Endothelin-1
Also known as: Big endothelin-1 (precursor), EDN1, Endothelin‑1, ET-1, Preproendothelin-1 (mature form), Vasoconstrictin
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Summary
Endothelin‑1 (ET‑1) is a 21‑amino‑acid peptide produced by endothelial cells; it is the most potent endogenous vasoconstrictor and contributes to cardiovascular homeostasis and disease.
Mechanism of Action
Binds endothelin receptor type A (ETA) and type B (ETB) on vascular smooth muscle cells, activating Gq protein signaling that leads to potent vasoconstriction and cellular proliferation.
Routes of Administration
Goals & Uses
- Research tool for vasoconstriction studiesResearchHigh
- Model of renal vasoconstriction and injuryResearchModerate
- Pharmacological target for PAH treatmentTherapeutic TargetHigh
- Cancer biology research (tumor angiogenesis)ResearchModerate
- Biomarker for pulmonary arterial hypertensionDiagnostics / BiomarkerHigh
Contraindications
- Systemic administration in humans outside controlled researchGeneralHigh
- Coronary artery diseaseCardiovascularHigh
- Renal impairmentOrgan DysfunctionHigh
- Pre-existing severe hypertensionCardiovascularHigh
Adverse Effects
- Pulmonary vasoconstrictionPulmonaryCommon
- Nausea and flushingGeneralCommon
- Myocardial ischemia / coronary vasospasmCardiovascularUncommon
- BronchoconstrictionRespiratoryUncommon
- Severe vasoconstriction / hypertensionCardiovascularCommon
- Renal vasoconstriction and reduced GFRRenalCommon
Drug Interactions
- Endothelin receptor antagonists (bosentan, ambrisentan, macitentan)High
- Vasopressors (e.g., norepinephrine, vasopressin)High
- Nitric oxide donors / nitratesModerate
- ACE inhibitorsLow
Population Constraints
- Patients with heart failureCardiovascularAbsolute
- Patients with chronic kidney diseaseRenalRelative
- Pregnant womenReproductiveAbsolute
- Neonates and pediatric populationsPediatricAbsolute
Regulatory Status
- European UnionUnapprovedNot approved by EMA as a therapeutic agent. Used only in controlled research settings.
- United StatesUnapprovedNot an approved therapeutic; classified as a research peptide. Endothelin pathway antagonists (not ET-1 itself) are FDA-approved for PAH.
- United KingdomUnapprovedNot approved by MHRA as a medicine. Used as a research tool only.
Endothelin‑1 is an endogenous peptide and is not approved as a pharmaceutical product.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Endothelin-1?
Endothelin‑1 (ET‑1) is a 21‑amino‑acid peptide produced by endothelial cells; it is the most potent endogenous vasoconstrictor and contributes to cardiovascular homeostasis and disease.
What is Endothelin-1 used for?
Endothelin-1 is educationally associated with: Research tool for vasoconstriction studies, Model of renal vasoconstriction and injury, Pharmacological target for PAH treatment, Cancer biology research (tumor angiogenesis), Biomarker for pulmonary arterial hypertension. Educational only — not medical advice.
How is Endothelin-1 administered?
Recorded routes of administration: Intracoronary, Intrathecal, Intravenous.
What are the potential side effects of Endothelin-1?
Reported adverse effects include: Pulmonary vasoconstriction, Nausea and flushing, Myocardial ischemia / coronary vasospasm, Bronchoconstriction, Severe vasoconstriction / hypertension, Renal vasoconstriction and reduced GFR. This list is not exhaustive — consult a qualified clinician.
Who should avoid Endothelin-1?
Recorded contraindications: Systemic administration in humans outside controlled research, Coronary artery disease, Renal impairment, Pre-existing severe hypertension. Consult a qualified clinician before use.