Vilazodone | EMD 68843 | Serotonin Reuptake Inhibitor | AmBeed-信号通路专用抑制剂

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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 is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.

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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

5-羟色胺受体亚型比较

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								{[allProObj[0].p_purity_real_show]}
Lamotrigine	+ 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								{[allProObj[0].p_purity_real_show]}
Venlafaxine	✔								{[allProObj[0].p_purity_real_show]}
Fluvoxamine maleate	✔								{[allProObj[0].p_purity_real_show]}
Iloperidone	✔								{[allProObj[0].p_purity_real_show]}
Ziprasidone HCl	✔								{[allProObj[0].p_purity_real_show]}
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								{[allProObj[0].p_purity_real_show]}
Dapoxetine HCl	✔								{[allProObj[0].p_purity_real_show]}
Trazodone	✔								{[allProObj[0].p_purity_real_show]}
Clomipramine HCl	✔								{[allProObj[0].p_purity_real_show]}
Mirtazapine	✔								{[allProObj[0].p_purity_real_show]}
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								{[allProObj[0].p_purity_real_show]}
Duloxetine	✔								{[allProObj[0].p_purity_real_show]}
Sertraline HCl	++ 5-HT, Ki: 13 nM								{[allProObj[0].p_purity_real_show]}
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								{[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl	✔							GluR	{[allProObj[0].p_purity_real_show]}
Fluoxetine HCl	✔								{[allProObj[0].p_purity_real_show]}
Paroxetine hydrochloride	✔							AChR	{[allProObj[0].p_purity_real_show]}
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						{[allProObj[0].p_purity_real_show]}
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						{[allProObj[0].p_purity_real_show]}
LY310762		+ 5-HT1D, Ki: 249 nM							{[allProObj[0].p_purity_real_show]}
Cyclobenzaprine HCI			✔						{[allProObj[0].p_purity_real_show]}
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						{[allProObj[0].p_purity_real_show]}
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						{[allProObj[0].p_purity_real_show]}
Olanzapine			✔						{[allProObj[0].p_purity_real_show]}
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						{[allProObj[0].p_purity_real_show]}
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						{[allProObj[0].p_purity_real_show]}
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						{[allProObj[0].p_purity_real_show]}
Agomelatine			✔						{[allProObj[0].p_purity_real_show]}
Clozapine			✔						{[allProObj[0].p_purity_real_show]}
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	{[allProObj[0].p_purity_real_show]}
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						{[allProObj[0].p_purity_real_show]}
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						{[allProObj[0].p_purity_real_show]}
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						{[allProObj[0].p_purity_real_show]}
Tropisetron				✔					{[allProObj[0].p_purity_real_show]}
Palonosetron				✔					{[allProObj[0].p_purity_real_show]}
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					{[allProObj[0].p_purity_real_show]}
Ondansetron				✔					{[allProObj[0].p_purity_real_show]}
Granisetron				✔					{[allProObj[0].p_purity_real_show]}
Alosetron HCl				✔					{[allProObj[0].p_purity_real_show]}
Ondansetron hydrochloride dihydrate				✔					{[allProObj[0].p_purity_real_show]}
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					{[allProObj[0].p_purity_real_show]}
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
Risperidone		++ 5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM	++++ 5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		{[allProObj[0].p_purity_real_show]}
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			{[allProObj[0].p_purity_real_show]}
Intepirdine						++++ 5-HT6, pKi: 9.63			{[allProObj[0].p_purity_real_show]}
SB-269970 HCl							++ 5-HT7, pKi: 8.3		{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
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

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

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

动物实验配方

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	-	-
NCT01469377	-		Completed	-	-
NCT02883660	-		Completed	-	United States, Pennsylvania ... 展开 >> Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT02893371	-		Enrolling by invitation	June 2019	United States, New Mexico ... 展开 >> Christophe G Lambert Albuquerque, New Mexico, United States, 87131 收起 <<
NCT00290914	Major Depressive Disorder	Phase 2	Completed	-	-
NCT01473381	Major Depressive Disorder	Phase 4	Completed	-	-
NCT00683592	Major Depressive Disorder	Phase 3	Completed	-	United States, California ... 展开 >> Pharmacology Research Institute Newport Beach, California, United States, 92660 United States, Florida Florida Clinical Research Center Bradenton, Florida, United States, 34208 United States, Georgia Atlanta Institute of Medicine and Research Atlanta, Georgia, United States, 30328 United States, Oregon Summit Research Network Portland, Oregon, United States, 97210 United States, Pennsylvania University of Pennsylvania Department of Psychiatry Mood and Anxiety Disorders Philadelphia, Pennsylvania, United States, 19104 United States, Texas Mood Disorders Research Program and Clinic Exchange Park Dallas, Texas, United States, 75235 United States, Utah University of Utah Health Sciences Ctr, Dept of Psychiatry Mood Disorders Clinic Salt Lake City, Utah, United States, 84132 United States, Washington Northwest Clinical Research Center Bellevue, Washington, United States, 98004 Summit Research Network Seattle, Washington, United States, 98104 收起 <<
NCT01473381	-		Completed	-	-
NCT01629966	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT00285376	Depressive Disorder, Major	Phase 3	Completed	-	United States, California ... 展开 >> Pharmacology Research Institute Los Alamitos, California, United States, 90720 Pharmacology Research Institute Newport Beach, California, United States, 92660 Pharmacology Research Institute Northridge, California, United States, 91324 Pharmacology Research Institute Riverside, California, United States, 92506 United States, Georgia Atlanta Institute of Medicine & Research Atlanta, Georgia, United States, 30328 Atlanta Institute of Medicine & Research Marietta, Georgia, United States, 30060 United States, Michigan Summit Research Network (Michigan), Inc. Farmington Hills, Michigan, United States, 48336 Summit Research Network (Michigan), Inc. Flint, Michigan, United States, 48507 United States, New York Social Psychiatry Research Institute Brooklyn, New York, United States, 11235 United States, Oregon Summit Research Network (Oregon) Inc. Portland, Oregon, United States, 97210 United States, Pennsylvania University of Pennsylvania Department of Psychiatry Mood and Anxiety Disorders Section Philadelphia, Pennsylvania, United States, 19104-3309 United States, South Carolina Southeast Health Consultants, LLC Charleston, South Carolina, United States, 29407 United States, Utah University of Utah health Services Center Dept. of Psychiatry Mood and Anxiety Disorders Salt Lake City, Utah, United States, 84132 United States, Washington Northwest Clinical Research Center Bellevue, Washington, United States, 98004 Summit Research Network (Seattle) LLC Seattle, Washington, United States, 98104 收起 <<
NCT02372799	Major Depressive Disorder	Phase 3	Completed	-	-
NCT02097147	Healthy	Phase 1	Completed	-	United States, Florida ... 展开 >> Forest Investigative Site 001 Miami, Florida, United States, 33014 United States, Kansas Forest Investigative Site 002 Overland Park, Kansas, United States, 66212 United States, Minnesota Forest Investigative Site 003 St. Paul, Minnesota, United States, 55114 United States, Virginia Forest Investigative Site 004 Charlottesville, Virginia, United States, 22903 收起 <<
NCT00644358	Major Depressive Disorder	Phase 3	Completed	-	-
NCT00644358	-		Completed	-	-
NCT01742832	Major Depressive Disorder	Phase 2	Completed	-	United States, Illinois ... 展开 >> University of Chicago Chicago, Illinois, United States, 60615 收起 <<
NCT01742832	-		Completed	-	-
NCT01680900	-		Completed	-	-
NCT01608295	-		Completed	-	-
NCT01573598	Major Depressive Disorder	Phase 4	Completed	-	-
NCT00683592	-		Completed	-	-
