ArticleBritish journal of pharmacology2017
The anti-migraine component of butterbur extracts, isopetasin, desensitizes peptidergic nociceptors by acting on TRPA1 cation channel.
Article in British journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 76 citations in OpenAlex.
- Sesquiterpene Lactone Derivatives ofPharmaceuticals (Basel, Switzerland) · 2026Article
- Evaluation of the antimigraine and anti-neuroinflammatory activity of purified constituents of Petasites hybridus L. in a migraine-like pain model in mice.Inflammopharmacology · 2026Article
- Nutraceuticals and Headache 2024: Riboflavin, Coenzyme Q10, Feverfew, Magnesium, Melatonin, and Butterbur.Current pain and headache reports · 2025Review
- Bridging Gaps in Migraine Management: A Comprehensive Review of Conventional Treatments, Natural Supplements, Complementary Therapies, and Lifestyle Modifications.Pharmaceuticals (Basel, Switzerland) · 2025Review
- The TRPA1 Ion Channel Mediates Oxidative Stress-Related Migraine Pathogenesis.Molecules (Basel, Switzerland) · 2024Review
- Genetic and immune identification and functional analysis of TRPM8 as a potential biomarker for pancreatic adenocarcinoma proliferation.Cancer reports (Hoboken, N.J.) · 2024Article
- New perspectives on migraine treatment: a review of the mechanisms and effects of complementary and alternative therapies.Frontiers in neurology · 2024Review
- Xenobiotic Exposure and Migraine-Associated Signaling: A Multimethod Experimental Study Exploring Cellular Assays in Combination withEnvironmental health perspectives · 2023Article
- Epigenetic Connections of the TRPA1 Ion Channel in Pain Transmission and Neurogenic Inflammation - a Therapeutic Perspective in Migraine?Molecular neurobiology · 2023Review
- Targeting Nociceptive Neurons and Transient Receptor Potential Channels for the Treatment of Migraine.International journal of molecular sciences · 2023Review
- Modification of the TRP Channel TRPA1 as a Relevant Factor in Migraine-Related Intracranial Hypersensitivity.International journal of molecular sciences · 2023Review
- Exploration of phytochemicals and probing potential effects of3 Biotech · 2023Article
- Bipartite Activation of Sensory Neurons by a TRPA1 Agonist Allyl Isothiocyanate Is Reflected by Complex CaInternational journal of molecular sciences · 2023Article
- Neuronal and non-neuronal TRPA1 as therapeutic targets for pain and headache relief.Temperature (Austin, Tex.) · 2023Review
- Different Involvement of ASIC and TRPA1 in Facial and Hindpaw Allodynia in Nitroglycerin-Induced Peripheral Hypersensitivities in Mice.Life (Basel, Switzerland) · 2022Article
- Petasites for Migraine Prevention: New Data on Mode of Action, Pharmacology and Safety. A Narrative Review.Frontiers in neurology · 2022Review
- Brain Energy Deficit as a Source of Oxidative Stress in Migraine: A Molecular Basis for Migraine Susceptibility.Neurochemical research · 2021Review
- Petasin and isopetasin reduce CGRP release from trigeminal afferents indicating an inhibitory effect on TRPA1 and TRPV1 receptor channels.The journal of headache and pain · 2021Article
- The Role of TRPA1 in Skin Physiology and Pathology.International journal of molecular sciences · 2021Review
- Herbal Medicine for Pain Management: Efficacy and Drug Interactions.Pharmaceutics · 2021Review
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe mechanism of the anti-migraine action of extracts of butterbur [Petasites hybridus (L.) Gaertn.] is unknown. Here, we investigated the ability of isopetasin, a major constituent of these extracts, to specifically target TRPA1 channel and to affect functional responses relevant to migraine. EXPERIMENTAL APPROACH: Single-cell calcium imaging and patch-clamp recordings in human and rodent TRPA1-expressing cells, neurogenic motor responses in rodent isolated urinary bladder, release of CGRP from mouse spinal cord in vitro and facial rubbing in mice and meningeal blood flow in rats were examined. KEY
resultsIsopetasin induced (i) calcium responses and currents in rat/mouse trigeminal ganglion (TG) neurons and in cells expressing the human TRPA1, (ii) substance P-mediated contractions of rat isolated urinary bladders and (iii) CGRP release from mouse dorsal spinal cord, responses that were selectively abolished by genetic deletion or pharmacological antagonism of TRPA1 channels. Pre-exposure to isopetasin produced marked desensitization of allyl isothiocyanate (AITC, TRPA1 channel agonist)- or capsaicin (TRPV1 channel agonist)-evoked currents in rat TG neurons, contractions of rat or mouse bladder and CGRP release from mouse central terminals of primary sensory neurons. Repeated intragastric administration of isopetasin attenuated mouse facial rubbing, evoked by local AITC or capsaicin, and dilation of rat meningeal arteries by acrolein or ethanol (TRPA1 and TRPV1 channel agonists respectively). CONCLUSION AND IMPLICATIONS: Activation of TRPA1 channels by isopetasin results in excitation of neuropeptide-containing nociceptors, followed by marked heterologous neuronal desensitization. Such atten uation in pain and neurogenic inflammation may account for the anti-migraine action of butterbur.
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