ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2023
Opioid antagonism in humans: a primer on optimal dose and timing for central mu-opioid receptor blockade.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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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.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.
- Endogenous mu-opioid modulation of social connection in humans: a systematic review and meta-analysis.Translational psychiatry · 2024Pooled it
- Seeing the bigger picture: endogenous opioids mediate attentional broadening after reward receipt.Psychological medicine · 2025Trial
- Effect of oral naloxone on opioid-induced constipation in methadone maintenance treatment patients, a double-blind, placebo-control, clinical trial.Irish journal of medical science · 2024Trial
- The role of endogenous opioids in mindfulness and sham mindfulness-meditation for the direct alleviation of evoked chronic low back pain: a randomized clinical trial.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Trial
- Facial mimicry is not modulated by dopamine D2/3 and opioid receptor antagonism.Psychopharmacology · 2023Trial
- Potential Protective Effects of Naloxone in Traumatic Brain Injury Through JAK2/STAT3 Signaling Modulation.Life (Basel, Switzerland) · 2026Article
- Exploring wanting and liking during positive human-animal interactions.Psychopharmacology · 2026Article
- The role of central versus peripheral opioid receptors in fentanyl-induced brain hypoxia.Journal of neurophysiology · 2026Article
- Trends and Outcomes of Naloxone Use for Iatrogenic Opioid Overdose in Patients on General Wards in a Swiss Hospital: A Ten-Year Retrospective Case Series Analysis.Drug, healthcare and patient safety · 2026Article
- Effects of Rosa damascena and its compounds on smooth muscle contractility.Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi · 2026Review
- Sleep Quality in Chronic Pain Patients With and Without Strong Opioid Use: An Observational Study Using a Wearable Device.Neuropsychopharmacology reports · 2025Observational
- Sedation in endoscopy: Finding the balance between safety and efficacy.World journal of gastrointestinal endoscopy · 2025Article
- Article
- Artificial intelligence approaches for anti-addiction drug discovery.Digital discovery · 2025Review
- Self-regulated analgesia in males but not females is mediated by endogenous opioids.PNAS nexus · 2024Article
- Enhancing translation: A need to leverage complex preclinical models of addictive drugs to accelerate substance use treatment options.Pharmacology, biochemistry, and behavior · 2024Review
- Clinical Pharmacokinetics and Pharmacodynamics of Naloxone.Clinical pharmacokinetics · 2024Review
- Article
- Clinical Implications of the Relationship Between Naltrexone Plasma Levels and the Subjective Effects of Heroin in Humans.Journal of addiction medicineArticle
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
Abstract
Non-human animal studies outline precise mechanisms of central mu-opioid regulation of pain, stress, affiliation and reward processing. In humans, pharmacological blockade with non-selective opioid antagonists such as naloxone and naltrexone is typically used to assess involvement of the mu-opioid system in such processing. However, robust estimates of the opioid receptor blockade achieved by opioid antagonists are missing. Dose and timing schedules are highly variable and often based on single studies. Here, we provide a detailed analysis of central opioid receptor blockade after opioid antagonism based on existing positron emission tomography data. We also create models for estimating opioid receptor blockade with intravenous naloxone and oral naltrexone. We find that common doses of intravenous naloxone (0.10-0.15 mg/kg) and oral naltrexone (50 mg) are more than sufficient to produce full blockade of central MOR (>90% receptor occupancy) for the duration of a typical experimental session (~60 min), presumably due to initial super saturation of receptors. Simulations indicate that these doses also produce high KOR blockade (78-100%) and some DOR blockade (10% with naltrexone and 48-74% with naloxone). Lower doses (e.g., 0.01 mg/kg intravenous naloxone) are estimated to produce less DOR and KOR blockade while still achieving a high level of MOR blockade for ~30 min. The models and simulations form the basis of two novel web applications for detailed planning and evaluation of experiments with opioid antagonists. These tools and recommendations enable selection of appropriate antagonists, doses and assessment time points, and determination of the achieved receptor blockade in previous studies.
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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.