| Description | Almorexant hydrochloride (ACT-078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. |
| In vitro | Almorexant在中华仓鼠卵巢细胞中，通过10 nM人源性orexin-A诱导的细胞内Ca2+增加中表现出抑制作用，对OX1受体的IC50为16 nM（大鼠）和13 nM（人），对OX2受体的IC50为15 nM（大鼠）和8 nM（人）。[1] |
| In vivo | Almorexant (300 mg/kg p.o.) 在雄性Wistar大鼠中降低警觉性，并增加非REM睡眠和REM睡眠的电生理指标。在狗中，Almorexant (100 mg/kg p.o.) 引起嗜睡并增加REM睡眠的代理标志。[1] Almorexant 诱导出强烈的抗抑郁样效果，并独立于神经生成作用恢复与压力相关的HPA轴缺陷。[2] 此外，Almorexant 还在高饮酒的啮齿动物模型中减少乙醇自我给药。[3] |
| Target activity | OX2:0.17 nM(ki), OX1:1.3 nM(ki) |
| Synonyms | ACT-078573 hydrochloride, Almorexant HCl |
| molecular weight | 549.02 |
| Molecular formula | C29H32ClF3N2O3 |
| CAS | 913358-93-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | Ethanol: 48 mg/mL (87.4 mM) DMSO: 67 mg/mL (122 mM) H2O: <1 mg/mL |
| References | 1. Brisbare-Roch C, et al. Nat Med. 2007, 13(2), 150-155. 2. Nollet M, et al. Neuropsychopharmacology. 2012, 37(10), 2210-2221. 3. Anderson RI, et al. Front Neurosci. 2014, 8, 33. |