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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

Recent Developments in the Study of Opioid Receptors

Brian M. Cox
Molecular Pharmacology April 2013, 83 (4) 723-728; DOI: https://doi.org/10.1124/mol.112.083279
Brian M. Cox
Department of Pharmacology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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Abstract

It is now about 40 years since Avram Goldstein proposed the use of the stereoselectivity of opioid receptors to identify these receptors in neural membranes. In 2012, the crystal structures of the four members of the opioid receptor family were reported, providing a structural basis for understanding of critical features affecting the actions of opiate drugs. This minireview summarizes these recent developments in our understanding of opiate receptors. Receptor function is also influenced by amino acid substitutions in the protein sequence. Among opioid receptor genes, one polymorphism is much more frequent in human populations than the many others that have been found, but the functional significance of this single nucleotide polymorphism (SNP) has been unclear. Recent studies have shed new light on how this SNP might influence opioid receptor function. In this minireview, the functional significance of the most prevalent genetic polymorphism among the opioid receptor genes is also considered.

Footnotes

  • dx.doi.org/10.1124/mol.112.083279.

  • Received October 26, 2012.
  • Accepted December 17, 2012.
  • U.S. Government work not protected by U.S. copyright
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Molecular Pharmacology: 83 (4)
Molecular Pharmacology
Vol. 83, Issue 4
1 Apr 2013
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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

Recent Developments in the Study of Opioid Receptors

Brian M. Cox
Molecular Pharmacology April 1, 2013, 83 (4) 723-728; DOI: https://doi.org/10.1124/mol.112.083279

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Rapid CommunicationMinireview—Special Issue In Memory Of Avram Goldstein

Recent Developments in the Study of Opioid Receptors

Brian M. Cox
Molecular Pharmacology April 1, 2013, 83 (4) 723-728; DOI: https://doi.org/10.1124/mol.112.083279
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  • Article
    • Abstract
    • Introduction
    • Insights from Structural Studies of Opioid Receptors
    • Antagonist Ligands in the Receptor Complexes
    • TM Domains
    • Ligand-Binding Pocket
    • Receptor Oligomerization
    • Agonism at Opioid Receptors
    • Opioid Receptor Polymorphisms and Receptor Function
    • Concluding Thoughts
    • Authorship Contributions
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  • Enduring Impact of Avram Goldstein’s Discovery of Dynorphin
  • Sex-Biased Stress Signaling
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