ArticleBritish journal of pharmacology2004
Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 181 papers, 3 of them syntheses that pooled it.
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Who cites it
181 citing papers in PubMed, 3 syntheses or guidelines pooled it, 446 citations in OpenAlex.
- Influence of Inflammation, Gut Microbiota, and Stress on Cognition and Oral Health Therapies.Current Alzheimer research · 2025Pooled it
- Modulation of transient receptor potential (TRP) channels by plant derived substances used in over-the-counter cough and cold remedies.Respiratory research · 2023Pooled it
- Capsaicin for non-allergic rhinitis.The Cochrane database of systematic reviews · 2015Pooled it
- Human heat sensation: A randomized crossover trial.Science advances · 2024Trial
- An Innervated Human Skin Equivalent that Electrically Encodes Mechanical and Thermal Stimuli.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Symmetry-driven gating of TRPM8 by PIPNature communications · 2026Article
- Temperature-Dependent Menthol Binding across TRPM8 Conformational States.Journal of the American Chemical Society · 2026Article
- Influence of Cooling Agents on the Arrhythmogenic and Autonomic Effects of Electronic Cigarettes in an in vivo Model.Circulation. Arrhythmia and electrophysiology · 2026Article
- TRP-Dependent Calcium Regulation in HCEC-12 Cells: Involvement of Ascorbic Acid and Cannabinoid Receptor Signaling.International journal of molecular sciences · 2026Article
- Deletion of the TRPV1 channel attenuates afferent renal nerve responses to renal artery occlusion but not elevated renal pelvic pressure.The Journal of physiology · 2026Article
- Orthonasal bioactive volatiles and their effects on salivation: a pilot study.Clinical oral investigations · 2026Article
- CaCurrent research in toxicology · 2026Article
- The tip of the iceberg: Profiling cooling agents using computational approaches to inform tobacco regulatory science.PloS one · 2026Article
- Cooling sensation biosensor coupled with the Chou-Talalay method for quantitative assessment of interaction patterns in binary cooling agent mixtures.Current research in food science · 2026Article
- Suppression of neuropathic pain hypersensitivity by TRPM8 is mediated by mGluR group II and III receptors acting differentially on distinct nociceptor inputs to spinal cord.Frontiers in pharmacology · 2026Article
- Cold- and TRPM8-dependent shaking in mammals and birds.Communications biology · 2025Article
- Transient receptor melastatin channel in colorectal cancer: pathophysiological mechanisms and a promising drug target.Cancer chemotherapy and pharmacology · 2025Review
- Secondary Metabolites Composition and Their Histochemical Localization in the Fruit of Piper malgassicum Papini, Palchetti, Gori and Rota Nodari (Piperaceae).Chemistry & biodiversity · 2025Article
- Anti-seizure effects of WS-3, a TRPM8 agonist, on focal onset seizure mouse model via reduction of extracellular glutamate levels.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Menthol in Livestock: Unveiling Its Multifaceted Properties and Future Potential for Sustainable Agriculture.International journal of molecular sciences · 2025Review
121 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin. It belongs to the transient receptor potential (TRP) family, and therefore is related to vanilloid receptor type-1 (VR1, TRPV1). We tested whether substances which are structurally related to menthol, or which produce a cooling sensation, could activate TRPM8, and compared the responses of TRPM8 and VR1 to these ligands. 2. The effects of 70 odorants and menthol-related substances on recombinant mouse TRPM8 (mTRPM8), expressed in HEK293 cells, were examined using a FLIPR assay. In all, 10 substances (linalool, geraniol, hydroxycitronellal, WS-3, WS-23, FrescolatMGA, FrescolatML, PMD38, CoolactP and Cooling Agent 10) were found to be agonists. 3. The EC(50) values of the agonists defined their relative potencies: icilin (0.2+/-0.1 microM)>FrescolatML (3.3+/-1.5 microM) > WS-3 (3.7+/-1.7 microM) >(-)menthol (4.1+/-1.3 microM) >frescolatMAG (4.8+/-1.1 microM) > cooling agent 10 (6+/-2.2 microM) >(+)menthol (14.4+/-1.3 microM) > PMD38 (31+/-1.1 microM) > WS-23 (44+/-7.3 microM) > Coolact P (66+/-20 microM) > geraniol (5.9+/-1.6 mM) > linalool (6.7+/-2.0 mM) > eucalyptol (7.7+/-2.0 mM) > hydroxycitronellal (19.6+/-2.2 mM). 4. Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively). 5. The Ca(2+) response of hVR1-transfected HEK293 cells to the endogenous VR1 agonist N-arachidonoyl-dopamine was potentiated by low pH. In contrast, menthol- and icilin-activated TRPM8 currents were suppressed by low pH. 6. In conclusion, in the present study, we identified 10 new agonists and three antagonists of TRPM8. We found that, in contrast to VR1, TRPM8 is inhibited rather than potentiated by protons.
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