T66082 |
GR-46611 |
源叶(MedMol) | 98% |
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)