The endomorphin-1/2 and dynorphin-B peptides display biased agonism at the mu opioid receptor
AffiliationUniv Arizona, Coll Med, Dept Pharmacol
Endogenous opioid peptides
Forskolin-stimulated cAMP accumulation
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CitationLaVigne, J., Keresztes, A., Chiem, D. et al. The endomorphin-1/2 and dynorphin-B peptides display biased agonism at the mu opioid receptor. Pharmacol. Rep 72, 465–471 (2020). https://doi.org/10.1007/s43440-020-00061-x
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AbstractDynorphins, enkephalins, and endomorphins are endogenous opioid agonist peptides that may possess distinct bias profiles; biased agonism of endogenous peptides could explain the selective roles of these ligands in vivo. Our purpose in the present study was to investigate biased signaling and potential underlying molecular mechanisms of bias using 35S-GTPγS and cAMP assays, specifically focusing on the role of adenylyl cyclases (ACs) and regulators of G-protein signaling proteins (RGSs) in CHO, N2a, and SH-SY5Y cell lines, all expressing the human MOR.
Note12 month embargo; published online: 28 February 2020
VersionFinal accepted manuscript