Chemistry:RTIOX-276
From HandWiki
Short description: Orexin antagonist
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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
- ↑ "Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Journal of Medicinal Chemistry 56 (17): 6901–16. September 2013. doi:10.1021/jm400720h. PMID 23941044.
- ↑ "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. September 2015. doi:10.1016/j.bmc.2015.07.013. PMID 26216017.
- ↑ "Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor". ACS Chemical Neuroscience 6 (4): 599–614. April 2015. doi:10.1021/cn500330v. PMID 25643283.
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