Endothelin receptor antagonists: a place in the management of essential hypertension?

摘要

The endothelin system is a potent endothelial system that controls vascular tone and regulates regional blood flow [1]. Today, three isoforms of the endothelin peptide have been described (endothelin-1, -2 and -3) but most biological effects of endothelin are mediated by the 21 amino acid endothelin-1. In addition to its vascular properties, endothelin influences cell proliferation and extracellular matrix synthesis and contributes to the homeostasis of water and electrolytes by direct effects on the kidney [1]. Endothelin acts through the activation of two specific G-protein-coupled receptors, i.e. endothelin Type A (ETA) and endothelin Type B (ETB) receptors. Stimulation of vascular ETA receptors induces vasoconstriction, whereas activation of vascular ETB receptors promotes vasodilatation.