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Biased mu-opioid receptor agonists confer analgesia with reduced side effects
2018
University of Western Ontario Medical Journal
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Along with the analgesic benefits, opioid use also commonly induces a number of side effects. Respiratory depression is an especially dangerous and potentially lethal example. ...
Downstream to the mu-opioid receptor, which is responsible for the analgesic effects of opioids, β-arrestin-2 signaling has been suggested to be important for the manifestation of side effects, including ...
Biased mu-opioid receptor agonists confer analgesia with reduced side effects Chloe Gui, Sean Wong current limitations of opioids Though opioid addiction has been described as early as the sixteenth century ...
doi:10.5206/uwomj.v87i1.1910
fatcat:r2iboy25lbfrpcouylpxsc2emu
The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics
2020
Frontiers in Chemistry
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Herein, we reviewed the computational-guided studies on opioid receptors for the discovery of new analgesics, the structural basis of receptor subtype selectivity, agonist interaction mechanism, and biased ...
In the past few years, published high-resolution crystal structures of opioid receptor laid a solid basis for both experimental and computational studies. ...
modification of this manuscript. ...
doi:10.3389/fchem.2020.00335
pmid:32500054
pmcid:PMC7242749
fatcat:aohqt6wzsjap3n4wrnkrwkegty
Novel Molecular Strategies and Targets for Opioid Drug Discovery for the Treatment of Chronic Pain
2017
The Yale Journal of Biology and Medicine
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Other novel approaches include targeting heterodimers of the opioid and other receptor systems which may drive side effects, and making endogenous opioid peptides druggable, which may also reduce opioid ...
Taken together, these advances in our molecular understanding provide a path forward to break the barrier in producing an opioid with reduced or eliminated side effects, especially addiction, which may ...
valid targets for drug discovery to reduce opioid side effects. ...
pmid:28356897
pmcid:PMC5369049
fatcat:5pgcyk4jpnc5zfb5xkb7atxz3q
Biased agonism
2018
PAIN Reports
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They find that increased bias towards G-protein signaling produces better antinociception with minimal side effects in mice models. G-protein-biased opioids may provide a safer treatment strategy. ...
Opioids alleviate pain, but adverse effects severely limit their usefulness. ...
in opioid-based analgesic drug discovery is biased agonism. ...
doi:10.1097/pr9.0000000000000650
pmid:29922742
pmcid:PMC5999417
fatcat:4qbjk7aldva67pi3qo22tjz73a
Biased ligands at opioid receptors: Current status and future directions
2021
Science Signaling
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We also discuss an example of structure-based biased ligand discovery at the μ-opioid receptor, an approach that could revolutionize drug discovery at opioid and other receptors. ...
effects of current opioid medications. ...
A potential framework to overcome opioid side effects has emerged in the last decade based on the design and discovery of functionally selective ligands at opioid receptors. ...
doi:10.1126/scisignal.aav0320
pmid:33824179
pmcid:PMC7611221
fatcat:dkbbdswtdnfsbde6gnho7ygfzi
Designing Safer Analgesics via μ-Opioid Receptor Pathways
2017
TIPS - Trends in Pharmacological Sciences
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In this review we outline recent progress towards the discovery of safer opioid analgesics. ...
It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. ...
Unlike morphine and codeine, novel μOR agonists, such as PZM21 [28] and TRV130 [65] , retain most the opioid analgesic effects but with reduced toxic side effects, in part because of their biased agonism ...
doi:10.1016/j.tips.2017.08.004
pmid:28935293
pmcid:PMC5690544
fatcat:rpftdsj3xzghtntkysn4gveehq
Is tapentadol different from classical opioids? A review of the evidence
2016
British Journal of Pain
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The reduced incidence of some of the typical opioid induced side-effects, compared to equianalgesic doses of classical opioids supports the hypothesis that tapentadol analgesia is only partially mediated ...
Preclinical studies suggest that this combined and synergistic MOR and NRI activity might translate to an ability to be effective in a wide range of painful conditions with reduced opioid related side ...
doi:10.1177/2049463716657363
pmid:27867511
pmcid:PMC5102094
fatcat:gqeukihlbfamxgyxxbunvg5xm4
Opioid receptors: toward separation of analgesic from undesirable effects
2013
TIBS -Trends in Biochemical Sciences. Regular ed
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Recently, attempts to develop analgesic agents with reduced side effects have targeted either the putative opioid receptor splice variants or the receptor heterooligomers. ...
This review discusses the potential for receptor splice variant-and the hetero-oligomer-based discovery of new opioid analgesics. ...
