ArticleEuropean journal of pharmacology2012
Differences in the characteristics of tolerance to μ-opioid receptor agonists in the colon from wild type and β-arrestin2 knockout mice.
Article in European journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 36 citations in OpenAlex.
- Fentanyl-induced changes in brain activity in awake nonhuman primates at 9.4 Tesla.Brain imaging and behavior · 2022Article
- Opioid Analgesia and Opioid-Induced Adverse Effects: A Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- The Guts of the Opioid Crisis.Physiology (Bethesda, Md.) · 2021Article
- A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects.Neuropharmacology · 2021Article
- Mechanism of μ-Opioid Receptor-Magnesium Interaction and Positive Allosteric Modulation.Biophysical journal · 2020Article
- Agonist-dependent development of delta opioid receptor tolerance in the colon.Cellular and molecular life sciences : CMLS · 2019Article
- Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation.Neurogastroenterology and motility · 2019Article
- Insights from molecular dynamics simulations to exploit new trends for the development of improved opioid drugs.Neuroscience letters · 2019Review
- Dynamic and Kinetic Elements of µ-Opioid Receptor Functional Selectivity.Scientific reports · 2017Article
- Effects of acute and repeated treatment with the biased mu opioid receptor agonist TRV130 (oliceridine) on measures of antinociception, gastrointestinal function, and abuse liability in rodents.Journal of psychopharmacology (Oxford, England) · 2017Article
- How Oliceridine (TRV-130) Binds and Stabilizes a μ-Opioid Receptor Conformational State That Selectively Triggers G Protein Signaling Pathways.Biochemistry · 2016Article
- Allostatic Mechanisms of Opioid Tolerance Beyond Desensitization and Downregulation.Trends in pharmacological sciences · 2016Review
- 6β-N-Heterocyclic Substituted Naltrexamine Derivative BNAP: A Peripherally Selective Mixed MOR/KOR Ligand.ACS chemical neuroscience · 2016Article
- G Protein-Coupled Receptor Trafficking and Signalling in the Enteric Nervous System: The Past, Present and Future.Advances in experimental medicine and biology · 2016Review
- Inflammation-induced abnormalities in the subcellular localization and trafficking of the neurokinin 1 receptor in the enteric nervous system.American journal of physiology. Gastrointestinal and liver physiology · 2015Article
- Opioid receptors and associated regulator of G protein signaling are involved in the cathartic colon of rats.Experimental and therapeutic medicine · 2015Article
- Site and mechanism of morphine tolerance in the gastrointestinal tract.Neurogastroenterology and motility · 2014Review
- Morphine dependence in single enteric neurons from the mouse colon requires deletion of β-arrestin2.Physiological reports · 2014Article
- Biological redundancy of endogenous GPCR ligands in the gut and the potential for endogenous functional selectivity.Frontiers in pharmacology · 2014Review
- Specific localization of β-Arrestin2 in myenteric plexus of mouse gastrointestinal tract.PloS one · 2014Article
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Authors and funding
3 authors at 1 institution in 1 country.
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Abstract
Drawbacks to opioid use include development of analgesic tolerance and persistent constipation. We previously reported that tolerance to morphine develops upon repeated exposure in the isolated ileum but not the isolated colon. The cellular mechanisms of antinociceptive tolerance vary among μ-opioid receptor agonists. In this study, we assess β-arrestin2 deletion on the development of tolerance to different opioids in ileum and colon circular muscle. Tolerance was determined by assessing the ability of repeated in-vitro opioid exposure to induce contraction of the circular muscle from C57BL/6 wild type (WT) and β-arrestin2 knockout (KO) mice. Repeated exposure every 30 min with in-between washes resulted in tolerance to all agonists in the ileum of both WT and KO mice. However, in the colon of WT mice, comparison of the contractions between the 4th exposure and 1st response was similar to DAMGO (100 ± 10%; N=5) but reduced to fentanyl (62 ± 13%; N=8) and etorphine (38 ± 4%; N=7) indicative of tolerance to fentanyl and etorphine but not DAMGO. In contrast, all agonists produced tolerance in the colon of KO: DAMGO response at the 4th exposure decreased to 52 ± 10% (N=5), fentanyl to 20 ± 5% (N=6) and etorphine 33 ± 7% (N=6). Differences in tolerance among opioid agonists in the colon suggest ligand bias. The deletion of β-arrestin2 in colon appears to be necessary for tolerance to DAMGO but not fentanyl or etorphine. β-arrestin2 potentially represents an important target for treating opioid-induced bowel dysfunction and warrants further exploration of its ligand bias.
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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.