The TRPM4 channel inhibitor 9-phenanthrol

Authors

R. Guinamard
T. Hof
C. A. Del Negro, William & Mary

Document Type

Article

Department/Program

Applied Science

Journal Title

British Journal of Pharmacology

Pub Date

2014

Volume

171

Issue

7

First Page

1600

Abstract

The phenanthrene-derivative 9-phenanthrol is a recently identified inhibitor of the transient receptor potential melastatin (TRPM) 4 channel, a Ca2+-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 TRPM4. In addition, 9-phenanthrol modulates a variety of physiological processes through TRPM4 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.

Recommended Citation

Guinamard, R.; Hof, T.; and Del Negro, C. A., The TRPM4 channel inhibitor 9-phenanthrol (2014). British Journal of Pharmacology, 171(7), 1600-1613.
10.1111/bph.12582

DOI

10.1111/bph.12582