What is the mechanism of action of almorexant, the dual orexin receptor antagonist (DORA)?

Label:chem

Topic
Almorexant is the first dual orexin receptor antagonist (DORA) to be investigated in clinical studies. It decreases alertness and wakefulness in a dose-dependent manner and blocks both OX1 and OX2 receptors with almost equimolar potency.
Answer
Almorexant acts by blocking both orexin-1 (OX1) and orexin-2 (OX2) receptors, thereby reducing the effects of orexin-A and orexin-B. This blockade results in decreased alertness and wakefulness, promoting sleep. Almorexant has an IC50 of 16 nM and 15 nM for OX1 and OX2 receptors, respectively.
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