372163-84-3
物理化学性质
| 沸点 | 395.2±32.0 °C(Predicted) |
| 密度 | 1.28±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 8.95±0.10(Predicted) |
| 形态 | Oil |
| 颜色 | Light yellow to brown |
常见问题列表
|
5-HT 2A Receptor 13 nM (Ki) |
5-HT 2B Receptor 2.5 nM (Ki) |
5-HT 2C Receptor 0.89 nM (Ki) |
5-HT 2A Receptor 93 nM (EC 50 ) |
5-HT 2B Receptor 3.2 nM (EC 50 ) |
5-HT 2C Receptor 1 nM (EC 50 ) |
YM348 has high affinity for cloned human 5-HT 2C receptors with a K i value of 0.89 nM and lower affinities for human-cloned 5-HT 2B (K i : 2.5 nM) and 5-HT 2A receptors (K i : 13 nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC 50 values of YM348 are found to be >1 μM for all of the binding sites except for the human 5-HT 1A receptors (K i : 130 nM), bovine 5-HT 1D receptors (K i : 481 nM), human 5-HT 7 receptors (K i : 177 nM), and human α 2A receptors (K i : 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT 2A and 5-HT 2B receptors. The EC 50 values of YM348 for 5-HT 2C , 5-HT 2A , and 5-HT 2B receptors are 1.0, 93 and 3.2 nM, respectively.
Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT 2C receptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg.