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
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SB-334867
CAS number：249889-64-3 molecular formula：C17H14ClN5O2
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| Chinese alias | SB-334867 hydrochloride | ||
| English alias | 1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea | SB334867 | SB-334867 | SB-334867 free base | SB 334867 | 1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea | C17H13N5O2 | SB334867A free base | SB-334867 (free base) | SB-334867 | ||
| CAS number | 249889-64-3 | molecular formula | C17H14ClN5O2 |
| molecular weight | 355.78 g/mol | Exact mass | - |
| PSA | 92.900 Ų | logp | 2.000 |
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