Almorexant

A dual Orexin receptor OX1/OX2 antagonist with Ki of 1.3/0.17 nM for hOX1/hOX2 respectively; selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+ mobilization.Sleep Disorder Phase 3 Discontinued (In Vitro) :Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex.Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells. (In Vivo) :Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors.Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning.Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance.