| 产品描述: | L-AP4 (L-APB) 是一种有效的、代谢型谷氨酸受体 (mGluR) 的特异性激动剂,其对 mGlu4, mGlu8, mGlu6 和 mGlu7 受体的 EC50 值分别为 0.13, 0.29, 1.0, 249 μM。 |
| 靶点: |
mGlu4 0.13 μM (EC50); mGlu8 0.29 μM (EC50); mGlu6 1.0 μM (EC50); mGlu7 249 μM (EC50) |
| 体内研究: |
L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunction. Intrathecal injection of 30 μg of L-AP4 does not significantly alter the paw withdrawal latency in these normal rats. Topical application of 5 to 50 μM L-AP4 to the spinal cord significantly inhibited the evoked response of neurons to touch, pressure, pinch, and von Frey filaments in a concentration-dependent fashion. |
| 参考文献: |
1. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. 2. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6. |
| 保存条件: |
避光,-20℃,干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
5.461 ml |
27.307 ml |
54.615 ml |
| 5 mM |
1.092 ml |
5.461 ml |
10.923 ml |
| 10 mM |
0.546 ml |
2.731 ml |
5.461 ml |
| 50 mM |
0.109 ml |
0.546 ml |
1.092 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。 |