ArticleMolecules (Basel, Switzerland)2021
Antipruritic Effect of Nalbuphine, a Kappa Opioid Receptor Agonist, in Mice: A Pan Antipruritic.
Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 19 citations in OpenAlex.
- Kappa opioids suppress histaminergic itch by inhibiting mediodorsal thalamus-projecting claustrum glutamatergic neurons.Science advances · 2026Article
- Genetic Variation A118G in the OPRM1 Gene Underlies the Dimorphic Response to Epidural Opioid-Induced Itch.Neuroscience bulletin · 2025Article
- Opioid-Induced Pruritus: A Case Series on Novel Uses of Nalbuphine in the Emergency Department.Journal of the American College of Emergency Physicians open · 2025Article
- Identification of VGLUT3-expressing LTMRs-recruited spinal circuits for itch inhibition.Molecular brain · 2025Article
- Anti-inflammatory and renoprotective effects of difelikefalin, a kappa opioid receptor agonist, in a rat model of renal ischemia-reperfusion-induced acute kidney injury.BMC nephrology · 2025Article
- Limitations and potential of κOR biased agonists for pain and itch management.Neuropharmacology · 2024Review
- Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine-Independent and Chronic Itch.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Nalbuphine May Be Superior to Sufentanil in Relieving Postcesarean Uterine Contraction Pain in Multiparas: A Retrospective Cohort Study.Drug design, development and therapy · 2023Article
- Role of kappa-opioid and mu-opioid receptors in pruritus: Peripheral and central itch circuits.Experimental dermatology · 2022Article
- Cholestatic Itch: Our Current Understanding of Pathophysiology and Treatments.American journal of clinical dermatology · 2022Review
- Difelikefalin in the Treatment of Chronic Kidney Disease-Associated Pruritus: A Systematic Review.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery II.Molecules (Basel, Switzerland) · 2022Article
- Opioidergic Signaling-A Neglected, Yet Potentially Important Player in Atopic Dermatitis.International journal of molecular sciences · 2022Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Antipruritic effects of kappa opioid receptor (KOR) agonists have been shown in rodent models of acute and chronic scratching (itchlike behavior). Three KOR agonists, nalfurafine, difelikefalin, and nalbuphine, are in clinical studies for antipruritic effects in chronic itch of systemic and skin diseases. Nalfurafine (in Japan) and difelikefalin (in the USA) were approved to be used in the treatment of chronic itch in hemodialysis patients. The FDA-approved nalbuphine has been used in clinic for over 40 years, and it is the only narcotic agonist that is not scheduled. We aimed to study (a) antiscratch activity of nalbuphine against TAT-HIV-1 protein (controls HIV transcription)-, deoxycholic acid (DCA, bile acid)-, and chloroquine (CQ)-induced scratching in a mouse model of acute itch; and (b) whether the effect of nalbuphine is produced via KORs. First, dose-responses were developed for pruritogens. Mice were pretreated with nalbuphine (0.3-10 mg/kg) and then a submaximal dose of pruritogens were administered and the number of scratching bouts was counted. To study if the antiscratch effect of nalbuphine is produced via KOR, we used KOR knock out mice and pharmacologic inhibition of KORs using nor-binaltorphimine, a KOR antagonist. For this aim, we used CQ as a pruritogen. We found that: (a) TAT-HIV-1 protein elicits scratching in a dose-dependent manner; (b) nalbuphine inhibits scratching induced by TAT-HIV-1, DCA, and CQ dose-dependently; and (c) nalbuphine inhibits scratching induced by CQ through KORs. In conclusion, nalbuphine inhibits scratching elicited by multiple pruritogens.
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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.