Target intelligence / Profile preview

Vasopressin Receptor 1A (V1aR)

Target
V1aR
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

Vasopressin Receptor 1A (V1aR), encoded by the AVPR1A gene, is a G protein-coupled receptor that mediates the effects of arginine vasopressin (AVP). Primarily coupled to Gq/11 proteins, its activation leads to increased intracellular calcium levels through the phospholipase C/IP3/DAG pathway. It is widely expressed in the brain and peripheral tissues, including vasculature, liver, kidney, and heart. V1aR plays a key role in vasoconstriction, hepatic glycogenolysis, and social behaviors. Selective agonists and antagonists are used to differentiate its functions from other vasopressin receptors, such as V2 and V1b.

Other names
AVPR1AV1aAVPR V1aAntidiuretic hormone receptor 1Avascular/hepatic-type arginine vasopressin receptor
02

Mechanism of action

Gq/11 protein activation leading to phospholipase C activation, increased IP3/DAG, and raised intracellular Ca2+ levels.

03

Biological functions

VasoconstrictionHepatic glycogenolysisSocial behavior modulationSignal transductionCalcium mobilization
04

Disease associations

Cardiovascular diseaseSocial behavior disorders
05

Safety considerations

Potential for vasoconstriction-related side effectsOff-target effects on other vasopressin receptors
06

Interacting drugs

Arginine vasopressin (AVP)

2 more in the full profile.

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