Opioid receptors in GtoPdb v.2025.1

Opioid and opioid-like receptors are activated by a variety of endogenous peptides including [Met]enkephalin (met), [Leu]enkephalin (leu), β-endorphin (β-end), α-neodynorphin, dynorphin A (dynA), dynorphin B (dynB), big dynorphin (Big dyn), nociceptin/orphanin FQ (N/OFQ); endomorphin-1 and endomorphin-2 are also potential endogenous peptides. The Greek letter nomenclature for the opioid receptors, μ, δ and κ, is well established, and NC-IUPHAR considers this nomenclature appropriate, along with the symbols spelled out (mu, delta, and kappa), and the acronyms, MOP, DOP, and KOP [126, 103, 94]. However the acronyms MOR, DOR and KOR are still widely used in the literature. The human N/OFQ receptor, NOP, is considered 'opioid-related' rather than opioid because, while it exhibits a high degree of structural homology with the conventional opioid receptors [310], it displays a distinct pharmacology. Currently there are numerous clinically used drugs, such as morphine and many other opioid analgesics, as well as antagonists such as naloxone. The majority of clinically used opiates are relatively selective μ agonists or partial agonists, though there are some μ/κ compounds, such as butorphanol, in clinical use. κ opioid agonists, such as the alkaloid nalfurafine and the peripherally acting peptide difelikefalin, are in clinical use for itch.

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Publication Details

Journal
IUPHAR/BPS Guide to Pharmacology CITE
Published
2025-04-01
DOI
https://doi.org/10.2218/gtopdb/f50/2025.1
Primary Topic
Cardiac, Anesthesia and Surgical Outcomes
Type
article
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article

Opioid receptors in GtoPdb v.2025.1

Andreas Zimmer, Mark Connor, Stephen M. Husbands, Ian Kitchen et al.
IUPHAR/BPS Guide to Pharmacology CITE
Cardiac, Anesthesia and Surgical Outcomes
article

Opioid receptors in GtoPdb v.2025.1

Andreas Zimmer, Mark Connor, Stephen M. Husbands, Ian Kitchen, Hiroshi Ueda, Stefan Schulz, Lawrence Toll, John R. Traynor, Dominique Massot, Graeme Henderson, Michael R. Bruchas, Girolamo Calò, Brigitte L. Kieffer, MacDonald J. Christie, Eric J. Simon, Toni S. Shippenberg, Lakshmi A. Devi, Eamonn Kelly, Olivier Civelli, Nurulain T. Zaveri, Lee‐Yuan Liu‐Chen, Davide Malfacini, Anna Borsodi, Philip S. Portoghese, Yung Hou Wong, Christopher J. Evans, Charles Chavkin, Brian M. Cox, Volker Höllt, Mary-Jeanne Kreek, Jean‐Claude Meunier
article en

Abstract

Opioid and opioid-like receptors are activated by a variety of endogenous peptides including [Met]enkephalin (met), [Leu]enkephalin (leu), β-endorphin (β-end), α-neodynorphin, dynorphin A (dynA), dynorphin B (dynB), big dynorphin (Big dyn), nociceptin/orphanin FQ (N/OFQ); endomorphin-1 and endomorphin-2 are also potential endogenous peptides. The Greek letter nomenclature for the opioid receptors, μ, δ and κ, is well established, and NC-IUPHAR considers this nomenclature appropriate, along with the symbols spelled out (mu, delta, and kappa), and the acronyms, MOP, DOP, and KOP [126, 103, 94]. However the acronyms MOR, DOR and KOR are still widely used in the literature. The human N/OFQ receptor, NOP, is considered 'opioid-related' rather than opioid because, while it exhibits a high degree of structural homology with the conventional opioid receptors [310], it displays a distinct pharmacology. Currently there are numerous clinically used drugs, such as morphine and many other opioid analgesics, as well as antagonists such as naloxone. The majority of clinically used opiates are relatively selective μ agonists or partial agonists, though there are some μ/κ compounds, such as butorphanol, in clinical use. κ opioid agonists, such as the alkaloid nalfurafine and the peripherally acting peptide difelikefalin, are in clinical use for itch.

IUPHAR/BPS Guide to Pharmacology CITEVol. 2025(1)
Unifor (NO), The University of Sydney (AU), National Institutes of Health (US), University of Bonn (DE), University of Padua (IT), University of California, Los Angeles (US), Hong Kong University of Science and Technology (HK), University of Washington (US), University of California, Irvine (US), University of Michigan (US), University of Minnesota System (US), Temple College (US), University of Surrey (GB), University of Bristol (GB), Institut de Pharmacologie et de Biologie Structurale (FR), Astraea Therapeutics (United States) (US), Nagasaki University (JP), University of Bath (GB), New York University (US), Florida Atlantic University (US), Université de Strasbourg (FR), Hungarian Academy of Sciences (HU), Friedrich Schiller University Jena (DE), Rockefeller University (US), Temple University (US), Otto-von-Guericke-Universität Magdeburg (DE), Icahn School of Medicine at Mount Sinai (US), Macquarie University (AU)
Openalex Percentile: Top 88%
Cardiac, Anesthesia and Surgical Outcomes
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