ArticleNeuroscience2009
Nalfurafine prevents 5'-guanidinonaltrindole- and compound 48/80-induced spinal c-fos expression and attenuates 5'-guanidinonaltrindole-elicited scratching behavior in mice.
Article in Neuroscience, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 47 citations in OpenAlex.
- The synthetic cannabinoid agonist WIN 55,212-2 reduces experimental pruritus via CBNeuropharmacology · 2025Article
- Treatment Options for Troublesome Itch.Pharmaceuticals (Basel, Switzerland) · 2022Review
- The Kappa Opioid Receptor: A Promising Therapeutic Target for Multiple Pathologies.Frontiers in pharmacology · 2022Review
- Antipruritic Effects of Kappa Opioid Receptor Agonists: Evidence from Rodents to Humans.Handbook of experimental pharmacology · 2022Article
- Kappa Opioid Receptor Ligands and Pharmacology: Diphenethylamines, a Class of Structurally Distinct, Selective Kappa Opioid Ligands.Handbook of experimental pharmacology · 2022Review
- Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist.Handbook of experimental pharmacology · 2022Article
- Antinociceptive and Antipruritic Effects of HSK21542, a Peripherally-Restricted Kappa Opioid Receptor Agonist, in Animal Models of Pain and Itch.Frontiers in pharmacology · 2021Article
- 3'-O-Methylorobol Inhibits the Voltage-Gated Sodium Channel Nav1.7 with Anti-Itch Efficacy in A Histamine-Dependent Itch Mouse Model.International journal of molecular sciences · 2019Article
- Nalbuphine, a kappa opioid receptor agonist and mu opioid receptor antagonist attenuates pruritus, decreases IL-31, and increases IL-10 in mice with contact dermatitis.European journal of pharmacology · 2019Article
- A Review of the Therapeutic Potential of Recently Developed G Protein-Biased Kappa Agonists.Frontiers in pharmacology · 2019Review
- Manual acupuncture relieves bile acid-induced itch in mice: the role of microglia and TNF-α.International journal of medical sciences · 2018Article
- Nalfurafine is a G-protein biased agonist having significantly greater bias at the human than rodent form of the kappa opioid receptor.Cellular signalling · 2017Article
- Generation of a KOR-Cre knockin mouse strain to study cells involved in kappa opioid signaling.Genesis (New York, N.Y. : 2000) · 2016Article
- Phoenixin: A candidate pruritogen in the mouse.Neuroscience · 2015Article
- Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritus.Neuropharmacology · 2015Article
- Salvinorin A analogues PR-37 and PR-38 attenuate compound 48/80-induced itch responses in mice.British journal of pharmacology · 2015Article
- Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.ACS chemical neuroscience · 2015Article
- Scratching activates microglia in the mouse spinal cord.Journal of neuroscience research · 2015Article
- Nalfurafine suppresses pruritogen- and touch-evoked scratching behavior in models of acute and chronic itch in mice.Acta dermato-venereologica · 2015Article
- Neuraxial opioid-induced itch and its pharmacological antagonism.Handbook of experimental pharmacology · 2015Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The aims of the present study were to establish if nalfurafine, a kappa opioid agonist, inhibits compulsive scratching in mice elicited by the s.c. administration (behind the neck) of 5'-guanidinonaltrindole (GNTI), a kappa opioid antagonist; to assess if nalfurafine prevents c-fos expression provoked by GNTI or compound 48/80, two chemically diverse pruritogens; and to distinguish on the basis of neuroanatomy, those neurons in the brainstem activated by either GNTI-induced itch or formalin-induced pain (both compounds given s.c. to the right cheek). Pretreatment of mice with nalfurafine (0.001-0.03 mg/kg s.c.) attenuated GNTI (0.3 mg/kg)-evoked scratching dose-dependently. A standard antiscratch dose of nalfurafine (0.02 mg/kg) had no marked effect on the spontaneous locomotion of mice. Tolerance did not develop to the antiscratch activity of nalfurafine. Both GNTI and compound 48/80 provoked c-fos expression on the lateral side of the superficial layer of the dorsal horn of the cervical spinal cord and pretreating mice with nalfurafine inhibited c-fos expression induced by both pruritogens. In contrast to formalin, GNTI did not induce c-fos expression in the trigeminal nucleus suggesting that pain and itch sensations are projected differently along the sensory trigeminal pathway. Our data indicate that the kappa opioid system is involved, at least in part, in the pathogenesis of itch; and that nalfurafine attenuates excessive scratching and prevents scratch-induced neuronal activity at the spinal level. On the basis of our results, nalfurafine holds promise as a potentially useful antipruritic in human conditions involving itch.
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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.