| 產品描述： | 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. |
| 靶點： |
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);DopamineReceptor;?5-HTReceptor;?SodiumChannel |
| 體內研究： |
Metergoline (5 mg/kg; i.p.) completely blocks the response to intrathecal 5-HT (2 μg) |
| 參考文獻： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京