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SB-334867
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SB-334867图片
CAS NO: 249889-64-3
包装与价格：
包装 价格(元)
5mg 电议
10mg 电议
50mg 电议
100mg 电议

半岛bd体育手机客户端 名称
SB 334867A
半岛bd体育手机客户端 介绍
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( pKb=7.4)，对 5-HT 2B、5-HT 2C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敏感性。
生物活性

SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeableorexin-1 (OX1) receptorantagonist, shows selectivity overOX2(pKb=7.4), 100-fold over 5-HT2B, 5-HT2CwithpKivalues 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].
IC50& Target[1]

OX1
体外研究
(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 pKbvalues 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[4].
体内研究
(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[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.
分子量

355.78
性状

Solid
Formula

C17H14ClN5O2
CAS 号

249889-64-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vivo:
  • 1.

    SB-334867 is dissolved in the aCSF (in mM: 133.3 NaCl, 3.4 KCl, 1.3 CaCl2, 1.2 MgCl2, 0.6 NaH2PO4, 32.0 NaHCO3, and 3.4 glucose, with pH adjusted to 7.4)[5].
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