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The Endothelin B receptor (ETB) is a G protein-coupled receptor that binds all three endothelins (ET-1, ET-2, and ET-3). In endothelial cells, it mediates the release of vasodilators, playing a role in blood pressure regulation and clearance of circulating endothelins. In vascular smooth muscle cells, it can mediate vasoconstriction. Mutations in EDNRB are linked to Hirschsprung disease type II and Waardenburg syndrome type IV. BQ-788 is a selective antagonist used to study ETB function.
Agonist binding activates G proteins, leading to activation of the phosphatidylinositol-calcium second messenger system. In endothelial cells, this promotes release of vasodilators like nitric oxide and prostacyclin. In smooth muscle cells, it can mediate vasoconstriction via increased intracellular calcium.
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