Why is endothelin-1 important in medicine?

ET-1 is the most potent endogenous vasoconstrictor and plays a central role in pulmonary arterial hypertension, heart failure, and chronic kidney disease. Three classes of endothelin receptor antagonists (bosentan, ambrisentan, macitentan) are FDA-approved for PAH. ET-1 also serves as a biomarker for cardiovascular disease severity.

What are endothelin receptor antagonists?

ERAs are drugs that block the effects of ET-1. Bosentan is a dual ETA/ETB antagonist. Ambrisentan is selective for ETA. Macitentan is a dual antagonist with improved tissue penetration. All are used for pulmonary arterial hypertension and carry teratogenic risk (pregnancy category X).

How was endothelin-1 discovered?

ET-1 was isolated from porcine aortic endothelial cell culture supernatant by Yanagisawa et al. and reported in Nature in 1988 (PMID: 2451132). It was identified as a 21-residue peptide with two disulfide bonds and unprecedented vasoconstrictor potency.

What is the recommended dose range for Endothelin-1?

The research dose range is 0.5–5 ng/kg/min in human research protocols, administered via Intravenous infusion (research only), Single-dose or short-duration infusion.

peptide dosing

Endothelin-1 Dosing & Reconstitution Guide

Complete dosing reference for Endothelin-1 (Cardiovascular / Vasoactive). Covers reconstitution, dose range, titration schedule, pharmacokinetics, and storage protocols for research use.

Dosing Protocol

Route: Intravenous infusion (research only) Frequency: Single-dose or short-duration infusion Dose Range: 0.5–5 ng/kg/min in human research protocols

Safety & Contraindications

Safety: ET-1 is not used as an exogenous therapeutic agent Endogenous ET-1 overproduction is implicated in pulmonary hypertension, heart failure, chronic kidney disease, and systemic hypertension Experimental IV ET-1 infusion causes marked vasoconstriction, hypertension, and reduced cardiac output

Contraindications: Not applicable as a therapeutic agent; For endothelin receptor antagonists: pregnancy (teratogenic, category X), significant hepatic impairment (bosentan), concurrent use with cyclosporine (bosentan)

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Endothelin-1 Dosing Guide Peptides for Reference Peptides for Pulmonary Hypertension Research

Research Use Only. The information on this page is compiled from published research literature and is provided for educational purposes only. It does not constitute medical advice. All compounds referenced are intended for in vitro research use by qualified laboratories and institutions.