Endothelin receptor (ETA and ETB subtypes) (ETA, ETB)

Endothelin receptors (endothelin receptor type A and endothelin receptor type B) are members of the G protein-coupled receptor family that mediate the effects of endothelin-1, one of the most potent endogenous vasoconstrictors. ETA is predominantly found on vascular smooth muscle cells where its activation causes vasoconstriction and cell proliferation, while ETB is present on both endothelial and smooth muscle cells, where it can cause either vasodilation (by releasing nitric oxide and prostacyclin) or vasoconstriction, depending on the subtype and tissue. These receptors are key regulators of vascular tone and tissue remodeling. Overactivation of endothelin signaling is implicated in the pathogenesis of pulmonary arterial hypertension and several cardiovascular and fibrotic diseases. Pharmacological antagonism of these receptors with drugs such as bosentan leads to vasodilation, reduced vascular resistance, and improved outcomes in pulmonary arterial hypertension.

Other names

Endothelin-1 receptorET receptorETA receptorETB receptor

Competitive antagonism of endothelin-1 at ETA and ETB receptors, leading to reduced vasoconstriction and vascular remodeling