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Discovery and Characterization of ACT‐335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist
Author(s) -
Steiner Michel A.,
Gatfield John,
BrisbareRoch Catherine,
Dietrich Hendrik,
Treiber Alexander,
Jenck Francois,
Boss Christoph
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201300003
Subject(s) - penetrant (biochemical) , antagonist , orexin , neuropeptide , orexin receptor , arousal , chemistry , pharmacology , orexin a , receptor , receptor antagonist , neuroscience , biology , biochemistry , organic chemistry
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.