| 产品描述: | Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA) |
| 靶点: |
H1 Receptor;H3 receptor;HistamineReceptor |
| 体内研究: |
Betahistine (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice.Betahistine (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice. Animal Model: Collagen-induced arthritis (CIA) DBA/1 male mouse model Dosage: 1 mg/kg; 5mg/kg Administration: Oral adminstration; day 21 to day 42 after a 21-day CIA induction Result: Ameliorated mouse CIA by decreasing joint destruction. |
| 参考文献: |
1. Poyurovsky M, et al. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. 2. Gbahou F, et al. Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54. 3. Tang KT, et al. Betahistine attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
7.343 ml |
36.713 ml |
73.427 ml |
| 5 mM |
1.469 ml |
7.343 ml |
14.685 ml |
| 10 mM |
0.734 ml |
3.671 ml |
7.343 ml |
| 50 mM |
0.147 ml |
0.734 ml |
1.469 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。 |