ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2013
Increased agonist affinity at the μ-opioid receptor induced by prolonged agonist exposure.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 33 citations in OpenAlex.
- ACKR3 Proximity Labeling Identifies Novel G protein- and β-arrestin-independent GPCR Interacting Proteins.bioRxiv : the preprint server for biology · 2024Article
- Key differences in regulation of opioid receptors localized to presynaptic terminals compared to somas: Relevance for novel therapeutics.Neuropharmacology · 2023Review
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- Recent Progress in Opioid Research from an Electrophysiological Perspective.Molecular pharmacology · 2020Review
- Simple ammonium salts acting on sigma-1 receptors yield potential treatments for cancer and depression.Scientific reports · 2020Article
- Unusually persistent GαCell communication and signaling : CCS · 2020Article
- Article
- Visualizing endogenous opioid receptors in living neurons using ligand-directed chemistry.eLife · 2019Article
- Separation of Acute Desensitization and Long-Term Tolerance ofMolecular pharmacology · 2019Article
- Noncanonical Ion Channel Behaviour in Pain.International journal of molecular sciences · 2019Review
- Serotonin receptor and dendritic plasticity in the spinal cord mediated by chronic serotonergic pharmacotherapy combined with exercise following complete SCI in the adult rat.Experimental neurology · 2018Article
- Ligand-specific conformational transitions and intracellular transport are required for atypical chemokine receptor 3-mediated chemokine scavenging.The Journal of biological chemistry · 2018Article
- Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling.The Journal of biological chemistry · 2016Article
- Agonist Binding and Desensitization of the μ-Opioid Receptor Is Modulated by Phosphorylation of the C-Terminal Tail Domain.Molecular pharmacology · 2015Article
- Molecular mechanism for opioid dichotomy: bidirectional effect of μ-opioid receptors on P2X₃ receptor currents in rat sensory neurones.Purinergic signalling · 2015Article
- Change in functional selectivity of morphine with the development of antinociceptive tolerance.British journal of pharmacology · 2015Article
- Does PKC activation increase the homologous desensitization of μ opioid receptors?British journal of pharmacology · 2015Article
- Desensitization of functional µ-opioid receptors increases agonist off-rate.Molecular pharmacology · 2014Article
- Morphine-induced trafficking of a mu-opioid receptor interacting protein in rat locus coeruleus neurons.Progress in neuro-psychopharmacology & biological psychiatry · 2014Article
- Cocaine dysregulates opioid gating of GABA neurotransmission in the ventral pallidum.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
Abstract
Prolonged exposure to high-efficacy agonists results in desensitization of the μ-opioid receptor (MOR). Desensitized receptors are thought to be unable to couple to G-proteins, preventing downstream signaling; however, the changes to the receptor itself are not well characterized. In the current study, confocal imaging was used to determine whether desensitizing conditions cause a change in agonist-receptor interactions. Using rapid solution exchange, the binding kinetics of fluorescently labeled opioid agonist, dermorphin Alexa594 (derm A594), to MORs was measured in live cells. The affinity of derm A594 binding increased after prolonged treatment of cells with multiple agonists that are known to cause receptor desensitization. In contrast, binding of a fluorescent antagonist, naltrexamine Alexa594, was unaffected by similar agonist pretreatment. The increased affinity of derm A594 for the receptor was long-lived and partially reversed after a 45 min wash. Treatment of the cells with pertussis toxin did not alter the increase in affinity of the derm A594 for MOR. Likewise, the affinity of derm A594 for MORs expressed in mouse embryonic fibroblasts derived from arrestin 1 and 2 knock-out animals increased after treatment of the cells with the desensitization protocol. Thus, opioid receptors were "imprinted" with a memory of prior agonist exposure that was independent of G-protein activation or arrestin binding that altered subsequent agonist-receptor interactions. The increased affinity suggests that acute desensitization results in a long-lasting but reversible conformational change in the receptor.
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Registered trials
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.