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Updated: Jun 5, 2026
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Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3
Published on: August 17, 2011
Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3
Chihab Klose1, Isabelle Straub, Marc Riehle
1Department of Pharmacology and Experimental Therapy, Institute of Experimental and Clinical Pharmacology and Toxicology, Interfaculty Center of Pharmacogenomics and Pharmaceutical Research (ICePhA), Eberhard-Karls-University, Tübingen, Germany.
British Journal of Pharmacology
|January 5, 2011
Summary
Mefenamic acid selectively blocks the TRPM3 channel, a key player in cellular calcium regulation. This finding offers new insights into the function of TRPM3 channels and potential therapeutic applications.
Area of Science:
- Pharmacology
- Cell Biology
- Ion Channel Physiology
Background:
- Fenamates are non-steroid anti-inflammatory drugs.
- Fenamates are known to affect cellular volume regulation.
- Interest in transient receptor potential (TRP) channels, specifically TRPM3 and TRPV4.
Purpose of the Study:
- To investigate fenamates as modulators of TRP channels.
- To characterize the blocking potencies and selectivities of fenamates on TRPM3, TRPV4, TRPC6, and TRPM2.
- To examine the effects of mefenamic acid on calcium (Ca2+) and membrane voltage in cells expressing TRPM3.
Main Methods:
- Calcium imaging in HEK293 cells to measure fenamate blocking potencies.
- Electrophysiology to assess membrane voltage changes.
- Experiments in insulin-secreting INS-1E cells to validate mefenamic acid's effects on Ca2+ and insulin secretion.
Main Results:
- Mefenamic acid was identified as a selective and potent blocker of TRPM3.
- Other fenamates showed non-selective blocking of TRPM3, TRPV4, TRPC6, and TRPM2.
- Mefenamic acid selectively inhibited TRPM3-mediated calcium entry and pregnenolone sulphate-induced insulin secretion.
Conclusions:
- Mefenamic acid is a selective inhibitor of TRPM3.
- The study confirmed mefenamic acid's selectivity in insulin-secreting cells.
- Further research is needed to understand TRPM3's physiological role and the impact of its inhibition on pancreatic beta-cell function.
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