A REVIEW ON ENDOTHELINS: AN UPDATE
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i4.23255Keywords:
Endothelin, Vasoconstriction, Endothelin receptors, Endothelin agonists, AntagonistsAbstract
 Endothelin (ET) is the most potent vasoconstrictor. It is secreted by the endothelial cells. At low concentration, it acts as an agonist for endothelium-derived relaxing factors and thereby causes vasodilatation, and at higher concentration it acts as a potent vasoconstrictor. It is synthesized by proteolytic cleavage of preproendothelin to proendothelin by the action of metallopeptidases and chymase, which is further cleaved into mature form of ET by endothelin converting enzyme. There are four isoforms of ET, namely, ET-1, ET-2, ET-3, and ET-4. ET acts on 2 types of receptors. Binding of ET-1 to ETA receptor at the vascular smooth muscle cells induces vasoconstriction. It also produces vasoconstriction by acting on the ETB2 receptor of vascular smooth muscle cells but promotes vasodilatation at ETB1 receptor present on the endothelial cell.
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