nounIntermediate
Definition
Family of 21-amino-acid vasoconstrictor peptides (ET-1, ET-2, ET-3) produced primarily by endothelial cells; ET-1 is the most potent vasoconstrictor identified in the human body.
Detailed Explanation
Endothelin-1 was discovered in 1988 by Masashi Yanagisawa and is approximately 100× more potent than norepinephrine as a vasoconstrictor. It acts through ETA and ETB receptors on vascular smooth muscle. Under normal conditions, endothelin is balanced by the vasodilator nitric oxide. In disease states — pulmonary arterial hypertension, chronic kidney disease, heart failure — endothelin is overproduced. Endothelin receptor antagonists (bosentan, ambrisentan, macitentan) are the standard treatment for pulmonary arterial hypertension, directly blocking ET-1's vasoconstrictive effects on pulmonary vessels.
Key Facts
- Endothelin-1 was discovered in 1988 by Masashi Yanagisawa and is approximately 100× more potent than norepinephrine as a vasoconstrictor
- It acts through ETA and ETB receptors on vascular smooth muscle
- Under normal conditions, endothelin is balanced by the vasodilator nitric oxide
- In disease states — pulmonary arterial hypertension, chronic kidney disease, heart failure — endothelin is overproduced
- Endothelin receptor antagonists (bosentan, ambrisentan, macitentan) are the standard treatment for pulmonary arterial hypertension, directly blocking ET-1's vasoconstrictive effects on pulmonary vessels
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