ArticleThe Journal of biological chemistry2014
Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel.
Article in The Journal of biological chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 54 citations in OpenAlex.
- Clinical Efficacy of Hexue Tongbi Formula on Oxaliplatin-Induced Peripheral Neuropathy: A Randomized Controlled Study.Integrative cancer therapiesTrial
- Article
- New options for targeting TRPV1 receptors for cancer treatment: odorous Chinese herbal medicine.Frontiers in oncology · 2025Review
- Phytochemical-based therapeutics from traditional eastern medicine: analgesic effects and ion channel modulation.Frontiers in pain research (Lausanne, Switzerland) · 2025Review
- Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.Current topics in medicinal chemistry · 2025Review
- Dihydroceramides Derived from Bacteroidetes Species Sensitize TRPV1 Channels.International journal of molecular sciences · 2023Article
- Neuropathic ocular surface pain: Emerging drug targets and therapeutic implications.Expert opinion on therapeutic targets · 2022Review
- TheFrontiers in pharmacology · 2022Review
- Regulation of transient receptor potential channels by traditional Chinese medicines and their active ingredients.Frontiers in pharmacology · 2022Review
- Molecular Mechanism of theEvidence-based complementary and alternative medicine : eCAM · 2022Article
- Review
- Desensitization of TRPV1 Involved in the Antipruritic Effect of Osthole on Histamine-Induced Scratching Behavior in Mice.Evidence-based complementary and alternative medicine : eCAM · 2021Article
- Long-Term Diabetic Microenvironment Augments the Decay Rate of Capsaicin-Induced Currents in Mouse Dorsal Root Ganglion Neurons.Molecules (Basel, Switzerland) · 2019Article
- Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives.International immunopharmacology · 2016Review
- Osthole inhibits histamine-dependent itch via modulating TRPV1 activity.Scientific reports · 2016Article
- Selective Activation of Nociceptor TRPV1 Channel and Reversal of Inflammatory Pain in Mice by a Novel Coumarin Derivative Muralatin L from Murraya alata.The Journal of biological chemistry · 2016Article
- A Multicenter, Double-Blind, Randomized, Placebo-Controlled Trial to Evaluate the Efficacy and Safety of Duliang Soft Capsule in Patients with Chronic Daily Headache.Evidence-based complementary and alternative medicine : eCAM · 2015Article
- Mechanisms underlying capsaicin effects in canine coronary artery: implications for coronary spasm.Cardiovascular research · 2014Article
- Sensitive skin: review of an ascending concept.Anais brasileiros de dermatologiaReview
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
Furanocoumarin imperatorin is the major active component of Angelica dahurica root extracts, widely used in traditional medicine to treat headache, toothache, and orbital eye pain. In this study, we investigated the mechanisms that may underlie the pain-relieving effects of the compound. We found that imperatorin significantly inhibited formalin- and capsaicin-induced nocifensive responses but did not alter baseline thermal withdrawal thresholds in the rat. We established that imperatorin is a weak agonist of TRPV1, a channel implicated in detecting several noxious stimuli, exhibiting a 50% effective concentration (EC50) of 12.6 ± 3.2 μM. A specific TRPV1 antagonist, JNJ-17203212 (0.5 μM), potently inhibited imperatorin-induced TRPV1 activation. Site-directed mutagenesis studies revealed that imperatorin most likely acted via a site adjacent to or overlapping with the TRPV1 capsaicin-binding site. TRPV1 recovery from desensitization was delayed in the presence of imperatorin. Conversely, imperatorin sensitized TRPV1 to acid activation but did not affect the current amplitude and/or the activation-inactivation properties of Na(v)1.7, a channel important for transmission of nociceptive information. Thus, our data indicate that furanocoumarins represent a novel group of TRPV1 modulators that may become important lead compounds in the drug discovery process aimed at developing new treatments for pain management.
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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.