化合物 AP521
| 中文名称 | 化合物 AP521 |
|---|---|
| 中文同义词 | 化合物 T10344;化合物 AP521;AP521试剂;AP521试剂 |
| 英文名称 | AP521 |
| 英文同义词 | AP521;AP521,AP-521;N-(1,3-Benzodioxol-5-ylmethyl)-1,2,3,4-tetrahydro-[1]benzothiolo[2,3-c]pyridine-3-carboxamide hydrochloride |
| CAS号 | 151227-08-6 |
| 分子式 | C20H19ClN2O3S |
| 分子量 | 402.89 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 151227-08-6.mol |
| 结构式 |  |
化合物 AP521 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
|
5-HT 1A Receptor 94 nM (IC 50 , in human) |
5-HT 1A Receptor 135 nM (IC 50 , in rat) |
5-HT 1B Receptor 254 nM (IC 50 , in rat) |
5-HT 1B Receptor 5530 nM (IC 50 , in human) |
5-HT 1D Receptor 418 nM (IC 50 , in human) |
5-HT 5A Receptor 422 nM (IC 50 , in human) |
5-HT 7 Receptor 198 nM (IC 50 , in rat) |
AP521 is an agonist of human 5-HT 1A receptor with IC 50 s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT 1A (rat), 5-HT 1A (human), 5-HT 1B (rat), 5-HT 1B (human), 5-HT 1D (human), 5-HT 5a (human) and 5-HT 7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM.
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-100166 | 151227-08-6 AP521 | 151227-08-6 | 5 mg | 1700元 |
| 2025/12/22 | HY-100166 | 化合物 AP521 AP521 | 151227-08-6 | 10 mM * 1 mLin DMSO | 1870元 |