Target intelligence / Profile preview

Vasopressin Receptor Type 2 (V2R)

Target
V2R
Molecular classification
G protein-coupled receptor, GPCR, Class A GPCR, Rhodopsin-like GPCR
01

Overview

The Vasopressin Receptor Type 2 (V2R), also known as AVPR2, is a G protein-coupled receptor primarily expressed in the kidney's distal convoluted tubule and collecting ducts. It plays a crucial role in water homeostasis by mediating the effects of arginine vasopressin (AVP) on water reabsorption. Activation of V2R leads to increased cAMP production and the translocation of aquaporin-2 channels to the apical membrane, enhancing water permeability. Dysfunction of V2R is associated with nephrogenic diabetes insipidus and SIADH. Clinically, it is targeted by agonists like desmopressin and antagonists like tolvaptan to manage water balance disorders and bleeding disorders.

Other names
AVPR2
02

Mechanism of action

The V2 receptor is a G protein-coupled receptor that primarily couples to Gs, stimulating adenylate cyclase and increasing cAMP levels upon activation by vasopressin. This leads to PKA activation and aquaporin-2 translocation to the apical membrane of collecting duct cells, increasing water reabsorption. Antagonists block vasopressin binding, inhibiting this process.

03

Biological functions

Water homeostasisRegulation of aquaporin-2 traffickingRegulation of aquaporin-2 expressionRelease of von Willebrand factorRelease of factor VIIISignal transductioncAMP production
04

Disease associations

Nephrogenic Diabetes InsipidusSyndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH)Congestive Heart Failure (CHF)CirrhosisHyponatremiaHemophilia Avon Willebrand disease
05

Safety considerations

Hyponatremia (with agonists)Overcorrection of hyponatremia (with antagonists)
06

Interacting drugs

Arginine vasopressin (AVP)

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