Endothelin is a peptide produced by the endothelium using an endothelin converting enzyme (ECE) on the endothelial membrane. A representative of endothelins is endothelin-1. Endothelin release is stimulated by angiotensin II, ADH, thrombin, cytokines and oxygen radicals. Endothelin-1 acts as a vasoconstrictor, promotes fibrotization, cell proliferation, cardiac hypertrophy or remodeling, and has pro-inflammatory effects. By blocking its receptors (ETA or ETB) these effects are minimized. Inhibitors of these receptors are called sentanes and are used in pulmonary hypertension therapy.
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SLÍVA, Jiří, et al. Farmakologie. 1.. vydání. Praha : Nakladatelství TRITON, 2010. 238 s. s. 53. ISBN 978-80-7387-424-7.