Cardiovascular & General; Cardiovascular & Metabolic
Endothelin-1

Endothelin-1 is 21 amino acids long, released by the single layer of cells lining a blood vessel, and it is the most powerful and longest-acting constrictor the body makes: the vessel wall's own instruction to clamp down, issued to itself. Everything clinical about it runs in the opposite direction from supply. Levels climb in pulmonary hypertension, ischaemic heart disease and pre-eclampsia, so it serves as a warning sign, and the direction of interest has always been in restraining it rather than providing it. Nearly every human study on file is a measurement in patients or a brief research infusion in volunteers, and nothing on file records it being given to treat a condition.
Last updated
Mechanism
Activates ETA receptors on vascular smooth muscle for sustained vasoconstriction, and ETB receptors mediating clearance and nitric-oxide release.
Reported effects
What sources associate with this compound. Reported categories, not outcomes we have graded — each would need its own citation and rung.
- Vascular tone research
- Pulmonary hypertension context
- Cardiovascular marker research
Dosing on file unverified
Research: 0.4-5.0 pmol/kg/min; 0.2-8 pmol/kg/min; 1.0-2.5 ng/kg/min × 7h; Bolus: 0.001-7.5 µg/kg
Carried from a source that labels it unverified, and reproduced with that label attached. A record of what is reported, not a recommendation. No citation on this page establishes it.
Literature on file 11
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human observational
Endothelin-1/Endothelin-3 Ratio (2007, cited 54x) graded on: an observational human design — read from the indexed abstract — “cohort”
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review or editorial
Plasma homocysteine and Endothelin-1 dysregulation: Insights into retinal endothelial dysfunction. graded on: indexed as "Review" - secondary literature, not a study — “Review”
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in vitro
Endothelin-1 Signaling Mediates Hypoxia-Induced Microglial Activation Through Reactive Oxygen Species and Mitogen-Activated Protein Kinase Pathways. graded on: HMC3 human microglial cells under 1% oxygen — read from the abstract — “abstract review”
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animal in vivo
Endothelin-1 overexpression in mice increases vascular Vegfa164 and Vegfa188 alternative splice isoforms via enhanced Khdrbs3 expression. graded on: an animal model — “mice”
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human observational
Expression profile of apolipoproteins (APOE) and endothelin-1 (ET-1) genes in ischemic heart disease. graded on: case-control gene expression, 100 patients vs 100 controls — read from the abstract — “abstract review”
- animal in vivo
Not graded
5 citations whose study design could not be read from the title. Left ungraded rather than guessed at.
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not graded
NCT00406731: Role of endothelin-and Nitric Oxide-system in the Regulation of Optic Nerve Head Blood Flow During Changes in Ocular Perfusion Pressure graded on: NCT00406731 is withdrawn and has posted no results - a registration, not a reported outcome — “NCT00406731”
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not graded
NCT05653973: Protective Mechanisms of Prenatal Aspirin Therapy on Maternal Vascular Dysfunction Following Preeclampsia graded on: NCT05653973 is recruiting and has posted no results - a registration, not a reported outcome — “NCT05653973”
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not graded
NCT00745693: The Effects of Diesel Exhaust Inhalation on Vascular Function - the Role of Endothelin graded on: NCT00745693 is completed and has posted no results - a registration, not a reported outcome — “NCT00745693”
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not graded
NCT02906085: Investigations of the Endogenous Vasoconstrictor and Neuromodulator Peptide Endothelin-1 as a Potential Trigger of Migraine Aura graded on: NCT02906085 is unknown and has posted no results - a registration, not a reported outcome — “NCT02906085”
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not graded
NCT05703126: Clinical and Diagnostic Significance of Endothelial Dysfunction and Myocardial Contractility in Patients With Acute Myeloid Leukemia graded on: NCT05703126 is recruiting and has posted no results - a registration, not a reported outcome — “NCT05703126”
Identity
Skeletal formulathe canonical depiction
Drawn by PubChem from CID 16212950, the identifier on this record.
- Molecular weight
- 2491.9
- Molecular formula
- C109H159N25O32S5
- CAS number
- 117399-94-7
- PubChem CID
- 16212950
- UniProt
- P05305 (precursor)
- InChI key
- ZUBDGKVDJUIMQQ-ZTNLKOGPSA-N
- SMILES
- CC[C@H](C)[C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC3=CN=CN3)NC(=O)[C@@H]4CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H]5CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N4)CC6=CC=CC=C6)CC7=CC=C(C=C7)O)C(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC5=O)CO)CO)CC(C)C)CCSC)CC(=O)O)CCCCN)CCC(=O)O)CO)N
- InChI
- InChI=1S/C109H159N25O32S5/c1-12-56(9)87(107(163)125-76(109(165)166)39-60-43-113-65-24-18-17-23-63(60)65)134-108(164)88(57(10)13-2)133-99(155)75(42-85(143)144)123-94(150)70(36-54(5)6)118-97(153)73(40-61-44-112-52-114-61)121-103(159)80-49-169-168-48-64(111)89(145)126-77(45-135)102(158)131-81-50-170-171-51-82(105(161)132-86(55(7)8)106(162)124-72(38-59-26-28-62(138)29-27-59)95(151)120-71(96(152)130-80)37-58-21-15-14-16-22-58)129-91(147)67(30-31-83(139)140)116-90(146)66(25-19-20-33-110)115-98(154)74(41-84(141)142)122-92(148)68(32-34-167-11)117-93(149)69(35-53(3)4)119-100(156)78(46-136)127-101(157)79(47-137)128-104(81)160/h14-18,21-24,26-29,43-44,52-57,64,66-82,86-88,113,135-138H,12-13,19-20,25,30-42,45-51,110-111H2,1-11H3,(H,112,114)(H,115,154)(H,116,146)(H,117,149)(H,118,153)(H,119,156)(H,120,151)(H,121,159)(H,122,148)(H,123,150)(H,124,162)(H,125,163)(H,126,145)(H,127,157)(H,128,160)(H,129,147)(H,130,152)(H,131,158)(H,132,161)(H,133,155)(H,134,164)(H,139,140)(H,141,142)(H,143,144)(H,165,166)/t56-,57-,64-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,86-,87-,88-/m0/s1
Notes unverified prose
Human research studies only; Human research IV infusions
Not on file 2
1 of the 8 fields we track hold nothing on this record, and each says why. 1 further absence is named below. A blank field is a bug; a named absence is a finding.
- amino-acid sequencenothing we hold supplies it
- half-lifenothing we hold supplies it
Each field links to every other record missing the same thing. The full ledger holds 765 gaps across 163 records.