产品
编 号：F292259
分子式：C17H14ClN5O2
分子量：355.78
分子式：C17H14ClN5O2
分子量：355.78
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
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询价
结构图
CAS No: 249889-64-3
产品详情
生物活性：
SB-334867 (SB 334867A) 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.
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.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 lowerblood 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.
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.
SB-334867 (SB 334867A) 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.
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.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 lowerblood 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.
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.
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