Endomorphin-2: A Biased Agonist at the μ-Opioid Receptor

Previously we correlated the efficacy for G protein activation with that for arrestin recruitment for a number of agonists at the μ-opioid receptor (MOPr) stably expressed in HEK293 cells. We suggested that the endomorphins (endomorphin-1 and -2) might be biased toward arrestin recruitment. In the p...

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Veröffentlicht in:	Molecular pharmacology 2012-08, Vol.82 (2), p.178-188
Hauptverfasser:	Rivero, Guadalupe, Llorente, Javier, McPherson, Jamie, Cooke, Alex, Mundell, Stuart J., McArdle, Craig A., Rosethorne, Elizabeth M., Charlton, Steven J., Krasel, Cornelius, Bailey, Christopher P., Henderson, Graeme, Kelly, Eamonn
Format:	Artikel
Sprache:	eng
Schlagworte:	4′,6-diamidino-2-phenylindole dihydrochloride [d-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin Analgesics, Opioid - metabolism Analgesics, Opioid - pharmacology Animals CFP cyan fluorescent protein DAMGO DAPI Dose-Response Relationship, Drug Enkephalin, Ala-MePhe-Gly- - metabolism Enkephalin, Ala-MePhe-Gly- - pharmacology fluorescence resonance energy transfer FRET G protein-coupled receptor G protein-coupled receptor kinase 2 G protein-coupled, inwardly rectifying, K+ channel current GIRK GPCR GRK2 GTPγS guanosine 5′-O-(γ-thiotriphosphate) HEK293 Cells hemagglutinin Humans locus ceruleus Male MOPr noradrenaline Oligopeptides - physiology Organ Culture Techniques Rats Rats, Wistar Receptors, Opioid, mu - agonists Receptors, Opioid, mu - physiology yellow fluorescent protein YFP β-FNA β-funaltrexamine μ-opioid receptor
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