| 产品描述: | AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM. |
| 靶点: |
5-HT1A Receptor:94 nM (IC50, in human); 5-HT1A Receptor;5-HT1A Receptor:135 nM (IC50, in rat); 5-HT1B Receptor:254 nM (IC50, in rat) |
| 体外研究: |
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[1]. |
| 体内研究: |
AP521 is an agonist of human 5-HT1A receptor with IC50s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT1A (rat), 5-HT1A (human), 5-HT1B (rat), 5-HT1B (human), 5-HT1D (human), 5-HT5a (human) and 5-HT7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM. |
| 保存条件: |
-80°C 12个月; -20°C 6个月,干燥, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.482 ml |
12.41 ml |
24.821 ml |
| 5 mM |
0.496 ml |
2.482 ml |
4.964 ml |
| 10 mM |
0.248 ml |
1.241 ml |
2.482 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.496 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |