Pardoprunox
| 中文名称 | Pardoprunox |
|---|---|
| 中文同义词 | 帕多芦诺 |
| 英文名称 | Pardoprunox |
| 英文同义词 | Pardoprunox;DU 126891;pardoprunox (SLV308);SLV-308;SLV-308; DU-126891;Pardoprunox，DU 126891;7-(4-Methyl-1-piperazinyl)-2(3H)-benzoxazolone;7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one |
| CAS号 | 269718-84-5 |
| 分子式 | C12H15N3O2 |
| 分子量 | 233.27 |
| EINECS号 | 604-604-1 |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 269718-84-5.mol |
| 结构式 |  |
Pardoprunox 性质
| 密度 | 1.258±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.15±0.70(Predicted) |
|
5-HT 1A Receptor 6.3 (pEC 50 ) |
D 2 Receptor 8 (pEC 50 ) |
D 3 Receptor 9.2 (pEC 50 ) |
Pardoprunox (SLV-308) acts as a potent but partial D2 receptor agonist (pEC 50 = 8.0 and pA 2 =8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC 50 =9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA 2 =9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC 50 =6.3).