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Updated: Oct 6, 2025

Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
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Pharmacological Modulation and (Patho)Physiological Roles of TRPM4 Channel-Part 1: Modulation of TRPM4

Zsigmond Máté Kovács1,2, Csaba Dienes1,2, Tamás Hézső1,2

  • 1Department of Physiology, Faculty of Medicine, University of Debrecen, 4032 Debrecen, Hungary.

Pharmaceuticals (Basel, Switzerland)
|January 21, 2022
PubMed

Insights

Transient receptor potential melastatin 4 (TRPM4) is a Ca2+-sensitive ion channel involved in cell functions. This review details TRPM4

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Transient receptor potential melastatin 4 (TRPM4) is a Ca2+-sensitive ion channel permeable to monovalent cations.
  • TRPM4 plays a crucial role in regulating membrane potential and Ca2+ homeostasis in various cell types.
  • Its widespread expression highlights its significance in diverse physiological processes.

Purpose of the Study:

  • To review the pharmacological modulation of TRPM4.
  • To compare and describe endogenous and exogenous activators and inhibitors of TRPM4.
  • To outline alternative strategies for studying TRPM4 function.

Main Methods:

  • Literature review of pharmacological agents targeting TRPM4.
  • Description of TRPM4 activators and inhibitors.
  • Overview of TRPM4 research tools including siRNA, dominant-negative variants, and antibodies.

Main Results:

  • Identification and categorization of various TRPM4 modulators.
  • Detailed comparison of the effects of different activators and inhibitors.
  • Summary of the utility of different experimental approaches in TRPM4 research.

Conclusions:

  • TRPM4 is a significant ion channel with diverse functions.
  • Pharmacological strategies and other research tools are vital for understanding TRPM4.
  • TRPM4 is a promising target for future research and therapeutic development.
Keywords:
9-phenanthrolCBASUR1TRPM4TRPM4 activatorTRPM4 inhibitorantibodyflufenamic acidsiRNA

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