中文名 | 维拉佐酮 |
英文名 | Vilazodone |
别名 | 维拉唑酮 维拉佐酮 盐酸维拉佐酮 维拉唑酮杂质 维拉佐酮盐酸盐 维拉佐酮(游离碱) 盐酸维拉佐酮C10 甲基-2H-异吲哚-1,3-二酮 5-(4-(4-(5-氰基-1H-吲哚-3-基)丁基)哌嗪-1-基)苯并呋喃-2-甲酰胺 |
英文别名 | CS-108 VIIBRYD Vilazodone Vilazodonei UNII-S239O2OOV3 Verazodone hydrochloride 5-(4-(4-(5-Cyanoindol-3-yl)butyl)-1-piperazinyl)-2-benzofurancarboxamide 5-(4-(4-(5-Cyano-1H-indol-3-yl)butyl)piperazin-1-yl)benzofuran-2-carboxamide 5-(4-[4-(5-CYANO-1H-INDOL-3-YL)BUTYL]PIPERAZIN-1-YL)BENZOFURAN-2-CARBOXAMIDE 2-BenzofurancarboxaMide,5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]- 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl]-1-benzofuran-2-carboxamide Vilazodone 5-[4-[4-(5-Cyanoindol-3-yl)butyl]piperazin-1-yl]benzofuran-2-carboxamide |
CAS | 163521-12-8 |
EINECS | 1308068-626-2 |
化学式 | C26H27N5O2 |
分子量 | 441.52 |
密度 | 1.34±0.1 g/cm3(Predicted) |
熔点 | 203-205°C |
沸点 | 745.1±60.0 °C(Predicted) |
溶解度 | DMSO (微溶)) 、甲醇 (微溶) |
酸度系数 | 15.98±0.30(Predicted) |
存储条件 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
稳定性 | 非常吸湿 |
外观 | 固体 |
颜色 | Pale Yellow to Beige |
体外研究 | Vilazodone shows an IC 50 of 0.2 nM at the human 5-HT 1 A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT 1 Areceptors, and it displays high affinity (pK i ≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT 1A receptors.Vilazodone acts as a high efficacy partial agonist at 5-HT 1 Areceptors. In [ 35 S]GTPγS binding studies in Sf9 cells expressing h5-HT 1 Areceptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT 1 Areceptor agonist, 8‐OH‐PIPAT. In [ 35 S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5‐HT 1A receptor partial agonist with a pEC 50 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 [ 3 H]5‐HT uptake with a pIC 50 of 8.8. |
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 vivomicrodialysis 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.265 ml | 11.325 ml | 22.649 ml |
5 mM | 0.453 ml | 2.265 ml | 4.53 ml |
10 mM | 0.226 ml | 1.132 ml | 2.265 ml |
5 mM | 0.045 ml | 0.226 ml | 0.453 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!