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


 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.

Author Biographies

Anitha Nandagopal, Department of Pharmacology, Sultan-Ul-Uloom College of Pharmacy, Hyderabad - 500 034, Telangana, India.
Dept. of Pharmacology, Professor.
Mubeen Unnisa Shamsia, Department of Pharmacology, Sultan-Ul-Uloom College of Pharmacy, Hyderabad - 500 034, Telangana, India.
Dept. of Pharmacology, M.Pharm 2nd year Student


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How to Cite
Nandagopal, A., and M. U. Shamsia. “A REVIEW ON ENDOTHELINS: AN UPDATE”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 11, no. 4, Apr. 2018, pp. 38-42, doi:10.22159/ajpcr.2018.v11i4.23255.
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