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Research ArticleSpecial Section on 50 Years of Opioid Research — Minireview

Intrinsic Efficacy of Opioid Ligands and Its Importance for Apparent Bias, Operational Analysis, and Therapeutic Window

Alexander Gillis, Varun Sreenivasan and Macdonald J. Christie
Molecular Pharmacology October 2020, 98 (4) 410-424; DOI: https://doi.org/10.1124/mol.119.119214
Alexander Gillis
Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, New South Wales, Australia (A.G., M.J.C.) and EMBL Australia Node in Single Molecule Science, University of New South Wales, New South Wales, Australia (V.S.)
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Varun Sreenivasan
Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, New South Wales, Australia (A.G., M.J.C.) and EMBL Australia Node in Single Molecule Science, University of New South Wales, New South Wales, Australia (V.S.)
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Macdonald J. Christie
Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, New South Wales, Australia (A.G., M.J.C.) and EMBL Australia Node in Single Molecule Science, University of New South Wales, New South Wales, Australia (V.S.)
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Article Information

vol. 98 no. 4 410-424
DOI 
https://doi.org/10.1124/mol.119.119214
PubMed 
32665252

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received December 19, 2019
  • Accepted June 25, 2020
  • Published online September 21, 2020.

Article Versions

  • Earlier version (July 14, 2020 - 18:00).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2020 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Alexander Gillis,
  2. Varun Sreenivasan, and
  3. Macdonald J. Christie
  1. Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, New South Wales, Australia (A.G., M.J.C.) and EMBL Australia Node in Single Molecule Science, University of New South Wales, New South Wales, Australia (V.S.)
  1. Address correspondence to:
    Macdonald J. Christie, Discipline of Pharmacology, Faculty of Medicine and Health, University of Sydney, Main Quadrangle A14. D06, Sydney, NSW 2006, Australia. E-mail: mac.christie{at}sydney.edu.au
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Molecular Pharmacology: 98 (4)
Molecular Pharmacology
Vol. 98, Issue 4
1 Oct 2020
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Research ArticleSpecial Section on 50 Years of Opioid Research — Minireview

Pitfalls of Operational Analysis of Opioid Signaling Bias

Alexander Gillis, Varun Sreenivasan and Macdonald J. Christie
Molecular Pharmacology October 1, 2020, 98 (4) 410-424; DOI: https://doi.org/10.1124/mol.119.119214

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Research ArticleSpecial Section on 50 Years of Opioid Research — Minireview

Pitfalls of Operational Analysis of Opioid Signaling Bias

Alexander Gillis, Varun Sreenivasan and Macdonald J. Christie
Molecular Pharmacology October 1, 2020, 98 (4) 410-424; DOI: https://doi.org/10.1124/mol.119.119214
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  • Article
    • Abstract
    • Introduction
    • Assumptions of the Operational Model
    • Applicability to G Protein/Arrestin Bias at a Prototypical GPCR
    • Relevance of Efficacy and Biased Signaling to the Development of Safer Opioids
    • Conclusions
    • Acknowledgments
    • Appendix 1
    • Authorship Contributions
    • Footnotes
    • Abbreviations
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More in this TOC Section

  • New Frontiers for Opioid Systems and Disease
  • History of Opioid Research
  • Cellular Basis of Opioid Action
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