ArticleScientific reports2018
Pharmacological Characterization of Dezocine, a Potent Analgesic Acting as a κ Partial Agonist and μ Partial Agonist.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers, 2 of them syntheses that pooled it.
What it found
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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
35 citing papers in PubMed, 2 syntheses or guidelines pooled it, 51 citations in OpenAlex.
- Different interventions in preventing sufentanil-induced cough: a systematic review and network meta-analysis.Frontiers in pharmacology · 2025Pooled it
- Pooled it
- Dexmedetomidine-dezocine versus propofol-remifentanil anesthesia for ultrasound-guided transvaginal oocyte retrieval: a randomized controlled trial.BMC anesthesiology · 2025Trial
- Trial
- Comparison of the analgesic effect of dezocine and esketamine in combination with sufentanil respectively after laparoscopic cholecystectomy: a prospective randomized controlled study.BMC anesthesiology · 2024Trial
- The Effect of Dezocine on the Median Effective Dose of Sufentanil-Induced Respiratory Depression in Patients Undergoing Spinal Anesthesia Combined with Low-Dose Dexmedetomidine.Drug design, development and therapy · 2023Trial
- Effect of dezocine on the median effective dose of sufentanil for blunting hemodynamic responses to endotracheal intubation during anesthesia induction.Journal of thoracic disease · 2026Article
- Opioid receptor agonist-antagonists in pain management: receptor specific mechanisms, dose response relationships, and clinical combination strategies.Frontiers in pain research (Lausanne, Switzerland) · 2026Review
- Narcotics through time: exploring historical origins, synthetic advances, and clinical progress.Future medicinal chemistry · 2025Review
- Dezocine and Addiction: Friend or Foe?Pharmaceuticals (Basel, Switzerland) · 2025Review
- Anesthetic management of diabetic foot amputation in a patient with renal failure and maintenance hemodialysis: case report and short communication.American journal of translational research · 2025Article
- Postoperative Pain Management Strategies Following Peroral Endoscopic Myotomy (POEM): A Review.Journal of pain research · 2025Review
- Effects of dezocine with ropivacaine on epidural analgesia during labor: a randomized controlled trial.Frontiers in pharmacology · 2025Article
- Dezocine Exerts Analgesic Effects in Chronic Pain by Activation of κ- and μ-Opioid Receptors and Inhibition of Norepinephrine and Serotonin Reuptake.Pain research & management · 2025Article
- Opioid system and related ligands: from the past to future perspectives.Journal of anesthesia, analgesia and critical care · 2024Review
- Revisiting dezocine for opioid use disorder: A narrative review of its potential abuse liability.CNS neuroscience & therapeutics · 2024Review
- Case report: Dezocine's rapid and sustained antidepressant effects.Frontiers in pharmacology · 2024Article
- The cost-effectiveness analysis of analgesic treatment options for postoperative pain following laparotomy surgeries.International journal of clinical pharmacy · 2023Article
- Dezocine as a potent analgesic: overview of its pharmacological characterization.Acta pharmacologica Sinica · 2022Review
- Dezocine induces apoptosis in human cervical carcinoma Hela cells via the endoplasmic reticulum stress pathway.Toxicology research · 2022Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 1 country.
Funding
Abstract
Dezocine is becoming dominated in China market for relieving moderate to severe pain. It is believed that Dezocine's clinical efficacy and little chance to provoke adverse events during the therapeutic process are mainly attributed to its partial agonist activity at the μ opioid receptor. In the present work, we comprehensively studied the pharmacological characterization of Dezocine and identified that the analgesic effect of Dezocine was a result of action at both the κ and μ opioid receptors. We firstly found that Dezocine displayed preferential binding to μ opioid receptor over κ and δ opioid receptors. Dezocine, on its own, weakly stimulated G protein activation in cells expressing κ and μ receptors, but in the presence of full κ agonist U50,488 H and μ agonist DAMGO, Dezocine inhibited U50,488H- and DAMGO-mediated G protein activation, indicating that Dezocine was a κ partial agonist and μ partial agonist. Then the in intro results were verified by in vivo studies in mice. We observed that Dezocine-produced antinociception was significantly inhibited by κ antagonist nor-BNI and μ antagonist β-FNA pretreatment, indicating that Dezocine-mediated antinociception was via both the κ and μ opioid receptors. When co-administrating of Dezocine with U50,488 H or morphine, Dezocine was capable of inhibiting U50,488H- or morphine-induced antinociception. Finally, κ receptor activation-associated side effect sedation was investigated. We found that Dezocine displayed limited sedative effect with a ceiling effecting at a moderate dose. Thus, our work led to a better understanding of the analgesic mechanism of action of Dezocine in vivo.
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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.