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Related Concept Videos

Antiepileptic Drugs: Potassium Channel Activators01:20

Antiepileptic Drugs: Potassium Channel Activators

Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers01:22

Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers

Class I antiarrhythmic drugs are used to treat various types of arrhythmias or irregular heart rhythms. These drugs block the sodium (Na+) channels in the cardiac cells, thereby affecting the movement of electrical impulses across the heart. Class I antiarrhythmic drugs are divided into three subgroups: Class IA, Class IB, and Class IC, each with distinct mechanisms of action and effects on the heart.
Class 1A Antiarrhythmic Drugs: These drugs work by moderately blocking sodium channels,...
Ion Channels01:19

Ion Channels

The movement of ions like sodium, potassium, and calcium into and out of the cell is essential to maintain the electrochemical gradient in living cells. The ion channels—a class of membrane transport proteins—help maintain this ionic gradient for the smooth functioning of physiological activities such as maintaining cell size and volume, conducting nerve impulses, and gas and nutrient exchange.
Ion channels are specialized integral membrane proteins on the plasma membrane that allow specific...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers01:12

Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers

Class III antiarrhythmic drugs are a group of medications that can prolong action potentials in the heart. They achieve this by blocking potassium channels or enhancing inward currents from sodium channels. However, these drugs have a unique property of "reverse use-dependence," which is most pronounced at slower heart rates and can lead to torsades de pointes—a specific type of arrhythmia. However, it is essential to note that excessive QT interval prolongation—a measure of the heart's...
Antiepileptic Drugs: Sodium Channel Blockers01:08

Antiepileptic Drugs: Sodium Channel Blockers

Antiepileptic drugs are specialized medications that prevent seizures in individuals diagnosed with epilepsy. These drugs primarily function by blocking the movement of sodium ions through channels in the neuronal membrane, inhibiting the repetitive firing of action potentials often associated with seizures.
Sodium channel blockers modulate ion channels, particularly voltage-gated sodium channels. They block only sodium ion movement.
Among the most commonly prescribed antiepileptic drugs are...

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Related Experiment Video

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
06:59

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

Pharmacology & Therapeutics
|January 30, 2013
PubMed
Summary

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.

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  • 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.