Pharmacological Potential of Endothelin Receptors Agonists and Antagonists

Patočka, Jiří; Měrka, Vladimír; Hrdina, Vratislav; Hrdina, Radomír

doi:10.14712/18059694.2018.34

Acta Medica > Archive > 2005, Vol. 48 > Issue 2 > Pharmacological Potential of Endothelin…

Acta Med. 2005, 48: 67-73

https://doi.org/10.14712/18059694.2018.34

Pharmacological Potential of Endothelin Receptors Agonists and Antagonists

Jiří Patočka^a,b, Vladimír Měrka^a, Vratislav Hrdina, Radomír Hrdina^c

^aUniversity of Defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Department of Toxicology, Hradec Králové, Czech Republic
^bUniversity of South Bohemia, České Budějovice, Faculty of Health and Social Studies, Department of Radiology and Toxicology, České Budějovice, Czech Republic
^cCharles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmacology and Toxicology, Hradec Králové, Czech Republic

Received September 1, 2004
Accepted November 1, 2004

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.