Therapeutic targets in hypertension: Is there a place for antagonists of the most potent vasoconstrictors?

Fernanda R.C. Giachini, Glaucia E. Callera, Fernando S. Carneiro, Rita C. Tostes, R. Clinton Webb

Research output: Contribution to journalReview articlepeer-review

15 Scopus citations


Background: Endothelin-1 (ET-1) and urotensin II (U-II) are the most potent and unusually long-lasting constrictors of human vessels known to date. Objective: In this review, we focus on the vascular effects of endothelin-1 (ET-1) and urotensin II (U-II) and their role in the pathophysiology of hypertension. Results and conclusion: Unlike ET-1, which uniformly constricts most blood vessels, the vasoactive effects of U-II depend both on the species, vascular bed and vessel calibre. Both ET-1 and U-II have potent mitogenic, pro-inflammatory and pro-oxidative properties, which have been implicated in the pathogenesis of human cardiovascular and renal diseases. The availability of highly effective peptide and non-peptide antagonists both for ET-1 and U-II receptors has revealed a role for these potent vasoconstrictor peptides in human (patho)physiology.

Original languageEnglish (US)
Pages (from-to)327-339
Number of pages13
JournalExpert Opinion on Therapeutic Targets
Issue number3
StatePublished - Mar 1 2008
Externally publishedYes


  • Endothelial cells
  • Endothelin-1
  • Hypertension
  • Urotensin II
  • Vascular smooth muscle cells

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry


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