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维拉佐酮 /Vilazodone {[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,目前正在临床评估中,用于治疗重度抑郁症。

Vilazodone 化学结构 CAS号:163521-12-8
Vilazodone 化学结构
CAS号:163521-12-8
Vilazodone 3D分子结构
CAS号:163521-12-8
Vilazodone 化学结构 CAS号:163521-12-8
Vilazodone 3D分子结构 CAS号:163521-12-8
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Vilazodone 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]}
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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 (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 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 (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 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-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 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-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

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-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 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-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

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 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 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 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 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 技术信息

CAS号163521-12-8
分子式C26H27N5O2
分子量 441.525
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
动物实验配方
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