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Dr. Michel A. Steiner, Dr. John Gatfield, Dr. Catherine Brisbare-Roch, Dr. Hendrik Dietrich, Dr. Alexander Treiber, Dr. Francois Jenck and Dr. Christoph Boss Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist ChemMedChem 8

Article first published online: 15 APR 2013 | DOI: 10.1002/cmdc.201300003

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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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