Cardiovascular & General; Sleep, Mood & Stress / Cardiovascular

Urotensin II

Urotensin II is a small ring-shaped peptide and the most potent constrictor of blood vessels identified in any mammal. It arrived in human pharmacology in 1999 by way of an orphan: a receptor called GPR14 that had no known partner, matched to this peptide and then renamed after it. That potency is precisely why nobody is developing urotensin II as a treatment — the clinical effort has gone entirely into drugs designed to block it, and the human studies on file measure its levels in liver cirrhosis, kidney disease and heart disease rather than administering it. It is a research peptide and a drug target, not a therapy, and no approved product contains it.

Last updated 12 August 2026

Studied forVascular tone research · Cardiovascular disease markers · Receptor pharmacology

Evidence on file5 animal studies · 1 in-vitro study · 2 citations not yet graded

Strongest sourceHuman urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14 (Nature 1999, cited… (animal study)

Mechanism

Agonist at the UT receptor (formerly orphan GPR14) on vascular smooth muscle, producing sustained vasoconstriction.

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
Cardiovascular disease markers
Receptor pharmacology

Dosing on file unverified

No established human therapeutic dose; research infusions only

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 8

animal in vivo
Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14 (Nature 1999, cited 671x) graded on: an animal model — read from the indexed abstract — “rats”
animal in vivo
Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord (Proceedings of the National Academy of Sciences 1998, cited 339x) graded on: an animal model — “frog”
in vitro
In-vitro effects of the urotensin-II peptide and its receptor antagonists on mcf-7 breast cancer cell line. graded on: an in-vitro system — “cell line”
animal in vivo
Capsanthin Attenuates Osteoporosis by Targeting the Urotensin II Receptor Pathway to Inhibit Oxidative Stress and NLRP3 Inflammasome Activation. graded on: an animal model — read from the indexed abstract — “mice”
animal in vivo
EFFECTS OF THE UROTENSIN-II RECEPTOR ANTAGONIST SB-710411 ON REMOTE ISCHEMIC PRECONDITIONING IN A RAT MODEL OF LPS-INDUCED ENDOTOXIC SHOCK: CARDIOVASCULAR RESPONSE, INFLAMMATORY INJURY, AND SURVIVAL. graded on: an animal model — “RAT”
animal in vivo
Involvement of gap junction, calcium and potassium channels in Urotensin II reactivity in diabetic rat isolated aorta. graded on: an animal model — “rat”

Not graded

2 citations whose study design could not be read from the title. Left ungraded rather than guessed at.

not graded
Conflicting Roles of Urotensin II in Chronic Kidney Disease: Insights from Clinical and Mechanistic Studies.
not graded
NCT00163995: Urotensin II and Vascular Tone in Cirrhosis graded on: NCT00163995 is unknown and has posted no results - a registration, not a reported outcome — “NCT00163995”

Identity

Space-filling 3D model of Urotensin II, carbon grey, nitrogen blue, oxygen red — Built from the SMILES on this record — the atoms and bonds are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation, and where the SMILES leaves a stereocentre undefined the pose commits to one arbitrarily. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

2D chemical structure of Urotensin II — Built from the SMILES on this record — the atoms and bonds are exact. The shape is **one computed low-energy pose**, not a measured structure: a flexible peptide in solution has no single conformation, and where the SMILES leaves a stereocentre undefined the pose commits to one arbitrarily. The skeletal formula below claims connectivity and nothing more, which is what we actually know.

Molecular weight: 1388.6
Molecular formula: C64H85N13O18S2
CAS number: 9047-55-6
PubChem CID: 46225600
InChI key: HFNHAPQMXICKCF-USJMABIRSA-N
SMILES: C[C@H]([C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC2=O)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)CC6=CC=C(C=C6)O)C(=O)N[C@@H](C(C)C)C(=O)O)NC(=O)[C@H](CCC(=O)O)N)O
InChI: InChI=1S/C64H85N13O18S2/c1-33(2)52(64(94)95)75-61(91)48-32-97-96-31-47(73-59(89)46(29-51(82)83)72-62(92)49-17-11-25-77(49)63(93)53(34(3)78)76-54(84)40(66)22-23-50(80)81)60(90)70-43(26-35-12-5-4-6-13-35)56(86)71-45(28-37-30-67-41-15-8-7-14-39(37)41)58(88)68-42(16-9-10-24-65)55(85)69-44(57(87)74-48)27-36-18-20-38(79)21-19-36/h4-8,12-15,18-21,30,33-34,40,42-49,52-53,67,78-79H,9-11,16-17,22-29,31-32,65-66H2,1-3H3,(H,68,88)(H,69,85)(H,70,90)(H,71,86)(H,72,92)(H,73,89)(H,74,87)(H,75,91)(H,76,84)(H,80,81)(H,82,83)(H,94,95)/t34-,40+,42+,43+,44+,45+,46+,47+,48+,49+,52+,53+/m1/s1

Notes unverified prose

No FDA approval; preclinical only; no human therapeutic dosing; Phase 1 trials (antagonist); no approved therapeutic; preclinical

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.