Tale of 2 Endothelin Receptor Antagonists in Eisenmenger Syndrome复制标题

2内皮素受体拮抗剂在艾森曼格综合征中的作用

Endothelin is a potent vasoactive peptide discovered in 1988 by Yanagisawa et al. The effects of endothelin are mediated by Endothelin A (ETA) and Endothelin B (ETB) receptors. ETA receptors are located on vascular smooth muscle cells and mediate vasoconstriction. ETB receptors are on both endothelial cells and vascular smooth muscle cells. ETB receptors on endothelial cells may lead to the clearance of endothelin and production of nitric oxide, whereas ETB receptors on smooth muscle cells also mediate vasoconstriction. Several targeted therapies have been developed toward the endothelin receptors. In 2001, bosentan, a dual endothelin receptor antagonist, was approved by the US Food and Drug Administration as a treatment for group 1 PAH.

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