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Updated: May 14, 2026

A Fluorescence-Based Assay of Membrane Potential for High-Throughput Functional Study of Two Endogenous Ion Channels in Two Epithelial Cell Lines
Published on: June 22, 2022
Flufenamic acid as an ion channel modulator
Romain Guinamard1, Christophe Simard, Christopher Del Negro
1Normandie Univ, France. romain.guinamard@unicaen.fr
Abstract:
Flufenamic acid has been known since the 1960s to have anti-inflammatory properties attributable to the reduction of prostaglandin synthesis. Thirty years later, flufenamic acid appeared to be an ion channel modulator. Thus, while its use in medicine diminished, its use in ionic channel research expanded. Flufenamic acid commonly not only affects non-selective cation channels and chloride channels, but also modulates potassium, calcium and sodium channels with effective concentrations ranging from 10(-6)M in TRPM4 channel inhibition to 10(-3)M in two-pore outwardly rectifying potassium channel activation. Because flufenamic acid effects develop and reverse rapidly, it is a convenient and widely used tool. However, given the broad spectrum of its targets, experimental results have to be interpreted cautiously. Here we provide an overview of ion channels targeted by flufenamic acid to aid in interpreting its effects at the molecular, cellular, and system levels. If it is used with good practices, flufenamic acid remains a useful tool for ion channel research. Understanding the targets of FFA may help reevaluate its physiological impacts and revive interest in its therapeutic potential.
Insights
Flufenamic acid, known for anti-inflammatory effects, also modulates various ion channels. Careful interpretation is needed due to its broad targets, but it remains a valuable research tool.
Area of Science:
- Pharmacology
- Molecular Biology
- Physiology
Background:
- Flufenamic acid (FFA) was identified in the 1960s for anti-inflammatory properties via prostaglandin synthesis inhibition.
- Later, FFA was recognized as an ion channel modulator, shifting its application from medicine to research.
- Its rapid action and reversibility make FFA a convenient research tool.
Purpose of the Study:
- To provide an overview of ion channels modulated by flufenamic acid.
- To aid researchers in interpreting experimental results involving FFA.
- To explore the potential for reevaluating FFA's therapeutic applications.
Main Methods:
- Literature review of studies on flufenamic acid's effects on ion channels.
- Analysis of effective concentrations for FFA modulation across different channel types.
- Compilation of data on FFA's impact at molecular, cellular, and system levels.
Main Results:
- Flufenamic acid modulates non-selective cation, chloride, potassium, calcium, and sodium channels.
- Effective concentrations vary widely, from 10⁻⁶ M (TRPM4 inhibition) to 10⁻³ M (two-pore potassium channel activation).
- FFA exhibits a broad spectrum of ion channel targets.
Conclusions:
- Flufenamic acid is a versatile tool for ion channel research when used cautiously.
- Understanding FFA's diverse targets is crucial for accurate experimental interpretation.
- Further research into FFA's targets may reveal new therapeutic possibilities.
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