What is the Origin of Endothelin?

The name is a composite derived from the site of its primary production, the "endothelium," and the suffix "-in," commonly used to denote a protein or peptide. Endothelin was first identified and isolated in the late 1980s, fundamentally changing the understanding of endothelial cell function beyond a simple barrier.

What is the Mechanism of Endothelin?

Endothelin-1 exerts its constrictive effects by binding to the Endothelin A (ETA) and Endothelin B (ETB) receptors, which are G protein-coupled receptors located on the vascular smooth muscle cells. Activation of the ETA receptor is the principal mediator of vasoconstriction, leading to increased peripheral resistance. The ETB receptor also mediates constriction but additionally plays a crucial role in clearing circulating Endothelin-1 and promoting local vasodilation via nitric oxide release.

Endothelin ∞ Area

Endothelin

Meaning

Endothelin is a potent, small peptide synthesized predominantly by the endothelial cells lining the interior surface of blood vessels. Its primary biological function is a powerful and sustained vasoconstriction, making it a critical regulator of vascular tone and systemic blood pressure. Endothelin-1 (ET-1) is the most studied isoform, and its dysregulation is a significant contributor to conditions like hypertension and pulmonary arterial hypertension.

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