TRPM4 channels in the cardiovascular system: Physiology, pathophysiology, and pharmacology

The transient receptor potential channel (TRP) family comprises at least 28 genes in the human genome. These channels are widely expressed in many different tissues, including those of the cardiovascular system. The transient receptor potential channel melastatin 4 (TRPM4) is a Ca2+-activated non-sp...

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Bibliographic Details
Published in:Biochemical pharmacology 2012-10, Vol.84 (7), p.873-881
Main Authors: Abriel, Hugues, Syam, Ninda, Sottas, Valentin, Amarouch, Mohamed Yassine, Rougier, Jean-Sébastien
Format: Article
Language:English
Subjects:
Animals
Cardiovascular Agents - chemistry
Cardiovascular Agents - pharmacology
Cardiovascular Agents - therapeutic use
Cardiovascular Diseases - drug therapy
Cardiovascular Diseases - metabolism
Cardiovascular system
Cardiovascular System - metabolism
Channelopathies
Gene Expression Regulation - physiology
genes
Genetic Variation
hemorrhage
Humans
hypertension
hypertrophy
myocytes
pathophysiology
Pharmacology
Physiology
rats
smooth muscle
spinal cord
TRPM Cation Channels - administration & dosage
TRPM Cation Channels - antagonists & inhibitors
TRPM Cation Channels - genetics
TRPM Cation Channels - metabolism
TRPM4
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Summary:The transient receptor potential channel (TRP) family comprises at least 28 genes in the human genome. These channels are widely expressed in many different tissues, including those of the cardiovascular system. The transient receptor potential channel melastatin 4 (TRPM4) is a Ca2+-activated non-specific cationic channel, which is impermeable to Ca2+. TRPM4 is expressed in many cells of the cardiovascular system, such as cardiac cells of the conduction pathway and arterial and venous smooth muscle cells. This review article summarizes the recently described roles of TRPM4 in normal physiology and in various disease states. Genetic variants in the human gene TRPM4 have been linked to several cardiac conduction disorders. TRPM4 has also been proposed to play a crucial role in secondary hemorrhage following spinal cord injuries. Spontaneously hypertensive rats with cardiac hypertrophy were shown to over-express the cardiac TRPM4 channel. Recent studies suggest that TRPM4 plays an important role in cardiovascular physiology and disease, even if most of the molecular and cellular mechanisms have yet to be elucidated. We conclude this review article with a brief overview of the compounds that have been shown to either inhibit or activate TRPM4 under experimental conditions. Based on recent findings, the TRPM4 channel can be proposed as a future target for the pharmacological treatment of cardiovascular disorders, such as hypertension and cardiac arrhythmias.
ISSN:0006-2952
1873-2968
DOI:10.1016/j.bcp.2012.06.021