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
RightsCopyright © 2020, Springer Nature
Collection InformationThis item from the UA Faculty Publications collection is made available by the University of Arizona with support from the University of Arizona Libraries. If you have questions, please contact us at firstname.lastname@example.org.
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
- 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
- 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
- Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting.
- Authors: Zhou L, Stahl EL, Lovell KM, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM
- Issue date: 2015 Dec
- Plasticity of Signaling by Spinal Estrogen Receptor α, κ-Opioid Receptor, and Metabotropic Glutamate Receptors over the Rat Reproductive Cycle Regulates Spinal Endomorphin 2 Antinociception: Relevance of Endogenous-Biased Agonism.
- Authors: Liu NJ, Murugaiyan V, Storman EM, Schnell SA, Kumar A, Wessendorf MW, Gintzler AR
- Issue date: 2017 Nov 15
- 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