1-(2-甲基苯并[D]噁唑-6-基)-3-(1,5-萘啶-4-基)脲

SB-334867 是一种选择性 orexin-1 (OX1) receptor 拮抗剂。 In CHO-OX1 cells, SB-334867 inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses with pKB of 7.27 and 7.23 respectively, without effect on the UTP (3 microM)-induced calcium response. In both male and female rats, SB-334867 (30 mg/kg, i.p.) significantly reduces natural and orexin-A-induced food intake. SB-334867 (2 mg/kg, i.v.) blocks the effects of antipsychotic drugs on dopamine neuronal activity in rats. SB-334867 also inhibits the development of morphine analgesic tolerance in rats. SB-334867 是一种选择性 orexin-1 (OX1) receptor 拮抗剂。

Target	Value
OX1 receptor

在CHO-OX1细胞，SB-334867抑制orexin-A (10 nM)和orexin-B (100 nM)诱导的钙响应，pKB 分别为7.27 和7.23，对UTP (3 microM)诱导的钙反应没有作用。

在雄性和雌性大鼠体内，SB-334867 (30 mg/kg, i.p.)显著减少天然和orexin-A诱导的食物摄入。 在大鼠体内，867 (2 mg/kg, i.v.)阻断抗精神病药对多巴胺神经元活性的作用。在大鼠体内，SB-334867也会抑制吗啡镇痛耐受性的发展。