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The TRPM 4 channel inhibitor 9‐phenanthrol
Author(s) -
Guinamard R,
Hof T,
Del Negro C A
Publication year - 2014
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12582
Subject(s) - transient receptor potential channel , medicine , pharmacology , ion channel , biophysics , chemistry , receptor , biology
The phenanthrene‐derivative 9‐phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin ( TRPM ) 4 channel, a Ca 2+ ‐activated non‐selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity of the drug for TRPM 4. In addition, 9‐phenanthrol modulates a variety of physiological processes through TRPM 4 current inhibition and thus exerts beneficial effects in several pathological conditions. 9‐Phenanthrol modulates smooth muscle contraction in bladder and cerebral arteries, affects spontaneous activity in neurons and in the heart, and reduces lipopolysaccharide‐induced cell death. Among promising potential applications, 9‐phenanthrol exerts cardioprotective effects against ischaemia‐reperfusion injuries and reduces ischaemic stroke injuries. In addition to reviewing the biophysical effects of 9‐phenanthrol, here we present information about its appropriate use in physiological studies and possible clinical applications.