TCS-OX2-29 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor 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 in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, ...

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

almorexant Almorexant, also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treat ...

References

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