SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeableorexin-1 (OX1) receptorantagonist, shows selectivity overOX2(pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2CwithpK_ivalues 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_bvalues 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].

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].

355.78

Solid

C₁₇H₁₄ClN₅O₂

249889-64-3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• 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].