Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist.
CHEMMEDCHEM(2013)
摘要
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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关键词
anxiety,neurotransmitters,orexin receptor antagonists,peptides,sleep
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