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CAS No. : 792173-99-0
MCE 国际站:SB-334867 free base
产品活性:SB-334867 free base (SB334867A free base) 是一种优良的选择性血脑屏障通透性 orexin-1 (OX1) receptor 拮抗剂,对 OX2 有选择性 (pKb=7.4),对 5-HT2B、5-HT2C 的选择性是 100 倍,pKi 值分别为 5.4 和 5.3。SB-334867 降低体内乙醇消耗量,抑制吗啡诱导的对运动活性的增敏。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Orexin Receptor (OX Receptor)
In Vitro: 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.
In Vivo: 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.
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