RTIOX-276

RTIOX-276

RTIOX-276

Orexin antagonist

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]

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References

  1. [1]
    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.
  2. [2]
    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.
  3. [3]
    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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