TCS-OX2-29
Orexin antagonist
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Formula | C23H31N3O3 |
Molar mass | 397.519 g·mol−1 |
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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]
References
- ^ 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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Orexin receptor modulators
- Agonists: AEX-5
- AEX-19
- AEX-24
- Orexin (A, B)
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- AZD-4041
- C4X-3256 (INDV-2000)
- CR-5542
- CVN-766
- Daridorexant
- Fazamorexant (YZJ-1139)
- Filorexant
- GSK-649868 (SB-649868)
- Lemborexant
- Nivasorexant (ACT-539313)
- RTIOX-276
- SB-334867
- SB-408124
- Suvorexant
- TCS-1102
- Tebideutorexant (JNJ-61393215)
- Vornorexant (ORN-0829, TS-142)
- Agonists: AEX-19
- ALKS-2680
- Danavorexton (TAK-925)
- E-2086
- Firazorexton (TAK-994)
- Orexin (A, B)
- Oveporexton
- SB-668875
- Suntinorexton (TAK-861)
- Antagonists: ACT-335827
- ACT-462206
- Almorexant
- Daridorexant
- EMPA
- Fazamorexant (YZJ-1139)
- Filorexant
- GSK-649868 (SB-649868)
- JNJ-10397049
- Lemborexant
- MK-1064
- MK-3697
- MK-8133
- Seltorexant
- Suvorexant
- TCS-1102
- TCS-OX2-29
- Vornorexant (ORN-0829, TS-142)
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