The AAPS Journal

, Volume 7, Issue 3, pp E704–E722

Kappa opioid antagonists: Past successes and future prospects


DOI: 10.1208/aapsj070371

Cite this article as:
Metcalf, M.D. & Coop, A. AAPS J (2005) 7: E704. doi:10.1208/aapsj070371


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.



Copyright information

© American Association of Pharmaceutical Scientists 2005

Authors and Affiliations

  1. 1.Department of Pharmaceutical SciencesUniversity of Maryland School of PharmacyBaltimore