CAS NO: | 163521-12-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI)and partial 5-HT1A receptoragonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders[1][2]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Vilazodone shows an IC50of 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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[2].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[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 441.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H27N5O2 | ||||||||||||||||
CAS 号 | 163521-12-8 | ||||||||||||||||
中文名称 | 维拉佐酮 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 75 mg/mL(169.87 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用;
以下溶剂前显示的百
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