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Protein / target

Vasopressin V2 receptor

Encoded byAVPR2P30518Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
9
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Vasopressin receptor

Strongest disease association

Heart Failure

Via encoding gene AVPR2 · Clinical evidence · score 0.58

Therapeutic position

Established drug target

Small molecules

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

G protein-coupled receptor for arginine vasopressin, an antidiuretic that promotes renal water reabsorption.

View complete UniProt function annotation

G protein-coupled receptor for arginine vasopressin, an antidiuretic that promotes renal water reabsorption (PubMed:1534149, PubMed:19440390, PubMed:33664408, PubMed:33742150). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (cAMP) (PubMed:33664408, PubMed:33742150). AVPR2 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity (PubMed:33664408, PubMed:33742150)

Subcellular location

Cell membrane
Domains and Gene Ontology detail (25)

Gene Ontology

  • Cclathrin-coated endocytic vesicle membrane
  • Cendocytic vesicle
  • Cendoplasmic reticulum
  • Cendosome
  • CGolgi apparatus
  • Cmembrane
  • Cperinuclear region of cytoplasm
  • Cplasma membrane
  • Fvasopressin receptor activity
  • Pactivation of adenylate cyclase activity
  • Padenylate cyclase-activating G protein-coupled receptor signaling pathway
  • Padenylate cyclase-modulating G protein-coupled receptor signaling pathway

371 aa · 40 kDa · 2 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Cell proliferation & survivalGOG protein-coupled signallingUniProt · GO
View supporting evidence

Cell proliferation & survival

  • ·negative regulation of cell population proliferation
  • ·positive regulation of cell population proliferation

G protein-coupled signalling

  • ·G protein-coupled receptor for arginine vasopressin, an antidiuretic that promotes renal…
  • ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
  • ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
  • ·G protein-coupled receptor signaling pathway

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

1 medicine · 1 area

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Renal Insufficiency1 medicine

9 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

terlipressin
Narrow target profileApprovedBinding agent

Vasopressin V2 receptor binding agent

Indicated for Renal Insufficiency

Direct interaction with this protein · 1 of 3 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene AVPR2

Gene-level evidence surfaced through the gene AVPR2 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Polycystic Kidney, Autosomal Dominant
0.74Moderately supported

Clinical evidence dominant · Open Targets 0.57

Heart Failure
0.72Moderately supported

Clinical evidence dominant · Open Targets 0.58

View evidence synthesis (2)
Polycystic Kidney, Autosomal DominantModerately supported
0.74
agreement 0.610.87
Clinical80%Animal model14%Literature6%

Open Targets aggregate 0.57 · 3 independent evidence families

Heart FailureModerately supported
0.72
agreement 0.560.87
Clinical97%Literature3%

Open Targets aggregate 0.58 · 2 independent evidence families

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Heart Failure0.58
Polycystic Kidney, Autosomal Dominant0.57

Drug development

13 compounds recorded · 9 approved · 4 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
SATAVAPTANPhase 3
CONIVAPTAN HYDROCHLORIDEApproval
MOZAVAPTANApproval
LYPRESSINApproval
PECAVAPTANPhase 2
TERLIPRESSINApproval
TOLVAPTANApproval
DESMOPRESSIN ACETATEApproval
VASOPRESSINApproval
ARGIPRESSIN TANNATEPhase 3

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (9)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

UNKNOWN · via terlipressin · NCT00863837

ClinicalTrials.gov via the drug-target graph.

What's happening now

5

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Trial status changed2026-07-13

    Effect of Terlipressin for Intraoperative Blood Pressure Management in Kidney Transplantation, A Double-blind Randomized Controlled Trial

    Status changed to Active, not recruiting · ClinicalTrials.gov · via terlipressin

  2. Label change2026-06-10

    Label change: TERLIPRESSIN (NDA022231)

    fda · regulatory · fda · via terlipressin

  3. Safety communication2023-03-23

    Drug Safety Update: Terlipressin: new recommendations to reduce risks of respiratory failure and septic shock in patients with type 1 hepatorenal syndrome

    mhra · safety · mhra · via terlipressin

  4. Label change2023-01-09

    Label change: TERLIPRESSIN (NDA022231)

    fda · regulatory · fda · via terlipressin

  5. Regulatory approval2022-09-14

    Approval: TERLIPRESSIN (NDA022231)

    fda · regulatory · fda · via terlipressin

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.