| 产品描述： | SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo |
| 靶点： |
OX2;OXReceptor |
| 体外研究： |
SB-334867 (100 pM– 10 μM) inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses in a concentration-dependent manner, with apparent pKb values of 7.27±0.04 and 7.23±0.03, but has no effect on the calcium response elicited by UTP (3 μM), which activates an endogenous purinergic receptor in CHO-OX1 and CHO-OX2 cells |
| 体内研究： |
SB-334867 (intraperitoneal injection; 20 mg/kg; 20 days) administers 15 min before morphine injection can significantly decrease the effect of the morphine challenge dose in mice in comparison with the sporadically morphine-treated group. SB-334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) significantly reduces ethanol intake relative to vehicle and does not effect water consumption in female P rats. SB-334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) reduces ethanol consumption at the 30 mg/kg dose, high dose suppresses sucrose intake relative to vehicle, and it results in lower blood ethanol concentrations (BECs) relative to both the 10 and 30 mg/kg doses. Animal Model: Male Swiss mice Dosage: 20 mg/kg Administration: Intraperitoneal injection Result: Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice. Animal Model: C57BL/6J Mice Dosage: 3, 10 and 30 mg/kg Administration: Intraperitoneal injection Result: Reduced ethanol consumption, BECs and suppressed sucrose intake in mice. |
| 参考文献： |
1. Porter RA, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. 2. Łupina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms.Mol Neurobiol. 2018 Nov;55(11):8473-8485. 3. Anderson RI, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33. 4. Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist.Br J Pharmacol. 2001 Mar;132(6):1179-82. |
| 溶解性： |
Soluble in DMSO、0.1 M HCL |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.132 ml |
15.658 ml |
31.317 ml |
| 5 mM |
0.626 ml |
3.132 ml |
6.263 ml |
| 10 mM |
0.313 ml |
1.566 ml |
3.132 ml |
| 50 mM |
0.063 ml |
0.313 ml |
0.626 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