SB-334867 (SB 334867A) 是一种优良的、选择性的、血脑屏障通透性的orexin-1 (OX1) receptor拮抗剂，对OX2具有选择性(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 降低乙醇消耗量并抑制吗啡诱导的体内运动活性的敏感性。

SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist. SB-334867 shows selectivity over OX2 ( pK b =7.4), 100-fold over 5-HT 2B, 5-HT 2C with pK i values of 5.4 and 5.3, respectively [1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo [2] [3].

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. SB-334867 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 [4].

SB-334867 (intraperitoneal injection; 20 mg/kg; 20 days) administers 15 min before morphine injection can significantly reduce the effect of the morphine challenge dose in mice in comparison with the sporadically morphine-treated group [2].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 [3].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 [3]. Animal Model: Male Swiss mice [2] 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 [3] Dosage: 3, 10 and 30 mg/kg Administration: Intraperitoneal injection Result: Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.

249889-64-3

C17H14ClN5O2

355.78

SB334867 HCl

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years