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J Med Chem. 2013 Mar 28;56(6):2178-95. doi: 10.1021/jm301783x. Epub 2013 Feb 14.

Development of κ opioid receptor antagonists.

Author information

  • 1Center for Organic and Medicinal Chemistry, Research Triangle Institute , P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA. fic@rti.org

Abstract

κ opioid receptors (KORs) belong to the G-protein-coupled class of receptors (GPCRs). They are activated by the endogenous opioid peptide dynorphin (DYN) and expressed at particularly high levels within brain areas implicated in modulation of motivation, emotion, and cognitive function. Chronic activation of KORs in animal models has maladaptive effects including increases in behaviors that reflect depression, the propensity to engage in drug-seeking behavior, and drug craving. The fact that KOR activation has such a profound influence on behaviors often triggered by stress has led to interest in selective KOR antagonists as potential therapeutic agents. This Perspective provides a description of preclinical research conducted in the development of several different classes of selective KOR antagonists, a summary of the clinical studies conducted thus far, and recommendations for the type of work needed in the future to determine if these agents would be useful as pharmacotherapies for neuropsychiatric illness.

PMID:
23360448
PMCID:
PMC3612131
DOI:
10.1021/jm301783x
[PubMed - indexed for MEDLINE]
Free PMC Article
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