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SB-334867

CAS No. : 249889-64-3

MCE 站：SB-334867

产品活性：SB-334867 (SB 334867A) 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(pK_b=7.4)，对 5-HT_2B、5-HT_2C 的选择性是 100 倍，pK_i 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敏感性。

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 pK_b 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.
SB334867 (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.
SB334867 (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.

相关产品：Orexin A (human, rat, mouse)  |  TCS-OX2-29  |  GSK1059865  |  SB-674042  |  TCS 1102  |  EMPA  |  SB-408124  |  Orexin B, human TFA  |  IPSU  |  SB-649868  |  Orexin B, rat, mouse  |  Orexin receptor antagonist 2  |  OXA(17-33)  |  [Ala11,D-Leu15]-Orexin B(human)

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