ArticleBritish journal of pharmacology2018
Opioid-induced inhibition of the human 5-HT and noradrenaline transporters in vitro: link to clinical reports of serotonin syndrome.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers, 3 of them syntheses that pooled it.
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Who cites it
46 citing papers in PubMed, 3 syntheses or guidelines pooled it, 100 citations in OpenAlex.
- Precipitants and clinical features of serotonin syndrome: a systematic review with patient-level analysis of published case reports and series.European journal of clinical pharmacology · 2026Pooled it
- Executive summary of the guideline for prescribing opioid analgesics for chronic non-cancer pain (third edition) by the Japan Society of Pain Clinicians.Journal of anesthesia · 2025Guideline
- Pooled it
- AI-derived therapeutic development of a serotonin receptor-targeting drug for the treatment of opioid use disorder.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
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- Psychiatric, Cardiovascular and Skeletal Risks of Codeine versus Oxycodone in Hip Osteoarthritis: A Population-Based Cohort Study.Drug design, development and therapy · 2026Article
- Methadone Prescribing Patterns at a Single Institution: A Retrospective Study and Clinical Implications.Psychopharmacology bulletin · 2025Article
- Declines in Tapentadol Use in the US but Pronounced Regional Variation.Pharmacy (Basel, Switzerland) · 2025Article
- The Relevance of Pharmacokinetic Biomarkers in Response to Methadone Treatment: A Systematic Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Methadone for Chronic Pain: A Review of Pharmacology, Efficacy, and Safety Concerns.Health psychology research · 2025Article
- Individual Pharmacotherapy Management (IPM-II) for Patient and Drug Safety in Polypharmacy via Clinical Electronic Health Record Is Associated with Significant Fall Prevention.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Resolution of tonic concentrations of highly similar neurotransmitters using voltammetry and deep learning.Molecular psychiatry · 2024Article
- Cross state-dependent memory retrieval between tramadol and ethanol: involvement of dorsal hippocampal GABAA receptors.Psychopharmacology · 2024Article
- Guidelines for Rational Clinical Use of Fentanyl Transdermal Patch.Drug design, development and therapy · 2024Article
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- High and Hyper: Fentanyl Induces Psychomotor Side-Effects in Healthy Pigs.Animals : an open access journal from MDPI · 2023Article
- The Analysis of Pethidine Pharmacokinetics in Newborn Saliva, Plasma, and Brain Extracellular Fluid After Prenatal Intrauterine Exposure from Pregnant Mothers Receiving Intramuscular Dose Using PBPK Modeling.European journal of drug metabolism and pharmacokinetics · 2023Article
- Increase of high-risk tramadol use and harmful consequences in France from 2013 to 2018: Evidence from the triangulation of addictovigilance data.British journal of clinical pharmacology · 2022Article
- A Cross-sectional Analysis of Linezolid in Combination with Methadone or Buprenorphine as a Cause of Serotonin Toxicity.Open forum infectious diseases · 2022Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeOpioids may inhibit the 5-HT transporter (SERT) and the noradrenaline transporter (NET). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with 5-HT receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET and 5-HT receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected HEK293 cells. We also tested binding affinities at 5-HT KEY
resultsDextromethorphan, l(R)-methadone, racemic methadone, pethidine, tramadol and tapentadol inhibited the SERT at or close to observed drug plasma or estimated brain concentrations in patients. Tapentadol was the most potent NET inhibitor. Pethidine, tramadol, l(R)-methadone, racemic methadone, dextromethorphan and O-desmethyltramadol also inhibited the NET. 6-Monoacetylmorphine, buprenorphine, codeine, dihydrocodeine, heroin, hydrocodone, hydromorphone, morphine, oxycodone and oxymorphone did not inhibit the SERT or NET. Fentanyl interacted with 5-HT CONCLUSIONS AND IMPLICATIONS: Some synthetic opioids interact with the SERT and NET at potentially clinically relevant concentrations. SERT inhibition by tramadol, tapentadol, methadone, dextromethorphan and pethidine may contribute to the serotonin syndrome. Direct effects on 5-HT
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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.