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Novel GPCR paradigms at the ?-opioid receptor

Thompson, G L; Kelly, E; Christopoulos, A; Canals, M


G L Thompson

E Kelly

A Christopoulos


© 2014 The British Pharmacological Society. 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 GPCRs. As such, the recent GPCR 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.

Journal Article Type Review
Acceptance Date Jan 19, 2014
Online Publication Date Jul 1, 2014
Publication Date 2015-01
Deposit Date Jan 17, 2020
Journal British Journal of Pharmacology
Print ISSN 0007-1188
Electronic ISSN 1476-5381
Publisher Wiley
Peer Reviewed Peer Reviewed
Volume 172
Issue 2
Pages 287-296
Keywords allosterism; biased-agonism; GPCR; ?-opioid receptor; analgesic agent; G protein coupled receptor; mu opiate receptor; ligand; mu opiate receptor; narcotic analgesic agent; allosterism; cell activation; cell composition; conformational transition; drug sa
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