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.[1] Orexin antagonists are expected to be useful for the treatment of insomnia, with subtype-selective antagonists such as TCS-OX2-29 potentially offering more specificity of action compared to non-selective orexin antagonists like almorexant.[2]
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| Formula | C23H31N3O3 |
| Molar mass | 397.519 g·mol−1 |
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References
edit- ^ Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, et al. (December 2003). "N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist". Bioorganic & Medicinal Chemistry Letters. 13 (24): 4497–9. doi:10.1016/j.bmcl.2003.08.038. PMID 14643355.
- ^ Roecker AJ, Coleman PJ (2008). "Orexin receptor antagonists: medicinal chemistry and therapeutic potential". Current Topics in Medicinal Chemistry. 8 (11): 977–87. doi:10.2174/156802608784936746. PMID 18673167.
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