产品
编 号：F196629
分子式：C26H27N5O2
分子量：441.52
分子式：C26H27N5O2
分子量：441.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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50mg
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结构图
CAS No: 163521-12-8
产品详情
生物活性：
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active?serotonin?reuptake inhibitor (SSRI) and partial?5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
体内研究：
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.
体外研究：
Vilazodone shows an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT1A?receptors, and it displays high affinity (pKi≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A?receptors.Vilazodone acts as a high efficacy partial agonist at 5-HT1A?receptors. In [35S]GTPγS binding studies in Sf9 cells expressing h5-HT1A?receptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT1A?receptor agonist, 8‐OH‐PIPAT.In [35S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5‐HT1A?receptor partial agonist with a pEC50?of 8.1 and an intrinsic activity of 0.61.Vilazodone acts as a potent 5‐HT reuptake inhibitor in rat and guinea pig cortex. In LLCPK cells expressing human SERT, whereby vilazodone inhibits [3H]5‐HT uptake with a pIC50?of 8.8.
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active?serotonin?reuptake inhibitor (SSRI) and partial?5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
体内研究：
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.
体外研究：
Vilazodone shows an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT1A?receptors, and it displays high affinity (pKi≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A?receptors.Vilazodone acts as a high efficacy partial agonist at 5-HT1A?receptors. In [35S]GTPγS binding studies in Sf9 cells expressing h5-HT1A?receptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT1A?receptor agonist, 8‐OH‐PIPAT.In [35S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5‐HT1A?receptor partial agonist with a pEC50?of 8.1 and an intrinsic activity of 0.61.Vilazodone acts as a potent 5‐HT reuptake inhibitor in rat and guinea pig cortex. In LLCPK cells expressing human SERT, whereby vilazodone inhibits [3H]5‐HT uptake with a pIC50?of 8.8.
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