SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, 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 SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Swiss miceDosage: 20 mg/kg Administration: Intraperitoneal injection Result: Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice. Animal Model: C57BL/6J MiceDosage: 3, 10 and 30 mg/kg Administration: Intraperitoneal injection Result: Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.
Form:Solid
IC50& Target:OX1
G2508527