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Kappa Opioid Antagonists: Past Successes and Future Prospects

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Drug Addiction

Abstract

Antagonists of the kappa opioid receptor were initially investigated as pharmacological tools that would reverse the effects of kappa opioid receptor agonists. In the years following the discovery of the first selective kappa opioid antagonists, much information about their chemistry and pharmacology has been elicited and their potential therapeutic uses have been investigated. The review presents the current chemistry, ligand-based structure activity relationships, and pharmacology of the known nonpeptidic selective kappa opioid receptor antagonists. This manuscript endeavors to provide the reader with a useful reference of the investigations made to define the structure-activity relationships and pharmacology of selective kappa opioid receptor antagonists and their potential uses as pharmacological tools and as therapeutic agents in the treatment of disease states.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD, 21201

    Matthew D. Metcalf & Andrew Coop

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  1. Matthew D. Metcalf
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  2. Andrew Coop
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Correspondence to Andrew Coop .

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Editors and Affiliations

  1. National Institute on Drug Abuse, Bethesda, MD, USA

    Rao S. Rapaka

  2. College of Medicine and Public Health, Ohio State University, Columbus, OH, USA

    Wolfgang Sadée

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© 2008 American Association of Pharmaceutical Scientists

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Metcalf, M.D., Coop, A. (2008). Kappa Opioid Antagonists: Past Successes and Future Prospects. In: Rapaka, R.S., Sadée, W. (eds) Drug Addiction. Springer, New York, NY. https://doi.org/10.1007/978-0-387-76678-2_25

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