| 产品描述： | WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist |
| 靶点： |
5-HT6 Receptor:2.2 nM (Ki);5-HT6 Receptor:6.6 nM (EC50) |
| 体外研究： |
WAY181187 (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity. Western Blot Analysis Cell Line: HEK/HA-5-HT6 receptor cells Concentration: 1 and 10 μM Incubation Time: Pretreatment 5 minutes Result: Increased activation of ERK1/2 both at 1 and 10 μM concentrations. |
| 体内研究： |
Acute administration of WAY-181187 (3-30 mg/kg, s.c.) significantly increases extracellular GABA concentrations without altering the levels of glutamate or norepinephrine in the rat frontal cortex. Additionally, WAY-181187 (30 mg/kg, s.c.) produces modest yet significant decreases in cortical dopamine and 5-HT levels. Animal Model: Adult male Sprague-Dawley rats weighing 280–350 g Dosage: 3, 10, or 30 mg/kg Administration: Acute dministered by s.c. Result: Significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine. |
| 参考文献： |
1. Lee E Schechter, et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology. 2008 May;33(6):1323-35. 2. Teresa Riccioni, et al. ST1936 Stimulates cAMP, Ca2+, ERK1/2 and Fyn Kinase Through a Full Activation of Cloned Human 5-HT6 Receptors. Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.626 ml |
13.128 ml |
26.256 ml |
| 5 mM |
0.525 ml |
2.626 ml |
5.251 ml |
| 10 mM |
0.263 ml |
1.313 ml |
2.626 ml |
| 50 mM |
0.053 ml |
0.263 ml |
0.525 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京