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pubmed-article:21193310pubmed:abstractTextOpioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the ? opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications.lld:pubmed
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pubmed-article:21193310pubmed:copyrightInfoCopyright © 2010 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:21193310pubmed:year2011lld:pubmed
pubmed-article:21193310pubmed:articleTitleTetrahydroquinoline derivatives as opioid receptor antagonists.lld:pubmed
pubmed-article:21193310pubmed:affiliationDepartment of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. cunyu.a.zhang@gsk.comlld:pubmed
pubmed-article:21193310pubmed:publicationTypeJournal Articlelld:pubmed
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