ArticleBritish journal of pharmacology2006
Differential activation of G-proteins by mu-opioid receptor agonists.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
35 citing papers in PubMed, 80 citations in OpenAlex.
- Methadone versus morphine for treatment of neonatal abstinence syndrome: a prospective randomized clinical trial.Journal of perinatology : official journal of the California Perinatal Association · 2015Trial
- G protein regulatory network shapes magnitude and kinetics of behavioral responses in an engineered opioid receptor model.The Journal of biological chemistry · 2026Article
- Human cytomegalovirus UL78 is a nuclear-localized GPCR necessary for efficient reactivation from latent infection in CD34Journal of virology · 2025Article
- Buprenorphine Pharmacodynamics: A Bridge to Understanding Buprenorphine Clinical Benefits.Drugs · 2025Review
- Mapping Astrocytic and Neuronal μ-opioid Receptor Expression in Various Brain Regions Using MOR-mCherry Reporter Mouse.Experimental neurobiology · 2023Article
- Contribution of G-Protein α-Subunits to Analgesia, Hyperalgesia, and Hyperalgesic Priming Induced by Subanalgesic and Analgesic Doses of Fentanyl and Morphine.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2022Article
- A Narrative Pharmacological Review of Buprenorphine: A Unique Opioid for the Treatment of Chronic Pain.Pain and therapy · 2020Review
- Pharmacological and non-pharmacological treatments for the Neonatal Abstinence Syndrome (NAS).Seminars in fetal & neonatal medicine · 2019Review
- Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands.Journal of medicinal chemistry · 2019Article
- US28: HCMV's Swiss Army Knife.Viruses · 2018Review
- Expression of µ-Opioid Receptor in CA1 Hippocampal Astrocytes.Experimental neurobiology · 2018Article
- Characterization of structurally novel G protein biased CBPharmacological research · 2017Article
- Article
- Striatal dopamine D1 and D2 receptors are differentially regulated following buprenorphine or methadone treatment.Psychopharmacology · 2015Article
- Novel GPCR paradigms at the μ-opioid receptor.British journal of pharmacology · 2015Review
- Cellular signalling of non-synonymous single-nucleotide polymorphisms of the human μ-opioid receptor (OPRM1).British journal of pharmacology · 2015Review
- Dopamine D3 receptor dysfunction prevents anti-nociceptive effects of morphine in the spinal cord.Frontiers in neural circuits · 2014Article
- Nucleotide exchange factors: Kinetic analyses and the rationale for studying kinetics of GEFs.Cellular logistics · 2012Article
- Evidence for constitutively-active adenosine receptors at mammalian motor nerve endings.European journal of pharmacology · 2012Article
- Functional selectivity at the μ-opioid receptor: implications for understanding opioid analgesia and tolerance.Pharmacological reviews · 2011Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
We investigated the ability of the activated mu-opioid receptor (MOR) to differentiate between myristoylated G(alphai1) and G(alphaoA) type G(alpha) proteins, and the maximal activity of a range of synthetic and endogenous agonists to activate each G(alpha) protein. Membranes from HEK293 cells stably expressing transfected MOR were chaotrope extracted to denature endogenous G-proteins and reconstituted with specific purified G-proteins. The G(alpha) subunits were generated in bacteria and were demonstrated to be recognised equivalently to bovine brain purified G(alpha) protein by CB(1) cannabinoid receptors. The ability of agonists to catalyse the MOR-dependent GDP/[(35)S]GTP(gamma)S exchange was then compared for G(alphai1) and G(alphaoA). Activation of MOR by DAMGO produced a high-affinity saturable interaction for G(alphaoA) (K(m)=20+/-1 nM) but a low-affinity interaction with G(alphai1) (K(m)=116+/-12 nM). DAMGO, met-enkephalin and leucine-enkephalin displayed maximal G(alpha) activation among the agonists evaluated. Endomorphins 1 and 2, methadone and beta-endorphin activated both G(alpha) to more than 75% of the maximal response, whereas fentanyl partially activated both G-proteins. Buprenorphine and morphine demonstrated a statistically significant difference between the maximal activities between G(alphai1) and G(alphaoA). Interestingly, DAMGO, morphine, endomorphins 1 and 2, displayed significant differences in the potencies for the activation of the two G(alpha). Differences in maximal activity and potency, for G(alphai1) versus G(alphaoA), are both indicative of agonist selective activation of G-proteins in response to MOR activation. These findings may provide a starting point for the design of drugs that demonstrate greater selectivity between these two G-proteins and therefore produce a more limited range of effects.
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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.