Novel <scp>GPCR</scp> paradigms at the μ‐opioid receptor

DOI Web Site Web Site 被引用文献2件
  • G L Thompson
    Drug Discovery Biology and Department of Pharmacology Monash Institute of Pharmaceutical Sciences Monash University Parkville Vic. Australia
  • E Kelly
    School of Physiology and Pharmacology University of Bristol Bristol UK
  • A Christopoulos
    Drug Discovery Biology and Department of Pharmacology Monash Institute of Pharmaceutical Sciences Monash University Parkville Vic. Australia
  • M Canals
    Drug Discovery Biology and Department of Pharmacology Monash Institute of Pharmaceutical Sciences Monash University Parkville Vic. Australia

書誌事項

公開日
2014-07
権利情報
  • http://onlinelibrary.wiley.com/termsAndConditions#vor
DOI
  • 10.1111/bph.12600
公開者
Wiley

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説明

<jats:sec><jats:label/><jats:p>Opioids, such as morphine, are the most clinically useful class of analgesic drugs for the treatment of acute and chronic pain. However, the use of opioids is greatly limited by the development of severe adverse side effects. Consequently, drug discovery efforts have been directed towards improving the therapeutic profile of opioid‐based treatments. Opioid receptors are members of the family of <jats:styled-content style="fixed-case">GPCRs</jats:styled-content>. As such, the recent <jats:styled-content style="fixed-case">GPCR</jats:styled-content> paradigms of biased agonism and allosterism may provide novel avenues for more effective analgesics. Biased agonism (or functional selectivity) has been described for all the opioid receptor family members. Furthermore, the first allosteric modulators of opioid receptors have very recently been described. However, identification and quantification of biased agonism in a manner that is informative to medicinal chemists and drug discovery programmes still remains a challenge. In this review, we examine the progress, to date, towards identification and quantification of biased agonism and allosterism at the μ‐opioid receptor in the context of its implications for the discovery of better and safer analgesics.</jats:p></jats:sec><jats:sec><jats:title>Linked Articles</jats:title><jats:p>This article is part of a themed section on Opioids: New Pathways to Functional Selectivity. To view the other articles in this section visit <jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" xlink:href="http://dx.doi.org/10.1111/bph.2015.172.issue-2">http://dx.doi.org/10.1111/bph.2015.172.issue-2</jats:ext-link></jats:p></jats:sec>

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