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
MetadataShow full item record
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
- Specific activation of the mu opioid receptor (MOR) by endomorphin 1 and endomorphin 2.
- Authors: Monory K, Bourin MC, Spetea M, Tömböly C, Tóth G, Matthes HW, Kieffer BL, Hanoune J, Borsodi A
- Issue date: 2000 Feb
- Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor.
- Authors: Thompson GL, Lane JR, Coudrat T, Sexton PM, Christopoulos A, Canals M
- Issue date: 2015 Aug
- Endomorphin-1 and endomorphin-2 are partial agonists at the human mu-opioid receptor.
- Authors: Hosohata K, Burkey TH, Alfaro-Lopez J, Varga E, Hruby VJ, Roeske WR, Yamamura HI
- Issue date: 1998 Apr 3
- Biased μ-opioid receptor agonists diversely regulate lateral mobility and functional coupling of the receptor to its cognate G proteins.
- Authors: Melkes B, Hejnova L, Novotny J
- Issue date: 2016 Dec
- Differential involvement of mu(1)-opioid receptors in endomorphin- and beta-endorphin-induced G-protein activation in the mouse pons/medulla.
- Authors: Mizoguchi H, Narita M, Wu H, Narita M, Suzuki T, Nagase H, Tseng LF
- Issue date: 2000