ArticleBritish journal of pharmacology2012
Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 61 papers, 3 of them syntheses 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
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
61 citing papers in PubMed, 3 syntheses or guidelines pooled it, 119 citations in OpenAlex.
- Improvement of irritable bowel syndrome with glucagon like peptide-1 receptor agonists: a systematic review and meta-analysis.Frontiers in endocrinology · 2025Pooled it
- Efficacy of opioid receptor modulators in patients with irritable bowel syndrome: A systematic review and meta-analysis.Medicine · 2021Pooled it
- Pharmacological treatments for patients with irritable bowel syndrome: An umbrella review of systematic reviews and meta-analyses.Medicine · 2019Pooled it
- Effects of treatment with eluxadoline on abdominal pain in patients with IBS-D: Additional post hoc analyses of Phase 3 trials.Neurogastroenterology and motility · 2020Trial
- Efficacy and Safety of Eluxadoline in Patients With Irritable Bowel Syndrome With Diarrhea Who Report Inadequate Symptom Control With Loperamide: RELIEF Phase 4 Study.The American journal of gastroenterology · 2019Trial
- Evaluation of Eluxadoline Effect on Cardiac Repolarization.Clinical pharmacology in drug development · 2018Trial
- Eluxadoline Efficacy in IBS-D Patients Who Report Prior Loperamide Use.The American journal of gastroenterology · 2017Trial
- Early response predicts a sustained response to eluxadoline in patients with irritable bowel syndrome with diarrhoea in two Phase 3 studies.Alimentary pharmacology & therapeutics · 2017Trial
- Safety of Eluxadoline in Patients with Irritable Bowel Syndrome with Diarrhea.The American journal of gastroenterology · 2017Trial
- Abuse Potential and Pharmacodynamic Characteristics of Oral and Intranasal Eluxadoline, a Mixed μ- and κ-Opioid Receptor Agonist and δ-Opioid Receptor Antagonist.The Journal of pharmacology and experimental therapeutics · 2016Trial
- Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline.Journal of clinical pharmacology · 2015Trial
- Comparative evaluation of two herbal formulas for gastrointestinal function and gut microbiota modulation in rats with loperamide-induced dyspepsia.Scientific reports · 2025Article
- The impact of opioid administration on the incidence of postanaesthetic colic in horses.Frontiers in pain research (Lausanne, Switzerland) · 2024Article
- A MOR Antagonist with High Potency and Antagonist Efficacy among Diastereomeric C9-Alkyl-SubstitutedMolecules (Basel, Switzerland) · 2023Article
- Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans.Molecules (Basel, Switzerland) · 2023Article
- CYX-5, a G-protein biassed MOP receptor agonist, DOP receptor antagonist and KOP receptor agonist, evokes constipation but not respiratory depression relative to morphine in rats.Pharmacological reports : PR · 2023Article
- Eluxadoline-Loaded Eudragit Nanoparticles for Irritable Bowel Syndrome with Diarrhea: Formulation, Optimization Using Box-Behnken Design, and Anti-Diarrheal Activity.Pharmaceutics · 2023Article
- Single-dose Pharmacokinetics of Eluxadoline in Healthy Participants With Normal Renal Function and Participants With Renal Impairment.Clinical pharmacology in drug development · 2023Article
- The Potential Role of Human Milk Oligosaccharides in Irritable Bowel Syndrome.Microorganisms · 2022Review
- An Open-Label Study to Evaluate the Effect of Eluxadoline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Participants.Clinical pharmacology in drug development · 2022Article
1 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
14 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND & PURPOSE: Loperamide is a selective µ opioid receptor agonist acting locally in the gastrointestinal (GI) tract as an effective anti-diarrhoeal but can cause constipation. We tested whether modulating µ opioid receptor agonism with δ opioid receptor antagonism, by combining reference compounds or using a novel compound ('MuDelta'), could normalize GI motility without constipation. EXPERIMENTAL APPROACH: MuDelta was characterized in vitro as a potent µ opioid receptor agonist and high-affinity δ opioid receptor antagonist. Reference compounds, MuDelta and loperamide were assessed in the following ex vivo and in vivo experiments: guinea pig intestinal smooth muscle contractility, mouse intestinal epithelial ion transport and upper GI tract transit, entire GI transit or faecal output in novel environment stressed mice, or four weeks after intracolonic mustard oil (post-inflammatory). Colonic δ opioid receptor immunoreactivity was quantified. KEY
resultsδ Opioid receptor antagonism opposed µ opioid receptor agonist inhibition of intestinal contractility and motility. MuDelta reduced intestinal contractility and inhibited neurogenically-mediated secretion. Very low plasma levels of MuDelta were detected after oral administration. Stress up-regulated δ opioid receptor expression in colonic epithelial cells. In stressed mice, MuDelta normalized GI transit and faecal output to control levels over a wide dose range, whereas loperamide had a narrow dose range. MuDelta and loperamide reduced upper GI transit in the post-inflammatory model. CONCLUSIONS AND IMPLICATIONS: MuDelta normalizes, but does not prevent, perturbed GI transit over a wide dose-range in mice. These data support the subsequent assessment of MuDelta in a clinical phase II trial in patients with diarrhoea-predominant irritable bowel syndrome.
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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.