Endothelin receptor Endothelin Endothelin:Endothelin receptor Endothelin receptors bind endothelin Authored: Jassal, B, 2008-12-12 14:37:44 Edited: Jassal, B, 2008-12-12 14:37:44 Endothelins are 21-amino acid vasoconstricting peptides produced primarily in the endothelium that play a key role in vascular homeostasis. An imbalance and over-expression of endothelins can contribute to hypertension (high blood pressure). Endothelins are implicated in vascular diseases of several organ systems, including the heart, general circulation and brain. There are 3 isoforms designated ET1, ET2 and ET3 (Inoue A et al, 1989).<br><br>These bind to two receptors, designated ETA (Adachi M et al, 1991) and ETB (Nakamuta M et al, 1991). ETA receptors are primarily located in smooth muscle of blood vessels. Endothelin binding to ETA causes vasoconstriction and sodium retention, leading to increased blood pressure. ETB are primarily located on endothelial cells lining the internal walls of vasculature. Endothelin binding to ETB leads to the release of NO (nitric oxide) which is a strong vasodilator. Pubmed1710450 Pubmed1719979 Pubmed2649896 Pubmed8440682 Reactome Database ID Release 43388560 Reactome, http://www.reactome.org ReactomeREACT_17040 Reviewed: D'Eustachio, P, 2009-03-02 09:24:35