Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.

@article{Steiner2013DiscoveryAC,
  title={Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.},
  author={Michel Alexander Steiner and John Gatfield and Catherine Brisbare-Roch and Hendrik Dietrich and Alexander Treiber and François Jenck and Christoph Boss},
  journal={ChemMedChem},
  year={2013},
  volume={8 6},
  pages={898-903}
}
Stress relief: Orexin neuropeptides regulate arousal and stress processing through orexin receptor type 1 (OXR-1) and 2 (OXR-2) signaling. A selective OXR-1 antagonist, represented by a phenylglycine-amide substituted tetrahydropapaverine derivative (ACT-335827), is described that is orally available, penetrates the brain, and decreases fear, compulsive behaviors and autonomic stress reactions in rats. 
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