TCS-OX2-29 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the

orexin receptor The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (, ). Both orexin receptors exhibit ...

subtype OX₂, with an IC₅₀ of 40nM and selectivity of around 250x for OX₂ over OX₁ receptors. Orexin antagonists are expected to be useful for the treatment of

insomnia Insomnia, also known as sleeplessness, is a sleep disorder where people have difficulty sleeping. They may have difficulty falling asleep, or staying asleep for as long as desired. Insomnia is typically followed by daytime sleepiness, low ene ...

, with subtype-selective antagonists such as TCS-OX2-29 potentially offering more specificity of action compared to non-selective orexin antagonists like almorexant.

References

Carboxamides Orexin antagonists Norsalsolinol ethers 4-Pyridyl compounds Sedatives Tert-butyl compounds {{sedative-stub