Target intelligence / Profile preview

Vasopressin 2 Receptor (V2R)

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

Overview

The vasopressin 2 receptor (V2R), also known as arginine vasopressin receptor 2 or AVPR2, is a G protein-coupled receptor that primarily acts as a receptor for the hormone arginine vasopressin (AVP), also called antidiuretic hormone (ADH). V2R is primarily located in the basolateral membrane of principal cells lining the distal tubule, connecting tubule, and collecting ducts of the kidney, where it regulates body water homeostasis by controlling water reabsorption from urine via aquaporin 2 channels. Mutations in V2R cause Nephrogenic Diabetes Insipidus. V2R antagonists are used to treat hyponatremia.

Other names
AVPR2Arginine Vasopressin Receptor 2
02

Mechanism of action

V2R agonists stimulate cAMP production and PKA activation, leading to increased aquaporin 2 expression and water reabsorption in the kidneys. V2R antagonists block this signaling pathway, promoting water excretion.

03

Biological functions

Water reabsorptionRegulation of body water homeostasisSignal transductionRelease of von Willebrand factorRelease of factor VIIIRegulation of membranous fluid turnover in inner earModulation of mitogenesis/apoptosis
04

Disease associations

Nephrogenic Diabetes InsipidusHyponatremiaHemophilia AVon Willebrand DiseaseTumor development
05

Safety considerations

Hyponatremia risk with V2R antagonists if not carefully monitored
06

Interacting drugs

Arginine vasopressin (AVP)

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