Target intelligence / Profile preview

Endothelin B Receptor (ETB)

Target
ETB
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

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.

Other names
EDNRBABCD5Etb ReceptorETRBWS4AHSCR/HSCR2Endothelin Receptor Type BEtb-svr
02

Mechanism of action

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.

03

Biological functions

Signal transductionRegulation of vascular toneBlood pressure regulationModulation of sodium excretionVasodilation (endothelial cells)Vasoconstriction (vascular smooth muscle cells)
04

Disease associations

Hirschsprung disease type IIWaardenburg syndrome type IV
05

Safety considerations

Potential for vasoconstriction in certain contexts.Impaired neural crest cell migration during development (Hirschsprung disease and Waardenburg syndrome).
06

Interacting drugs

Endothelin peptides: ET‑1

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