RTIOX-276 explained

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]

Notes and References

  1. Perrey DA, German NA, Gilmour BP, Li JX, Harris DL, Thomas BF, Zhang Y . Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor . Journal of Medicinal Chemistry . 56 . 17 . 6901–16 . September 2013 . 23941044 . 10.1021/jm400720h . 3849818 .
  2. Perrey DA, Decker AM, Li JX, Gilmour BP, Thomas BF, Harris DL, Runyon SP, Zhang Y . 6 . 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 . 26216017 . 10.1016/j.bmc.2015.07.013 . 4554834 .
  3. Perrey DA, German NA, Decker AM, Thorn D, Li JX, Gilmour BP, Thomas BF, Harris DL, Runyon SP, Zhang Y . 6 . Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor . ACS Chemical Neuroscience . 6 . 4 . 599–614 . April 2015 . 25643283 . 10.1021/cn500330v . 4400266 .

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