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

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

  • ChemMedChem. 2013 Jun;8(6):898-903. doi: 10.1002/cmdc.201300003.
Michel A Steiner 1,  John Gatfield,  Catherine Brisbare-Roch,  Hendrik Dietrich,  Alexander Treiber,  Francois Jenck,  Christoph Boss
Affiliations

Affiliation

  • 1 Actelion Pharmaceuticals Ltd. Gewerbestrasse 16, 4123 Allschwil, Switzerland. michel.steiner@actelion.com
PMID: 23589487 DOI: 10.1002/cmdc.201300003
Abstract

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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