RTIOX-276
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Orexin antagonist
Pharmaceutical compound
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| Formula | C29H32F3N3O5 |
| Molar mass | 559.586 g·mol−1 |
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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年07月01日3. 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.
