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.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
MeSH terms
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Administration, Oral
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Animals
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Benzeneacetamides / administration & dosage
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Benzeneacetamides / blood
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Benzeneacetamides / pharmacology*
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Brain / metabolism*
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Dose-Response Relationship, Drug
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Drug Discovery*
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Humans
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Isoquinolines / administration & dosage
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Isoquinolines / blood
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Isoquinolines / pharmacology*
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Orexin Receptor Antagonists*
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Orexin Receptors / metabolism
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Rats
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Structure-Activity Relationship
Substances
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2-(1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-isopropyl-2-phenylacetamide
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Benzeneacetamides
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Isoquinolines
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Orexin Receptor Antagonists
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Orexin Receptors