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• W2891638695 abstract "Mu opioid receptor agonists are among the most powerful analgesic medications but also among the most addictive. The current opioid crisis has energized a quest to develop opioid analgesics that are devoid of untoward effects. Since their discovery in the 1970's, there have been major advances in our understanding of the endogenous opioid systems that these drugs target. Yet many questions remain and the development of non-addictive opioid analgesics has not been achieved. However, access to new molecular, genetic and computational tools have begun to elucidate the structural dynamics of opioid receptors, the scaffolding that links them to intracellular signaling cascades, their cellular trafficking and the distinct ways that various opioid drugs modify them. This mini-review highlights some of the chemical and pharmacological findings and new perspectives that have arisen from studies using these tools. They reveal multiple layers of complexity of opioid receptor function, including a spatiotemporal specificity in opioid receptor-induced cellular signaling, ligand-directed biased signaling, allosteric modulation of ligand interactions, heterodimerization of different opioid receptors, and the existence of slice variants with different ligand specificity. By untangling these layers, basic research into the chemistry and pharmacology of opioid receptors is guiding the way towards deciphering the mysteries of tolerance and physical dependence that have plagued the field and is providing a platform for the development of more effective and safer opioids." @default.
• W2891638695 created "2018-09-27" @default.
• W2891638695 creator A5002969658 @default.
• W2891638695 creator A5017264993 @default.
• W2891638695 date "2018-09-24" @default.
• W2891638695 modified "2023-10-14" @default.
• W2891638695 title "Untangling the complexity of opioid receptor function" @default.
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• W2891638695 doi "https://doi.org/10.1038/s41386-018-0225-3" @default.
• W2891638695 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6224460" @default.
• W2891638695 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30250308" @default.
• W2891638695 hasPublicationYear "2018" @default.
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