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


CONCLUSIONS
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.
Giachini
Fernanda R C
FR
Medical College of Georgia, Department of Physiology, 1120 Fifteenth Street, CA-3141 Augusta, Georgia 30912-3000, USA. fgiachini@mcg.edu
Callera
Glaucia E
GE
Carneiro
Fernando S
FS
Tostes
Rita C
RC
Webb
R Clinton
RC
D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage*; D016503:Drug Delivery Systems / Q000379:methods*; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1 / Q000037:antagonists & inhibitors / Q000502:physiology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D017466:Receptors, Endothelin / Q000502:physiology; D014579:Urotensins / Q000037:antagonists & inhibitors / Q000502:physiology; D014661:Vasoconstriction / Q000187:drug effects* / Q000502:physiology; D014662:Vasoconstrictor Agents / Q000037:antagonists & inhibitors* / Q000494:pharmacology
D000959:Antihypertensive Agents; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1; D017466:Receptors, Endothelin; D014579:Urotensins; D014662:Vasoconstrictor Agents; C029677:urotensin II