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

Abstract

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.

• Authors: Fernanda R C Giachini, Glaucia E Callera, Fernando S Carneiro, Rita C Tostes, R Clinton Webb
• Journal: Expert opinion on therapeutic targets (Expert Opin Ther Targets) Vol. 12 Issue 3 Pg. 327-39 (Mar 2008) ISSN: 1744-7631 [Electronic] England
• PMID: 18269342 (Publication Type: Journal Article, Review)

Chemical References

• Antihypertensive Agents
• Endothelin Receptor Antagonists
• Endothelin-1
• Receptors, Endothelin
• Urotensins
• Vasoconstrictor Agents
• urotensin II

Topics

• Animals
• Antihypertensive Agents (administration & dosage)
• Drug Delivery Systems (methods)
• Endothelin Receptor Antagonists
• Endothelin-1 (antagonists & inhibitors, physiology)
• Humans
• Hypertension (drug therapy, physiopathology)
• Receptors, Endothelin (physiology)
• Urotensins (antagonists & inhibitors, physiology)
• Vasoconstriction (drug effects, physiology)
• Vasoconstrictor Agents (antagonists & inhibitors, pharmacology)