NCT01574183	Marijuana Dependence	Phase 2	Completed	-	United States, South Carolina ... 展开 >> Medical University of South Carolina Charleston, South Carolina, United States, 29425 收起 <<
NCT01574183	-		Completed	-	-
NCT01766401	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT01473394	Major Depressive Disorder	Phase 4	Completed	-	United States, California ... 展开 >> Forest Investigative Site 009 Beverly Hills, California, United States, 90210 Forest Investigative Site 003 Encino, California, United States, 91316 Forest Investigative Site 010 New port Beach, California, United States, 92660 United States, Florida Forest Investigative Site 005 Jacksonville, Florida, United States, 32216 Forest Investigative Site 004 Orlando, Florida, United States, 32806 United States, Georgia Forest Investigative Site 012 Atlanta, Georgia, United States, 30328 United States, Maryland Forest Investigative Site 001 Baltimore, Maryland, United States, 21285 United States, Ohio Forest Investigative Site 002 Dayton, Ohio, United States, 45417 United States, Pennsylvania Forest Investigative Site 011 Philadelphia, Pennsylvania, United States, 19104 United States, Rhode Island Forest Investigative Site 015 Lincoln, Rhode Island, United States, 02865 United States, Tennessee Forest Investigative Site 008 Memphis, Tennessee, United States, 38119 United States, Texas Forest Investigative Site 016 San Antonio, Texas, United States, 78229 United States, Washington Forest Investigative Site 006 Bellevue, Washington, United States, 98007 Forest Investigative Site 013 Seattle, Washington, United States, 98104 收起 <<
NCT01828515	Memory Impairment	Phase 2	Completed	-	United States, Texas ... 展开 >> UT Southwestern Medical Center Dallas, Texas, United States, 75390 收起 <<
NCT01680900	Hot Flushes	Not Applicable	Completed	-	United States, Pennsylvania ... 展开 >> Dept OB/GYN, Mudd Professorship Suite Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT01878292	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01608295	Major Depressive Disorder	Phase 4	Completed	-	United States, California ... 展开 >> UCLA Semel Institute Los Angeles, California, United States, 90095 收起 <<
NCT01828515	-		Completed	-	-
NCT01473394	-		Completed	-	-
NCT02028026	Major Depressive Disorder ... 展开 >> Anxiety Comorbidity 收起 <<	Phase 4	Withdrawn(Inability to recruit... 展开 >> eligible subjects) 收起 <<	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 收起 <<
NCT01999920	-		Completed	-	-
NCT01844115	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT01712321	Social Anxiety Disorder	Not Applicable	Unknown	April 2014	United States, New York ... 展开 >> The Medical Research Network, LLC New York, New York, United States, 10128 收起 <<
NCT01715519	PTSD Depressi... 展开 >>on 收起 <<	Phase 4	Completed	-	United States, California ... 展开 >> Veterans Affairs Long Beach Healthcare System Long Beach, California, United States, 90822 United States, Nebraska Veterans Affairs Nebraska Western-Iowa Healthcare Systems Omaha, Nebraska, United States, 68105 收起 <<
NCT02015546	Major Depressive Disorder (MDD... 展开 >>) 收起 <<	Phase 3	Completed	-	United States, North Carolina ... 展开 >> Duke University Medical Center / Civitan Building Durham, North Carolina, United States, 27705 收起 <<
NCT01856127	Sexual Dysfunction ... 展开 >> Major Depressive Disorder 收起 <<	Phase 4	Terminated(PI left institution... 展开 >>) 收起 <<	-	United States, Pennsylvania ... 展开 >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 United States, Virginia University of Virginia Charlottesville, Virginia, United States, 22908 收起 <<
NCT02436239	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01999920	Separation Anxiety Disorder	Phase 4	Completed	-	United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
NCT02015546	-		Completed	-	-

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

Vilazodone 纯度/质量文件产品仅供科研

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Vilazodone 质控信息

Vilazodone 生物活性

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Vilazodone 参考文献

Vilazodone 实验方案

Vilazodone 技术信息

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

Vilazodone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Vilazodone 质控信息

Vilazodone 生物活性

Vilazodone 临床研究

Vilazodone 参考文献

Vilazodone 实验方案

Vilazodone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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细胞研究

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Vilazodone 纯度/质量文件产品仅供科研