| 产品描述: | GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia |
| 靶点: |
5-HT1D Receptor;5-HTReceptor |
| 体外研究: |
GR-46611 (1 μM, 48 h) induces CEM cell proliferation. Cell Proliferation Assay Cell Line: CEM cells (human T lymphoblastic leukemia cell line) Concentration: 1 μM Incubation Time: 48 h Result: Induced a significant increase in cell proliferation by 37.0%. |
| 体内研究: |
GR-46611 (1 mg/kg, i.p. ) significantly improves survival of Dravet syndrome (DS) mice. GR-46611 (0.03-300 μg/kg, i.v.) increases threshold volume, bladder capacity, and residual volume in chronic spinal cord injury (SCI) cats. GR46611 (3-30 mg/kg, s.c.) causes a dose-related decrease in rectal temperature in the adult guinea-pig. Animal Model: Dravet syndrome (DS) mice Dosage: 0.01, 0.1 and 1 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Improved survival relative to vehicle treated controls with 89% surviving rate. |
| 参考文献: |
1. Paul G Hatini, et al. A 5-HT 1D -receptor agonist protects Dravet syndrome mice from seizure and early death. Eur J Neurosci. 2020 Nov;52(10):4370-4374. 2. C Sibella-Argüelle, et al. The proliferation of human T lymphoblastic cells induced by 5-HT1B receptors activation is regulated by 5-HT-moduline. C R Acad Sci III. 2001 Apr;324(4):365-72. 3. Baojun Gu, et al. Inhibition of bladder activity by 5-hydroxytryptamine1 serotonin receptor agonists in cats with chronic spinal cord injury. J Pharmacol Exp Ther. 2004 Sep;310(3):1266-72. 4. M Skingle, et al. Stimulation of central 5-HT1D receptors causes hypothermia in the guinea-pig. J Psychopharmacol. 1994 Jan;8(1):14-21. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.649 ml |
13.245 ml |
26.491 ml |
| 5 mM |
0.53 ml |
2.649 ml |
5.298 ml |
| 10 mM |
0.265 ml |
1.325 ml |
2.649 ml |
| 50 mM |
0.053 ml |
0.265 ml |
0.53 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。 |