ArticleJournal of psychopharmacology (Oxford, England)2017
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.
Article in Journal of psychopharmacology (Oxford, England), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 94 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
94 citing papers in PubMed, 1 synthesis or guideline pooled it, 156 citations in OpenAlex.
- Oliceridine for the Management of Moderate to Severe Acute Postoperative Pain: A Narrative Review.Drug design, development and therapy · 2023Pooled it
- Dual-target mu opioid-dopamine DEuropean journal of medicinal chemistry · 2026Article
- Internet Sales of "Research Grade Compounds": The Opioid SR-17018 (SR-17) as an Example.Cureus · 2026Review
- Arrestins as programmable integrators of GPCR signaling: structural microstates, spatiotemporal logic, and therapeutic control.Cell discovery · 2026Review
- β-arrestin recruitment facilitates a direct association with G proteins.Nature communications · 2026Article
- Article
- Knowledge graph and emerging trends in β-arrestin research on pain: a bibliometric analysis (1997-2025).Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Preoperative GNRI Predicts Postoperative Constipation after Fixation of Extracapsular Hip Fractures in Older Adults.Geriatric orthopaedic surgery & rehabilitation · 2026Article
- Agonism and Biased Signaling.Handbook of experimental pharmacology · 2026Review
- Role of β-Arrestin 2 in the antinociceptive and side effect profile of morphine and the novel mu opioid receptor agonists, kurkinorin and kurkinol.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Opioid Analgesics: Rise and Fall of Ligand Biased Signaling and Future Perspectives in the Quest for the Holy Grail.CNS drugs · 2025Review
- Caveolin-1 negatively regulates the calcitonin receptor-like receptor and neuroinflammation in a female mouse model of migraine.Journal of neuroinflammation · 2025Article
- Biased Opioid Receptor Agonists: Balancing Analgesic Efficacy and Side-Effect Profiles.International journal of molecular sciences · 2025Review
- A Bibliometric and Visual Analysis of Oliceridine Research (2013-2024).Drug design, development and therapy · 2025Review
- Overview and Prospects of the Clinical Application of Oliceridine.Drug design, development and therapy · 2025Review
- Comparison of the reinforcing, antinociceptive, and respiratory depressant effects of prototypical and G-protein biased mu-opioid receptor agonists in male and female Sprague-Dawley rats.Psychopharmacology · 2024Article
- Synthesis and Biological Evaluation of Novel Biased Mu-Opioid Receptor Agonists.Molecules (Basel, Switzerland) · 2024Article
- Adrenoceptor Desensitization: Current Understanding of Mechanisms.Pharmacological reviews · 2024Review
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- Assessment of the potential of novel and classical opioids to induce respiratory depression in mice.British journal of pharmacology · 2023Article
34 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
rationaleTRV130 (oliceridine; N-[(3-methoxythiophen-2-yl)methyl]-2-[(9 R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethanamine) is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs. Prevailing evidence suggests that TRV130 and other G-protein-biased MOR agonists may produce therapeutic analgesic effects with reduced adverse effects compared to existing MOR agonists.
objectivesThis study compared the effects of acute and repeated TRV130 administration on measures of antinociception, gastrointestinal function, and abuse liability in rodents. We hypothesized that TRV130 would produce robust and sustained antinociception and abuse-related effects during repeated treatment, but that tolerance would develop to gastrointestinal inhibition.
methodsAntinociception was assessed using a warm-water tail-withdrawal procedure in mice. Gastrointestinal function was assessed in mice using an in vivo measure of fecal output and in vitro assays of colonic propulsion and of colon and ileum circular muscle contraction. Abuse liability was assessed in rats using an intracranial self-stimulation (ICSS) procedure. (+)-TRV130 was administered with acute and repeated dosing regimens, and (-)-TRV130 was also examined in the ICSS procedure to assess stereoselectivity.
resultsAcute (+)-TRV130 treatment produced robust antinociception, complete inhibition of gastrointestinal function, and weak abuse-related effects. Repeated (+)-TRV130 treatment failed to produce tolerance to antinociception or gastrointestinal inhibition, and abuse-related effects were enhanced by repeated treatment. Effects of acute and repeated (+)-TRV130 in these procedures resemble effects of morphine, with the exception that TRV130 antinociception was more resistant to tolerance. (-)-TRV130 was inactive.
conclusionsThese results suggest that TRV130 retains undesirable constipating and abuse-related effects during repeated treatment despite its bias for G-protein signaling.
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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.