We also examine alternative approaches in reducing the side effects of opioid drugs. ...
doi:10.1016/j.tibs.2013.03.003
pmid:23598157
pmcid:PMC3665630
fatcat:odm2jg2vhnaq5h72u4kyuz42su
A "tail" of opioid receptor variants
2017
Journal of Clinical Investigation
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This discovery greatly improves our understanding of opioid side effects and suggests intriguing therapeutic approaches that could improve both the safety and long-term effectiveness of opioids. observed ...
This study adds additional support to the growing body of evidence that the desirable analgesic effects of opioids can be dissociated from undesirable side effects. ...
doi:10.1172/jci93582
pmid:28319052
pmcid:PMC5373875
fatcat:vfdfoupp55bvjcr4bffcop4tyy
A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor
2019
Proceedings of the National Academy of Sciences of the United States of America
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Bilorphin is both a unique molecular tool that enhances understanding of MOPr biased signaling and a promising lead in the development of next generation analgesics. ...
Given their resemblance to known short peptide opioid agonists, we elucidated that they were weak (Ki low micromolar) μ-opioid agonists, which led to the design of bilorphin, a potent and selective μ-opioid ...
This work was supported by Program Grant APP1072113 from the National Health and Medical Research Council of Australia (to P.F.A. and M.J.C.). ...
doi:10.1073/pnas.1908662116
pmid:31611414
pmcid:PMC6825270
fatcat:xgvua6aswbbolli2dq73vfhqya
Quantitative Systems Pharmacology and Biased Agonism at Opioid Receptors: A Potential Avenue for Improved Analgesics
2022
International Journal of Molecular Sciences
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Although opioid analgesics are widely used in chronic pain treatment, many patients report inadequate pain relief or relevant adverse effects, highlighting the need to develop analgesics with improved ...
complexity of opioid receptor pharmacology and the current limitations entailing the development of biased opioid agonists as improved analgesics. ...
opioid analgesic with increased efficacy/safety and lower side effects. ...
doi:10.3390/ijms23095114
pmid:35563502
pmcid:PMC9104178
fatcat:p2prttqsf5d2fiu5u36keehhh4
Biased versus Partial Agonism in the Search for Safer Opioid Analgesics
2020
Molecules
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with reduced side effects or 'apparent bias'. ...
Moreover, studies performed with mice genetically engineered with G-protein-biased mu receptors suggested increased sensitivity of these animals to both analgesic actions and side effects of opioid drugs ...
−) animals [18, 24] that βarr2 signaling is involved in the acute side effects of opioid analgesics. ...
doi:10.3390/molecules25173870
pmid:32854452
fatcat:kr2dlayrdnh43ef6zhvdz5tkxe
Recent Chemical and Pharmacological Developments on 14-Oxygenated-N-methylmorphinan-6-ones
2021
Molecules
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Morphine and structurally related derivatives (e.g., oxycodone, oxymorphone, buprenorphine) are highly effective opioid analgesics, mediating their effects via the activation of opioid receptors, with ...
We focus on drug design strategies and structure–activity relationships on specific modifications in positions 5, 6, 14 and 17 on the morphinan skeleton, with the goal of aiding the discovery of opioid ...
opioid analgesics with fewer unwanted side effects compared to currently available pain therapeutics. ...
doi:10.3390/molecules26185677
pmid:34577147
pmcid:PMC8464912
fatcat:cjtcb7rkibbepgyz4ec2pvpifq
A new splice of life for the μ-opioid receptor
2015
Journal of Clinical Investigation
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Acknowledgments This research was supported by the Intramural Research Program of the Clinical Center, NIH. ...
in the quest for a strong analgesic with a reduced side effect profile. ...
This observation led to the idea that these biased agonists of opioid receptors could be used to elicit the desired pain-reducing effects of opiates with minimal or no side effects. ...
doi:10.1172/jci82060
pmid:26011639
pmcid:PMC4563694
fatcat:beqjexxhv5dnzpabcgvjrq5hhm
Analgesic Potential of Extracts and Derived Natural Products from Medicinal Plants
[chapter]
2017
Pain Relief - From Analgesics to Alternative Therapies
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Chemically diverse structures have been identified as pain relievers; they relieve pain through various mechanisms and act either centrally (opioids receptor agonism) or peripherally. ...
Therefore, this chapter is intended to summarize the literature pertaining to plants and their constituents discovered with analgesic potential in the last four decades. ...
Acknowledgements The authors are grateful to the Higher Education Commission of Pakistan and the University of Swabi, KPK, for financial support. ...
doi:10.5772/intechopen.68631
fatcat:hbjczqcbprfqbgcoa66yvupoga
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