RTIOX-276
Orexin antagonist
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CompTox Dashboard (EPA) |
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Chemical and physical data | |
Formula | C29H32F3N3O5 |
Molar mass | 559.586 g·mol−1 |
3D model (JSmol) |
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RTIOX-276 is an orexin antagonist. RTIOX-276 binds selectively to the orexin 1 receptor (KE = 8.5nM) and lacks significant affinity for the orexin 2 receptor (KE = > 10,000nM). RTIOX-276 may have therapeutic utility for the treatment of cocaine addiction. In conditioned place preference studies, RTIOX-276 attenuated the development of place preference in mice exposed to cocaine.[1][2][3]
References
- ^ Perrey DA, German NA, Gilmour BP, Li JX, Harris DL, Thomas BF, Zhang Y (September 2013). "Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Journal of Medicinal Chemistry. 56 (17): 6901–16. doi:10.1021/jm400720h. PMC 3849818. PMID 23941044.
- ^ Perrey DA, Decker AM, Li JX, Gilmour BP, Thomas BF, Harris DL, et al. (September 2015). "The importance of the 6- and 7-positions of tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Bioorganic & Medicinal Chemistry. 23 (17): 5709–24. doi:10.1016/j.bmc.2015.07.013. PMC 4554834. PMID 26216017.
- ^ Perrey DA, German NA, Decker AM, Thorn D, Li JX, Gilmour BP, et al. (April 2015). "Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor". ACS Chemical Neuroscience. 6 (4): 599–614. doi:10.1021/cn500330v. PMC 4400266. PMID 25643283.
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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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