| 产品描述： | Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation. |
| 靶点： |
5-HT2A Receptor：8.64 (pKi)；5-HT2B Receptor：8.75 (pKi)；5-HT2C Receptor：8.75 (pKi)；Human 5-HT7 Receptor：16 nM (Ki) |
| 体内研究： |
Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg) |
| 参考文献： |
1. Antony R Knight, et al. Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. 2. Jessica A. Knight, et al. Pharmacological Analysis of the Novel, Rapid, and Potent Inactivation of the Human 5-Hydroxytryptamine7 Receptor by Risperidone, 9-OH-Risperidone, and Other Inactivating Antagonists. Mol Pharmacol. 2009 Feb; 75(2): 374-380. 3. Jun-ho Lee, et al. Metergoline inhibits the neuronal Nav1.2 voltage-dependent Na+ channels expressed in Xenopus oocytes. Acta Pharmacol Sin. 2014 Jul; 35(7): 862-868. 4. P K Eide, et al. The behavioural response to intrathecal serotonin is changed by acute but not by repeated treatment with zimelidine or metergoline. Pharmacol Toxicol. 1991 Nov;69(5):361-4. |
| 溶解性： |
DMSO : 125 mg/mL (309.77 mM; Need ultrasonic) |
| 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 |
2.478 ml |
12.391 ml |
24.782 ml |
| 5 mM |
0.496 ml |
2.478 ml |
4.956 ml |
| 10 mM |
0.248 ml |
1.239 ml |
2.478 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。 |
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