ArticleNaunyn-Schmiedeberg's archives of pharmacology2004
Inhibition of TRPM2 channels by the antifungal agents clotrimazole and econazole.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 80 papers.
What it found
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Who cites it
80 citing papers in PubMed, 160 citations in OpenAlex.
- Pathophysiological significance of the TRPM2 ion channel as a potential target in cancer, neurological disorders, and ischemia/reperfusion injury.Pharmacological research · 2026Review
- Physiological functions and pharmacological targeting of transient receptor potential channels.Pharmacological reviews · 2025Review
- ROS-Activated TRPM2 Channel: Calcium Homeostasis in Cardiovascular/renal System and Speculation in Cardiorenal Syndrome.Cardiovascular drugs and therapy · 2025Review
- TRPM2 channels mediate ROS-induced actin remodeling and cell migration of prostate cancer cells.BMC cancer · 2025Article
- Light-powered phagocytic macrophage microrobot (phagobot): both in vitro and in vivo.Light, science & applications · 2025Article
- Stimulus-Transcription Coupling of TRPM3 Channels: A Signaling Pathway from the Plasma Membrane to the Nucleus.Biomolecules · 2025Review
- [Advances in the development of transient receptor potential melastatin 2 channel inhibitors].Zhejiang da xue xue bao. Yi xue ban = Journal of Zhejiang University. Medical sciences · 2025Review
- Metal Ion Signaling in Biomedicine.Chemical reviews · 2025Review
- Nociceptive transient receptor potential ankyrin 1 (TRPA1) in sensory neurons are targets of the antifungal drug econazole.BMC pharmacology & toxicology · 2024Article
- TRPM2 and CaMKII Signaling Drives Excessive GABAergic Synaptic Inhibition Following Ischemia.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2024Article
- TLR4 induced TRPM2 mediated neuropathic pain.Frontiers in pharmacology · 2024Review
- The TRPM2 ion channel regulates metabolic and thermogenic adaptations in adipose tissue of cold-exposed mice.Frontiers in endocrinology · 2024Article
- The transient receptor potential melastatin 2: a new therapeutical target for Parkinson's disease?Neural regeneration research · 2023Review
- TRPM2 Channels: A Potential Therapeutic Target in Melanoma?International journal of molecular sciences · 2023Review
- Temperature modulates PVN pre-sympathetic neurones via transient receptor potential ion channels.Frontiers in pharmacology · 2023Article
- Cell death induction and protection by activation of ubiquitously expressed anion/cation channels. Part 3: the roles and properties of TRPM2 and TRPM7.Frontiers in cell and developmental biology · 2023Review
- TRPM2: bridging calcium and ROS signaling pathways-implications for human diseases.Frontiers in physiology · 2023Review
- Role of TRPM2 in brain tumours and potential as a drug target.Acta pharmacologica Sinica · 2022Review
- Inhibition of TRPM2 by AG490 Is Neuroprotective in a Parkinson's Disease Animal Model.Molecular neurobiology · 2022Article
- Pharmacological Modulation and (Patho)Physiological Roles of TRPM4 Channel-Part 1: Modulation of TRPM4.Pharmaceuticals (Basel, Switzerland) · 2022Review
20 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
TRPM2 is a Ca(2+)-permeable non-selective cation channel that uniquely is activated by intracellular ADP-ribose. To date, only one pharmacological blocker of this channel, namely flufenamic acid (FFA), has been described. Here we demonstrate, using patch clamp electrophysiology, that the antifungal imidazoles clotrimazole and econazole inhibit ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2 (hTRPM2). For both compounds, all concentrations in a range from 3 microM to 30 microM produced an essentially complete inhibition of the TRPM2-mediated current. The rate of current antagonism was dependent on the concentration applied, with higher concentrations producing faster block. In addition, decreasing extracellular pH accelerated inhibition of TRPM2 by both clotrimazole and econazole; extracellular alkalisation produced the converse effect. Additional experiments indicated hTRPM2 activation was required for the antagonism of either compound to develop, and that neither compound blocked from the intracellular face of the plasma membrane. ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1 were also antagonised by clotrimazole. Contrary to the observations made with hTRPM2, antagonism in CRI-G1 cells could be largely reversed following clotrimazole removal. These experiments suggest that imidazole antifungals may be useful tool antagonists for future studies of TRPM2 function.
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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.