Endothelin GPCR Family Subtypes and Products

What Are Endothelin Receptors?

Endothelin receptors are a family of G protein-coupled receptors (GPCRs) comprised of two receptor types: ETA and ETB. These receptors are mainly located in blood vessels, and the activation of these receptors plays a key role in mediating vasodilation and vasoconstriction. While no ETA agonist has been found, both ET-1 and sarafotoxin S6c are selective ETB agonists. Selective ETA and ETB antagonists are used in the treatment of pulmonary arterial hypertension. There has also been development in the utility of endothelin receptor antagonists as an anti-cancer drug.

Endothelin Receptor Information

Clickable Text Interaction



Endothelin is a hormone produced predominantly by endothelial cells that have been recognized to play a significant role in the development of several cardiovascular disease states. Its receptor ETA has been reported in a variety of tissues including placenta, uterus, testis, heart, adrenal gland, lung, kidney, ovary, skin, liver, bladder, large blood vessels, cerebellum, neurons, and meningioma tumor cells. In the vasculature, ETA receptors residing on smooth muscle cells mediate prolonged vasoconstriction. Furthermore, activation of the ETA mediates events that regulate mitogenesis, apoptosis, angiogenesis and metastasis in tumors.

ETB is mainly expressed in vascular endothelial and and epithelial tissues as well as by smooth muscle cells. ETB activation of smooth muscle cells results in vasoconstriction, whereas ETB activation on vascular endothelium causes vasodilation through the release of nitric oxide. ETB has also been found to lower blood pressure through natriuresis and diuresis, and to release prostaglandins. In the kidney, ETB also serves to clear endothelins from circulation by receptor-mediated endocytosis and subsequent lysosomal degradation. Mutations in the ETB gene have been linked to Waardenburg syndrome, as well as Hirschsprung disease type 2.

Endothelin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes