A REVIEW ON ENDOTHELINS: AN UPDATE


Anitha Nandagopal, Mubeen Unnisa Shamsia

Abstract


 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.


Keywords


Endothelin, Vasoconstriction, Endothelin receptors, Endothelin agonists, Antagonists.

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About this article

Title

A REVIEW ON ENDOTHELINS: AN UPDATE

Topics

Pharmacology

Keywords

Endothelin, Vasoconstriction, Endothelin receptors, Endothelin agonists, Antagonists.

DOI

10.22159/ajpcr.2018.v11i4.23255

Date

01-04-2018

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 11 Issue 4 April 2018 Page: 38-42

Print ISSN

0974-2441

Online ISSN

2455-3891

Authors & Affiliations

Anitha Nandagopal
Department of Pharmacology, Sultan-Ul-Uloom College of Pharmacy, Hyderabad - 500 034, Telangana, India.
India

Mubeen Unnisa Shamsia
Department of Pharmacology, Sultan-Ul-Uloom College of Pharmacy, Hyderabad - 500 034, Telangana, India.
India


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