ArticleBritish journal of pharmacology2015
μ-Opioid receptor activation and noradrenaline transport inhibition by tapentadol in rat single locus coeruleus neurons.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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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
8 citing papers in PubMed, 20 citations in OpenAlex.
- Characterization of the Pharmacokinetics and Physiological Effects of Tapentadol in Horses.Journal of veterinary pharmacology and therapeutics · 2026Article
- The role of perioperative tapentadol in inguinal hernia repair: Implications for acute analgesia and chronic postoperative pain - a narrative review.Hernia : the journal of hernias and abdominal wall surgery · 2026Review
- Analysis of Opioid-Related Adverse Events in Japan Using FAERS Database.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Tapentadol shows lower intrinsic efficacy at µ receptor than morphine and oxycodone.Pharmacology research & perspectives · 2022Article
- A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Tapentadol Extended Release in the Treatment of Severe Chronic Low Back Pain and Osteoarthritis Pain.Pain and therapy · 2018Review
- The switch from buprenorphine to tapentadol: is it worth?Romanian journal of anaesthesia and intensive care · 2016Review
- Themed section.British journal of pharmacology · 2015Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeTapentadol is a novel analgesic that combines moderate μ-opioid receptor agonism and noradrenaline reuptake inhibition in a single molecule. Both mechanisms of action are involved in producing analgesia; however, the potency and efficacy of tapentadol in individual neurons has not been characterized. EXPERIMENTAL APPROACH: Whole-cell patch-clamp recordings of G-protein-coupled inwardly rectifying K(+) (KIR 3.x) currents were made from rat locus coeruleus neurons in brain slices to investigate the potency and relative efficacy of tapentadol and compare its intrinsic activity with other clinically used opioids. KEY
resultsTapentadol showed agonist activity at μ receptors and was approximately six times less potent than morphine with respect to KIR 3.x current modulation. The intrinsic activity of tapentadol was lower than [Met]enkephalin, morphine and oxycodone, but higher than buprenorphine and pentazocine. Tapentadol inhibited the noradrenaline transporter (NAT) with potency similar to that at μ receptors. The interaction between these two mechanisms of action was additive in individual LC neurons. CONCLUSIONS AND IMPLICATIONS: Tapentadol displays similar potency for both µ receptor activation and NAT inhibition in functioning neurons. The intrinsic activity of tapentadol at the μ receptor lies between that of buprenorphine and oxycodone, potentially explaining the favourable profile of side effects, related to μ receptors. LINKED ARTICLES: This article is part of a themed section on Opioids: New Pathways to Functional Selectivity. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2015.172.issue-2.
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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.