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[Endothelins in chronic cardiac insufficiency]
1Service de cardiologie, groupe hospitalier Pitié-Salpêtrière, Paris.
Summary
Endothelin-1 (ET-1) is a peptide involved in vascular tone and cardiac function. Inhibiting ET-1 action may benefit cardiac failure patients by improving hemodynamics and ventricular remodeling.
Area of Science:
- Cardiovascular Physiology
- Molecular Biology
- Pharmacology
Context:
- Endothelins (ETs) are peptides regulating vascular tone.
- Endothelin-1 (ET-1) is a potent vasoconstrictor with roles in cardiac function.
- The ET system is implicated in the pathophysiology of cardiac failure.
Purpose:
- To review the role of the endothelin system in cardiac failure.
- To explore therapeutic strategies targeting ET-1 inhibition.
- To discuss the potential benefits of ET receptor blockade in cardiac failure.
Summary:
- ET-1, produced by endothelin-converting enzyme, acts on ETA and ETB receptors.
- Elevated ET-1, increased converting enzyme, and receptor density are observed in cardiac failure.
- ET-1 inhibition, via synthesis blockade or receptor antagonism, is a potential therapeutic approach.
Impact:
- ET receptor blockade shows promise for beneficial hemodynamic changes and ventricular remodeling in cardiac failure.
- Development of selective ETA or mixed ETA/ETB receptor blockers is ongoing.
- Large-scale clinical trials are necessary to confirm the efficacy of ET-targeted therapies.