Target intelligence / Profile preview

Arginine vasopressin receptor 1A (AVPR1A) (AVPR1A)

Target
AVPR1A
Molecular classification
G protein-coupled receptor, Rhodopsin-like GPCR, Receptor
01

Overview

Arginine vasopressin receptor 1A (AVPR1A) is a G protein-coupled receptor (GPCR) that serves as a primary mediator for the hormone arginine vasopressin (AVP) in vascular smooth muscle, the liver, and the central nervous system (UniProt P37288). Upon binding AVP, the receptor activates the Gq/11 signaling pathway, stimulating phospholipase C and increasing intracellular calcium levels to induce vasoconstriction and glycogenolysis (NCBI Gene ID: 552). In the brain, AVPR1A is expressed in areas like the amygdala and hypothalamus, where it plays a pivotal role in regulating social behaviors, including social recognition, aggression, and pair bonding (PMID: 28938441). Pathologically, dysregulation of AVPR1A signaling is implicated in cardiovascular diseases such as hypertension and heart failure, as well as neurodevelopmental conditions like autism spectrum disorder (PMID: 15107203). Therapeutic strategies include the use of selective agonists like selepressin for vasodilatory shock and antagonists like balovaptan for improving social communication in autism (ClinicalTrials.gov). The receptor's broad physiological impact makes it a versatile target, though selectivity remains a challenge to avoid cross-reactivity with V2 or oxytocin receptors.

Other names
Vasopressin V1a receptorV1aRAntidiuretic hormone receptor 1AAVPR1V1 receptor
02

Mechanism of action

AVPR1A ligands function as agonists to promote vasoconstriction in shock states or as antagonists to inhibit vasopressin-mediated effects in cardiovascular and behavioral disorders (PMID: 28938441).

03

Biological functions

Signal transductionVasoconstrictionPlatelet aggregationGlycogenolysisSocial behavior regulationCircadian rhythm regulation
04

Disease associations

Cardiovascular diseaseHypertensionHeart failureAutism spectrum disorderSocial anxiety disorderRaynaud's disease
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Safety considerations

Risk of excessive vasoconstriction and tissue ischemia with agonistsPotential for cross-reactivity with V2 and oxytocin receptorsHypotension with antagonistsPotential impact on social bonding and emotional processing
06

Interacting drugs

Conivaptan

6 more in the full profile.

07

Biomarkers

CopeptinArginine vasopressin (AVP) plasma levelsBlood pressureSocial Responsiveness Scale (SRS-2) scores

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