期刊
BRITISH JOURNAL OF PHARMACOLOGY
卷 171, 期 7, 页码 1600-1613出版社
WILEY
DOI: 10.1111/bph.12582
关键词
9-phenanthrol; TRPM4; calcium-activated non-selective cation channel; cardioprotection; NSCCa
资金
- French Ministere de l'Enseignement et de la Recherche
- National Institutes of Health [HL104127]
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.
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