Target intelligence / Profile preview

Vasopressin V₁A receptor (V₁A receptor (also AVPR1A))

Target
V₁A receptor (also AVPR1A)
Molecular classification
G protein-coupled receptor (GPCR), Membrane receptor, Peptide receptor, Family A GPCR
01

Overview

The Vasopressin V₁A receptor is a G protein-coupled receptor that mediates the physiological effects of the hormone arginine-vasopressin (AVP) primarily through activation of Gq/11 proteins, stimulating phospholipase C and increasing intracellular calcium. It is highly expressed on vascular smooth muscle cells and platelets but is also found in other tissues such as heart, brain, kidney, liver, and reproductive organs. Its activation results in vasoconstriction, regulation of blood pressure and circulating blood volume, thrombosis, and other endocrine and metabolic effects. Dysregulation or improper modulation of the V₁A receptor is implicated in a variety of disorders including cardiovascular diseases, thrombotic events, and renal pathologies. The receptor is targeted by both agonists (for vasoconstriction in shock) and antagonists (for specific vascular or renal conditions), with several therapeutic compounds and analogues developed for clinical management.

Other names
Vasopressin receptor type 1AV₁A receptorAVPR1AV1 receptor (colloquial but less specific)Vasopressin V1 receptor
02

Mechanism of action

Agonists induce vasoconstriction by increasing intracellular calcium in vascular smooth muscle via activation of phospholipase C signaling. Antagonists inhibit vasoconstriction, reduce vascular resistance, and may alleviate pathologic vascular contractility (e.g., in Raynaud's disease).

03

Biological functions

VasoconstrictionSignal transduction via Gq/11 proteins and phospholipase CRegulation of blood pressure and blood volumePlatelet aggregation (facilitates thrombosis)Modulation of vascular tone and cardiac functionLimiting antidiuretic effects in kidneyMyocardial hypertrophyGlycogenolysisUterine contraction
04

Disease associations

Cardiovascular disease (hypertension, shock states)ThrombosisCongestive heart failureLiver cirrhosis (risk of variceal bleeding with antagonists)Septic shockRaynaud's diseaseRenal pathologies
05

Safety considerations

Risk of excessive vasoconstriction, leading to hypertension, reduced tissue perfusionRisk of thrombosis from increased platelet aggregationPotential for variceal bleeding in liver cirrhosis if antagonizedRisk of altered renal blood flow or glomerular filtration with inappropriate agonist/antagonist use
06

Interacting drugs

Terlipressin (V₁ selective agonist)

4 more in the full profile.

07

Biomarkers

Circulating vasopressin levels (for patient selection/monitoring in certain syndromes)Platelet aggregation response variability as a marker of V₁A polymorphismBlood pressure and blood volume responses as indirect pharmacodynamic markers

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