Description
An OX1R and OX2R dual antagonist (Kis = 2.5 and 0.31 nM, respectively, for the recombinant human receptors); selectively inhibits OX1R and OX2R over a panel of >170 receptors and enzymes; inhibits orexin A-induced calcium mobilization in CHO cells expressing recombinant human OX1R or OX2R (Kb = 11 nM for both); decreases locomotor activity in rats during the dark cycle at 10 mg/kg; reduces the time spent awake and decreases the latency to SWS1 and SWS2, but not REM sleep, in dogs at 0.5 mg/kg; increases the duration of SWS2, but not SWS1 or REM sleep, in the same model
Formal name: [(2R,5R)-5-[[(5-fluoro-2-pyridinyl)oxy]methyl]-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]-methanone
Synonyms:
Molecular weight: 420.5
CAS: 1088991-73-4
Purity: ≥98%
Formulation: A solid
