉佐酮 亚型比较 | Vilazodone/维拉佐酮 生物活性 | Vilazodone/维拉佐酮 临床数据 | Vilazodone/维拉佐酮 参考文献 | Vilazodone/维拉佐酮 实验方案 | Vilazodone/维拉佐酮 技术信息

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