Products
Almorexant is not commercially available. Clinical development was discontinued by Actelion and GlaxoSmithKline (GSK) in 2011 due to adverse effects.
Structure and properties
Almorexant (C29H31F3N2O3, Mr = 512.6 g/mol) is a tetrahydroisoquinoline derivative. It is structurally related to the opioid methopholine.
Effects
Almorexant has sleep-inducing properties. It is a selective and dual antagonist at the orexin receptors OX1R and OX2R. It blocks the binding of the neuropeptides orexin A and orexin B, produced in the hypothalamus of neurons, to their receptors. This system is partly responsible for promoting wakefulness.
Indications
Almorexant was intended for the treatment of sleep disorders.