Development of κ Opioid Receptor Antagonists
نویسندگان
چکیده
منابع مشابه
Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the κ receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features. Assays on these compounds determined that one (compound 29) shows potent opioid receptor binding activity and significantly improved selectivity for th...
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The κ-opioid receptor (KOR)-dynorphin system has been implicated in the control of affect, cognition, and motivation, and is thought to be dysregulated in mood and psychotic disorders, as well as in various phases of opioid dependence. KOR agonists exhibit analgesic effects, although the adverse effects produced by some KOR agonists, including sedation, dysphoria, and hallucinations, have limit...
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Kenneth M. Wannemacher, Alexandra Terskiy, Shengjie Bian, Prem N. Yadav, Hong Li, Richard D. Howells⁎ Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry of New Jersey-Graduate School of Biomedical Science, Newark, NJ, USA Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry of New Jersey-New Jersey Medical School, Newark, NJ,...
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INTRODUCTION Nociceptive pain is one of the most common types of pain that originates from an injury involving nociceptors. Approximately 60% of the knee joint innervations are classified as nociceptive. The specific biological mechanism underlying the regulation of nociceptors is relevant for the treatment of symptoms affecting the knee joint. Intra-articular administration of exogenous hyalur...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2013
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm301783x