ArticleCellular signalling2008
Morphine-induced mu-opioid receptor rapid desensitization is independent of receptor phosphorylation and beta-arrestins.
Article in Cellular signalling, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 56 citations in OpenAlex.
- Carfentanil stabilizes µ opioid receptor conformations that are ultra-efficient in inhibiting cAMP, resistant to naloxone or nalmefene but sensitive to naltrexone.Archives of toxicology · 2025Article
- GM-1020: a novel, orally bioavailable NMDA receptor antagonist with rapid and robust antidepressant-like effects at well-tolerated doses in rodents.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Article
- Acute Delta 9-tetrahydrocannabinol administration differentially alters the hippocampal opioid system in adult female and male rats.Synapse (New York, N.Y.) · 2021Article
- Sex and chronic stress differentially alter phosphorylated mu and delta opioid receptor levels in the rat hippocampus following oxycodone conditioned place preference.Neuroscience letters · 2019Article
- Neuropathic Pain Induced Alterations in the Opioidergic Modulation of a Descending Pain Facilitatory Area of the Brain.Frontiers in cellular neuroscience · 2019Article
- Spinal or supraspinal phosphorylation deficiency at the MOR C-terminus does not affect morphine tolerance in vivo.Pharmacological research · 2017Article
- Thalidomide Promotes Morphine Efficacy and Prevents Morphine-Induced Tolerance in Rats with Diabetic Neuropathy.Neurochemical research · 2016Article
- MicroRNAs Are Involved in the Development of Morphine-Induced Analgesic Tolerance and Regulate Functionally Relevant Changes in Serpini1.Frontiers in molecular neuroscience · 2016Article
- G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro.Biochemistry · 2015Article
- Analgesic synergy between opioid and α2 -adrenoceptors.British journal of pharmacology · 2015Review
- Role of FK506 binding protein 12 in morphine-induced μ-opioid receptor internalization and desensitization.Neuroscience letters · 2014Article
- FK506-binding protein 12 modulates μ-opioid receptor phosphorylation and protein kinase C(ε)-dependent signaling by its direct interaction with the receptor.Molecular pharmacology · 2014Article
- Identification of phosphorylation sites in the COOH-terminal tail of the μ-opioid receptor.Journal of neurochemistry · 2013Article
- Regulation of μ-opioid receptors: desensitization, phosphorylation, internalization, and tolerance.Pharmacological reviews · 2013Review
- Posttranslation modification of G protein-coupled receptor in relationship to biased agonism.Methods in enzymology · 2013Article
- Deciphering µ-opioid receptor phosphorylation and dephosphorylation in HEK293 cells.British journal of pharmacology · 2012Article
- Endomorphin-2: a biased agonist at the μ-opioid receptor.Molecular pharmacology · 2012Article
- Cholesterol level influences opioid signaling in cell models and analgesia in mice and humans.Journal of lipid research · 2012Article
- GRK2 protein-mediated transphosphorylation contributes to loss of function of μ-opioid receptors induced by neuropeptide FF (NPFF2) receptors.The Journal of biological chemistry · 2012Article
- Palmitoylation and membrane cholesterol stabilize μ-opioid receptor homodimerization and G protein coupling.BMC cell biology · 2012Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Receptor desensitization involving receptor phosphorylation and subsequent betaArrestin (betaArr) recruitment has been implicated in the tolerance development mediated by mu-opioid receptor (OPRM1). However, the roles of receptor phosphorylation and betaArr on morphine-induced OPRM1 desensitization remain to be demonstrated. Using OPRM1-induced intracellular Ca(2+) ([Ca(2+)](i))release to monitor receptor activation, as predicted, [D-Ala(2), N-Me-Phe(4), Gly(5)-ol]-enkephalin (DAMGO), induced OPRM1 desensitization in a receptor phosphorylation- and betaArr-dependent manner. The DAMGO-induced OPRM1 desensitization was attenuated significantly when phosphorylation deficient OPRM1 mutants or Mouse Embryonic Fibroblast (MEF) cells from betaArr1 and 2 knockout mice were used in the studies. Specifically, DAMGO-induced desensitization was blunted in HEK293 cells expressing the OPRM1S375A mutant and was eliminated in MEF cells isolated from betaArr2 knockout mice expressing the wild type OPRM1. However, although morphine also could induce a rapid desensitization on [Ca(2+)](i) release to a greater extent than that of DAMGO and could induce the phosphorylation of Ser(375) residue, morphine-induced desensitization was not influenced by mutating the phosphorylation sites or in MEF cells lacking betaArr1 and 2. Hence, morphine could induce OPRM1 desensitization via pathway independent of betaArr, thus suggesting the in vivo tolerance development to morphine can occur in the absence of betaArr.
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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.