NDLI: Positive allosteric modulators of the μ-opioid receptor: a novel approach for future pain medications

Content Provider	PubMed Central
Author	Burford, N. T. Traynor, J. R. Alt, A.
Copyright Year	2015
Abstract	Morphine and other agonists of the μ-opioid receptor are used clinically for acute and chronic pain relief and are considered to be the gold standard for pain medication. However, these opioids also have significant side effects, which are also mediated via activation of the μ-opioid receptor. Since the latter half of the twentieth century, researchers have sought to tease apart the mechanisms underlying analgesia, tolerance and dependence, with the hope of designing drugs with fewer side effects. These efforts have revolved around the design of orthosteric agonists with differing pharmacokinetic properties and/or selectivity profiles for the different opioid receptor types. Recently, μ-opioid receptor-positive allosteric modulators (μ-PAMs) were identified, which bind to a (allosteric) site on the μ-opioid receptor separate from the orthosteric site that binds an endogenous agonist. These allosteric modulators have little or no detectable functional activity when bound to the receptor in the absence of orthosteric agonist, but can potentiate the activity of bound orthosteric agonist, seen as an increase in apparent potency and/or efficacy of the orthosteric agonist. In this review, we describe the potential advantages that a μ-PAM approach might bring to the design of novel therapeutics for pain that may lack the side effects currently associated with opioid therapy.
Related Links	http://dx.doi.org/10.1111/bph.12599
Ending Page	286
Page Count	10
Starting Page	277
File Format	PDF
ISSN	14765381
e-ISSN	14765381
Journal	British Journal of Pharmacology
Issue Number	2
Volume Number	172
Language	English
Publisher	Blackwell Publishing Ltd
Publisher Date	2015-01-01
Access Restriction	Open
Rights Holder	Blackwell Publishing Ltd
Subject Keyword	Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Pharmacology

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1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
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4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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