Progress in anti-endothelin therapy in the treatment of pulmonary arterial hypertension and heart failure

摘要

Endothelin-1 ( ET-1 ) is not only a potent vasoconstrictor , but causes proliferation of many of the vascular cells involved in vascular remodelling .ETA receptors mediate vasoconstriction and cell proliferation , whereas ETB receptors are important for the clearance of ET-1, endothelial cell survival , the release of nitric oxide and prostacyclin , and the inhibition of endothelin-converting enzyme ( ECE )-1.ET is activated in pulmonary arterial hypertension ( PAH) , heart failure ( HF) and many other cardiovascular diseases .The most efficient way to antagonize the ET-1 system is the use of ET-1 receptor antagonists that can block either ETA-or ETA-and ETB-receptors, or ECE inhibition which blocks the conversion of big ET-1 to ET-1.In this brief review , we will try to summarize the progress of anti-endothelin therapy in the treatment of PAH and HF treatment therapies .