Endothelin receptors

The endothelin family in mammals consists of three endogenous isoforms, ET-1, ET-2 and ET-3, which are highly potent vasoactive peptides.  There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, which are widely expressed in all tissues, consistent with the physiological role of endothelins as ubiquitous endothelium derived vasoactive peptides.  Endothelin receptors are widely distributed in the body, being present in blood vessels and cells of the brain, choroid plexus and peripheral nerves.   Under normal conditions, endothelins contribute to the maintenance of vascular tone but under pathophysiological conditions they can contribute to vascular remodeling, proliferation of mesangial cells, and extracellular matrix production and have been linked to cardiac, vascular and renal diseases.

Further reading

Khodorova et al (2009) Endothelin Receptors and Pain. J. Pain 10(1) 4 PMID: 19111868

Maguire and Davenport (2015) Endothelin receptors and their antagonists. Semin. Nephrol. 35(2) 125 PMID: 25966344

Davenport et al (2019). Endothelin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology 2019(4). Available from: https://doi.org/10.2218/gtopdb/F21/2019.4.

Smeijer et al (2024) Endothelin receptor antagonists in chronic kidney disease. Nat Rev Nephrol. Dec 6 Epub ahead of print. PMID: 39643698