ArticleThe Journal of biological chemistry2010
Morphine-like opiates selectively antagonize receptor-arrestin interactions.
Article in The Journal of biological chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 56 papers.
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Who cites it
56 citing papers in PubMed, 102 citations in OpenAlex.
- Beta-Arrestin-2 Binds to Nucleolar Organizing Regions With P2X7 Receptor Stimulation and During Cell Division.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026Article
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- Functional selectivity of EM-2 analogs at the mu-opioid receptor.Frontiers in pharmacology · 2023Article
- Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands.Frontiers in pharmacology · 2022Article
- Opioid Analgesia and Opioid-Induced Adverse Effects: A Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Mu Opioids Induce Biased Signaling at the Full-Length Seven Transmembrane C-Terminal Splice Variants of the mu Opioid Receptor Gene, Oprm1.Cellular and molecular neurobiology · 2021Article
- Mechanistic diversity involved in the desensitization of G protein-coupled receptors.Archives of pharmacal research · 2021Review
- Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NHJournal of medicinal chemistry · 2020Article
- Vasopressin receptor 2 mutations in the nephrogenic syndrome of inappropriate antidiuresis show different mechanisms of constitutive activation for G protein coupled receptors.Scientific reports · 2020Article
- The Delta-Opioid Receptor; a Target for the Treatment of Pain.Frontiers in molecular neuroscience · 2020Review
- A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response.Nature communications · 2019Article
- Rubiscolins are naturally occurring G protein-biased delta opioid receptor peptides.European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2019Article
- Therapeutic Potential of Targeting ß-Arrestin.Frontiers in pharmacology · 2019Review
- Complex formation between the vasopressin 1b receptor, β-arrestin-2, and the μ-opioid receptor underlies morphine tolerance.Nature neuroscience · 2018Article
- In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403.Pharmacology research & perspectives · 2017Article
- Systematic errors in detecting biased agonism: Analysis of current methods and development of a new model-free approach.Scientific reports · 2017Article
- Pharmacological studies on the NOP and opioid receptor agonist PWT2-[DmtEuropean journal of pharmacology · 2017Article
- Biased G Protein-Coupled Receptor Signaling: New Player in Modulating Physiology and Pathology.Biomolecules & therapeutics · 2017Review
- In vitro functional characterization of novel nociceptin/orphanin FQ receptor agonists in recombinant and native preparations.European journal of pharmacology · 2016Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The addictive potential of opioids may be related to their differential ability to induce G protein signaling and endocytosis. We compared the ability of 20 ligands (sampled from the main chemical classes of opioids) to promote the association of mu and delta receptors with G protein or beta-arrestin 2. Receptor-arrestin binding was monitored by bioluminescence resonance energy transfer (BRET) in intact cells, where pertussis toxin experiments indicated that the interaction was minimally affected by receptor signaling. To assess receptor-G protein coupling without competition from arrestins, we employed a cell-free BRET assay using membranes isolated from cells expressing luminescent receptors and fluorescent Gbeta(1). In this system, the agonist-induced enhancement of BRET (indicating shortening of distance between the two proteins) was G alpha-mediated (as shown by sensitivity to pertussis toxin and guanine nucleotides) and yielded data consistent with the known pharmacology of the ligands. We found marked differences of efficacy for G protein and arrestin, with a pattern suggesting more restrictive structural requirements for arrestin efficacy. The analysis of such differences identified a subset of structures showing a marked discrepancy between efficacies for G protein and arrestin. Addictive opiates like morphine and oxymorphone exhibited large differences both at delta and mu receptors. Thus, they were effective agonists for G protein coupling but acted as competitive enkephalins antagonists (delta) or partial agonists (mu) for arrestin. This arrestin-selective antagonism resulted in inhibition of short and long term events mediated by arrestin, such as rapid receptor internalization and down-regulation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.