The endomorphin-1/2 and dynorphin-B peptides display biased agonism at the mu opioid receptor

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Author
LaVigne, Justin
Keresztes, Attila
Chiem, Daniel
Streicher, John M
Affiliation
Univ Arizona, Coll Med, Dept Pharmacol
Issue Date
2020-04
Keywords
35S-GTPγS coupling
Biased agonism
Endogenous opioid peptides
Endomorphin
Forskolin-stimulated cAMP accumulation

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Publisher
SPRINGER HEIDELBERG
Citation
LaVigne, 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
Journal
PHARMACOLOGICAL REPORTS
Rights
Copyright © 2020, Springer Nature
Collection Information
This 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 repository@u.library.arizona.edu.
Abstract
Dynorphins, 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.
Note
12 month embargo; published online: 28 February 2020
ISSN
1734-1140
PubMed ID
32112361
DOI
10.1007/s43440-020-00061-x
Version
Final accepted manuscript
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