ArticleWorld journal of gastroenterology2012
Opiate-induced constipation related to activation of small intestine opioid μ2-receptors.
Article in World journal of gastroenterology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 42 citations in OpenAlex.
- Efficacy and Safety of Methylnaltrexone for Opioid-Induced Constipation in Patients With Chronic Noncancer Pain: A Placebo Crossover Analysis.Regional anesthesia and pain medicineTrial
- Analgesic effect of magnesium sulfate during total intravenous anesthesia: randomized clinical study.Brazilian journal of anesthesiology (Elsevier)Trial
- Effects of Rosa damascena and its compounds on smooth muscle contractility.Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi · 2026Review
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- Ameliorative Effects of Soybean Powder Fermented byInternational journal of molecular sciences · 2025Article
- Effects of Different Cow-Milk Beta-Caseins on the Gut-Brain Axis: A Narrative Review of Preclinical, Animal, and Human Studies.Nutrition reviews · 2025Review
- Comprehensive Analysis of Strong Opioid Side Effects in Palliative Care Using the SIDER Database.Journal of clinical medicine · 2025Article
- Effects of different opioids on the contractile tension of isolated rat intestinal smooth muscle.Frontiers in pharmacology · 2025Article
- Shouhui Tongbian Capsule ameliorates 5-fluorouracil induced constipation in mice by modulating gut microbiota and activating PI3K/AKT/AQP3 signaling pathway.Frontiers in microbiology · 2025Article
- Analysis of Opioid-Related Adverse Events in Japan Using FAERS Database.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Complement C3-Deficiency-Induced Constipation in FVB/N-C3International journal of molecular sciences · 2023Article
- P2Y1 receptor in the colonic submucosa of rats and its association with opioid‑induced constipation.Experimental and therapeutic medicine · 2023Article
- Slowed gastrointestinal transit is associated with an altered caecal microbiota in an aged rat model.Frontiers in cellular and infection microbiology · 2023Article
- Intraoperative Analgesia with Magnesium Sulfate versus Remifentanil Guided by Plethysmographic Stress Index in Post-Bariatric Dermolipectomy: A Randomized Study.Anesthesiology research and practice · 2022Article
- Evaluation of Antidiarrheal Activity of 80% Methanolic Extract of the Leaves ofEvidence-based complementary and alternative medicine : eCAM · 2021Article
- Heat-inactivated Lactobacillus plantarum nF1 promotes intestinal health in Loperamide-induced constipation rats.PloS one · 2021Article
- Article
- Characterization the response of Korl:ICR mice to loperamide induced constipation.Laboratory animal research · 2016Article
- Development of a novel mouse constipation model.World journal of gastroenterology · 2016Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo investigate the role of opioid μ-receptor subtype in opiate-induced constipation (OIC).
methodsThe effect of loperamide on intestinal transit was investigated in mice. Ileum strips were isolated from 12-wk-old male BALB/c mice for identification of isometric tension. The ileum strips were precontracted with 1 μmol/L acetylcholine (ACh). Then, decrease in muscle tone (relaxation) was characterized after cumulative administration of 0.1-10 μmol/L loperamide into the organ bath, for a concentration-dependent study. Specific blockers or antagonists were used for pretreatment to compare the changes in loperamide-induced relaxation.
resultsIn addition to the delay in intestinal transit, loperamide produced a marked relaxation in isolated ileum precontracted with ACh, in a dose-dependent manner. This relaxation was abolished by cyprodime, a selective opioid μ-receptor antagonist, but not modified by naloxonazine at a dose sufficient to block opioid μ-1 receptors. Also, treatment with opioid μ-1 receptor agonist failed to modify the muscle tone. Moreover, the relaxation by loperamide was attenuated by glibenclamide at a dose sufficient to block ATP-sensitive K+ (K(ATP)) channels, and by protein kinase A (PKA) inhibitor, but was enhanced by an inhibitor of phosphodiesterase for cyclic adenosine monophosphate (cAMP).
conclusionLoperamide induces intestinal relaxation by activation of opioid μ-2 receptors via the cAMP-PKA pathway to open K(ATP) channels, relates to OIC.
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