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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *