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Vilazodone

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Chemical Structure| 163521-12-8 同义名 : EMD 68843;SB659746A
CAS号 : 163521-12-8
货号 : A913265
分子式 : C26H27N5O2
纯度 : 98%
分子量 : 441.525
MDL号 : MFCD09838919
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：
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 ... 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 - -
实验方案
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
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