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CAS No.: 163521-12-8

Vilazodone/维拉佐酮 Catalog No. CSN12199

Synonyms: EMD 68843;SB659746A;维拉佐酮

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.

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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].
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 ... more >> Healthy Controls Collapse <<	Phase 4	Completed	-	United States, Georgia ... more >> Emory Mood and Anxiety Disorders Program Atlanta, Georgia, United States, 30322 Collapse <<
NCT01469377	Major Depressive Disorder	Phase 2	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2649 mL
- 11.3244 mL
- 22.6488 mL
- 5 mM
- 0.4530 mL
- 2.2649 mL
- 4.5298 mL
- 10 mM
- 0.2265 mL
- 1.1324 mL
- 2.2649 mL

技术信息

CAS号

163521-12-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27N5O2

运输

蓝冰

分子量

441.52

别名

EMD 68843;SB659746A;维拉佐酮

溶解度

DMSO	88.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	14.0 mg/mL (31.7 mM)

动物实验配方

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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 ... more >> Healthy Controls Collapse <<	Phase 4	Completed	-	United States, Georgia ... more >> Emory Mood and Anxiety Disorders Program Atlanta, Georgia, United States, 30322 Collapse <<
NCT01469377	Major Depressive Disorder	Phase 2	Completed	-	-
NCT01469377	-	-	Completed	-	-
NCT02883660	-	-	Completed	-	United States, Pennsylvania ... more >> Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 Collapse <<
NCT02893371	-	-	Enrolling by invitation	June 2019	United States, New Mexico ... more >> Christophe G Lambert Albuquerque, New Mexico, United States, 87131 Collapse <<
NCT00290914	Major Depressive Disorder	Phase 2	Completed	-	-
NCT01473381	Major Depressive Disorder	Phase 4	Completed	-	-
NCT00683592	Major Depressive Disorder	Phase 3	Completed	-	United States, California ... more >> 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 Collapse <<
NCT01473381	-	-	Completed	-	-
NCT01629966	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT00285376	Depressive Disorder, Major	Phase 3	Completed	-	United States, California ... more >> 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 Collapse <<
NCT02372799	Major Depressive Disorder	Phase 3	Completed	-	-
NCT02097147	Healthy	Phase 1	Completed	-	United States, Florida ... more >> 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 Collapse <<
NCT00644358	Major Depressive Disorder	Phase 3	Completed	-	-
NCT00644358	-	-	Completed	-	-
NCT01742832	Major Depressive Disorder	Phase 2	Completed	-	United States, Illinois ... more >> University of Chicago Chicago, Illinois, United States, 60615 Collapse <<
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 ... more >> Medical University of South Carolina Charleston, South Carolina, United States, 29425 Collapse <<
NCT01574183	-	-	Completed	-	-
NCT01766401	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT01473394	Major Depressive Disorder	Phase 4	Completed	-	United States, California ... more >> 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 Collapse <<
NCT01828515	Memory Impairment	Phase 2	Completed	-	United States, Texas ... more >> UT Southwestern Medical Center Dallas, Texas, United States, 75390 Collapse <<
NCT01680900	Hot Flushes	Not Applicable	Completed	-	United States, Pennsylvania ... more >> Dept OB/GYN, Mudd Professorship Suite Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT01878292	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01608295	Major Depressive Disorder	Phase 4	Completed	-	United States, California ... more >> UCLA Semel Institute Los Angeles, California, United States, 90095 Collapse <<
NCT01828515	-	-	Completed	-	-
NCT01473394	-	-	Completed	-	-
NCT02028026	Major Depressive Disorder ... more >> Anxiety Comorbidity Collapse <<	Phase 4	Withdrawn(Inability to recruit... more >> eligible subjects) Collapse <<	-	United States, Massachusetts ... more >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Collapse <<
NCT01999920	-	-	Completed	-	-
NCT01844115	Generalized Anxiety Disorder	Phase 3	Completed	-	-
NCT01712321	Social Anxiety Disorder	Not Applicable	Unknown	April 2014	United States, New York ... more >> The Medical Research Network, LLC New York, New York, United States, 10128 Collapse <<
NCT01715519	PTSD Depressi... more >>on Collapse <<	Phase 4	Completed	-	United States, California ... more >> 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 Collapse <<
NCT02015546	Major Depressive Disorder (MDD... more >>) Collapse <<	Phase 3	Completed	-	United States, North Carolina ... more >> Duke University Medical Center / Civitan Building Durham, North Carolina, United States, 27705 Collapse <<
NCT01856127	Sexual Dysfunction ... more >> Major Depressive Disorder Collapse <<	Phase 4	Terminated(PI left institution... more >>) Collapse <<	-	United States, Pennsylvania ... more >> 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 Collapse <<
NCT02436239	Major Depressive Disorder	Phase 3	Completed	-	-
NCT01999920	Separation Anxiety Disorder	Phase 4	Completed	-	United States, New York ... more >> New York State Psychiatric Institute New York, New York, United States, 10032 Collapse <<
NCT02015546	-	-	Completed	-	-

Vilazodone/维拉佐酮 Catalog No. CSN12199

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