Pharmacological potential of endothelin receptors agonists and antagonists.
Endothelins are potent predominantly vasoconstricting agents that act as local autocrine and paracrine mediators. Endothelin-1 is the most potent and sustained vasoconstrictor and pressor substance yet identified. Abnormalities of the endothelin system occur in a range of diseases associated with vasoconstriction, vasospasm, and vascular hypertrophy. ET receptor antagonists were until recently regarded as drugs of great promise in patients with congestive heart failure, pulmonary hypertension and others. The aim of this article is a survey of compounds that affect the endothelin receptors and clinical trials with these agents.
Patocka
Jirí
J
Department of Toxicology, University of Defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Czech Republic. patocka@pmfhk.cz
Merka
Vladimír
V
Hrdina
Vratislav
V
Hrdina
Radomír
R
D002318:Cardiovascular Diseases / Q000503:physiopathology*; D065128:Endothelin Receptor Antagonists; D017466:Receptors, Endothelin / Q000819:agonists / Q000502:physiology*; D014661:Vasoconstriction / Q000502:physiology
D065128:Endothelin Receptor Antagonists; D017466:Receptors, Endothelin