| 产品描述： | GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases |
| 靶点： |
human 5-HT1B Receptor:8.85 (pKi);human 5-HT1D Receptor:8.31 (pKi);5-HTReceptor |
| 体外研究： |
GR 125743 has a Kd of 0.61 nM for h5-HT1B |
| 体内研究： |
GR 125743 (0.3 mg/kg; i.p.) produces significant decreases in extracellular 5-HT in the frontal cortex of the conscious guinea pig. Animal Model: Male Dunkin Hartley guinea-pigs (350-450 g) Dosage: 0.3 mg/kg Administration: Intraperitoneal injection Result: Produced significant transient increases in extracellular 5-HT. |
| 参考文献： |
1. T Wurch, et al. Induction of a high-affinity ketanserin binding site at the 5-Hydroxytryptamine(1B) receptor by modification of its carboxy-terminal intracellular portion. Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a nov 2. Roberts, C., et al. The role of 5-HT1B/1D receptors in the modulation of 5-hydroxytryptamine levels in the frontal cortex of the conscious guinea pig. European Journal of Pharmacology. 1997 May 12;326(1):23-30. |
| 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 |
2.401 ml |
12.004 ml |
24.008 ml |
| 5 mM |
0.48 ml |
2.401 ml |
4.802 ml |
| 10 mM |
0.24 ml |
1.2 ml |
2.401 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 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