Concepedia

Discovery and Characterization of ACT‐335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist

Michel A. Steiner, John Gatfield, Catherine Brisbare‐Roch, Hendrik Dietrich, Alexander Treiber, François Jenck, Christoph Boss

ChemMedChem · 2013 · 95 citations · 13 references

DOI

Concepts

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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