ArticleNeurogastroenterology and motility2019
Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation.
Article in Neurogastroenterology and motility, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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.
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Who cites it
17 citing papers in PubMed, 34 citations in OpenAlex.
- Effect of add-on naldemedine treatment in patients with cancer and opioid-induced constipation insufficiently responding to magnesium oxide: a pooled, subgroup analysis of two randomized controlled trials.Japanese journal of clinical oncology · 2025Trial
- Opioid-Induced Constipation: Mechanistic Insights, Experimental Models, and Future Perspectives.Biomedicines · 2026Review
- Dose-dependent association of naldemedine and magnesium oxide in the management of opioid-induced constipation.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2026Observational
- Incidence of opioid-induced constipation in non-cancer patients using weak opioids for chronic pain in Japan: a cohort study.Scientific reports · 2025Article
- A Systematic Review of Naldemedine and Naloxegol for the Treatment of Opioid-Induced Constipation in Cancer Patients.Pharmacy (Basel, Switzerland) · 2024Review
- Article
- Insights into the Current and Possible Future Use of Opioid Antagonists in Relation to Opioid-Induced Constipation and Dysbiosis.Molecules (Basel, Switzerland) · 2023Review
- Influence of Brain Metastasis on Analgesia-Related Outcomes in Patients with Lung and Breast Cancers Treated with Naldemedine: A Propensity Score-Matched Analysis.Journal of clinical medicine · 2023Article
- Article
- In Silico Repurposed Drugs against Monkeypox Virus.Molecules (Basel, Switzerland) · 2022Article
- Post-marketing surveillance of the safety and effectiveness of naldemedine in the management of opioid-induced constipation in patients with cancer pain in Japan.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2022Article
- Rational Design, Chemical Syntheses, and Biological Evaluations of Peripherally Selective Mu Opioid Receptor Ligands as Potential Opioid Induced Constipation Treatment.Journal of medicinal chemistry · 2022Article
- Intranasal Low-Dose Naltrexone Against Opioid Side Effects: A Preclinical Study.Frontiers in pharmacology · 2020Article
- Naldemedine: A New Option for OIBD.Journal of pain research · 2020Review
- UEG Week 2019 Poster Presentations.United European gastroenterology journal · 2019Article
- Review
- 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
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundNaldemedine (S-297995) is a peripherally acting μ-opioid receptor antagonist developed as a once-daily oral drug for opioid-induced constipation (OIC) in adults with chronic noncancer or cancer pain. This study characterized the pharmacological effects of naldemedine in vitro and in vivo.
methodsThe binding affinity and antagonist activity of naldemedine against recombinant human μ-, δ-, and κ-opioid receptors were assayed in vitro. Pharmacologic effects of naldemedine were investigated using animal models of morphine-induced inhibition of small and large intestinal transit, castor oil-induced diarrhea, antinociception, and morphine withdrawal. KEY
resultsNaldemedine showed potent binding affinity and antagonist activities for recombinant human μ-, δ-, and κ-opioid receptors. Naldemedine significantly reduced opioid-induced inhibition of small intestinal transit (0.03-10 mg kg CONCLUSIONS & INFERENCES: Naldemedine displayed potent binding affinity to, and antagonistic activity against, μ-, δ-, and κ-opioid receptors. Naldemedine tempered OIC in vivo without compromising opioid analgesia.
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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.