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Endothelin receptor antagonists block endothelin type A and type B receptors (ETA, ETB) for vasoactive peptides. Endothelin-1 was isolated in 1988 from cultured porcine aortic endothelial cells as a 21-amino-acid vasoconstrictor peptide. Both receptors are G protein-coupled and were cloned in 1990, one selective for endothelin-1 and one binding all endothelin isopeptides alike. ETA receptors on smooth muscle mediate vasoconstriction, whereas endothelial ETB receptors release nitric oxide and clear endothelin from the circulation. Ambrisentan, zibotentan and sitaxsentan sodium are ETA-selective antagonists, whereas bosentan and macitentan block both receptor subtypes. (±)-WS75624B inhibits endothelin-converting enzyme (ECE) and acts one step earlier, on peptide formation.
![[Lys4] Sarafotoxin S6c](https://www.adooq.com/media/catalog/product/cache/16359f9c8ddfa823fcb5503b1e11b7ae/a/6/a60258-lys4-sarafotoxin-s6c.gif)
[Lys4] Sarafotoxin S6c is a potent partial agonist of the endothelin receptor. This sarafotoxin analogue induces contraction in pig coronary artery tissues, demonstrating an EC50 of 1.5 nM. It serves as a valuable tool for research in cardiovascular physiology and the study of endothelin receptor signaling pathways.
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