Target intelligence / Profile preview

Vasopressin receptor (V1 subtype) (V1 receptor)

Target
V1 receptor
Molecular classification
G protein-coupled receptor, Receptor, Peptide hormone receptor
01

Overview

The vasopressin receptor (V1 subtype) is a G protein-coupled receptor located on vascular smooth muscle, where it mediates vasoconstriction in response to the endogenous hormone vasopressin. Terlipressin is a synthetic analogue of vasopressin that acts as an agonist at this receptor, used primarily to treat hepatorenal syndrome and bleeding esophageal varices. By stimulating the V1 receptor, terlipressin induces splanchnic vasoconstriction, increases effective circulating volume, and improves renal perfusion. Terlipressin is notable for its longer duration of action compared to vasopressin and its use as a first-in-class medication for acute kidney injury in hepatorenal syndrome. Safety concerns include risk of ischemia, respiratory failure, and potential fetal harm.

Other names
Vasopressin receptor V1Vasopressin V1 receptorV1a receptorVascular vasopressin receptor
02

Mechanism of action

Vasopressin receptor agonism (V1 subtype): causes splanchnic and systemic vasoconstriction, increases mean arterial pressure, and reduces portal hypertension. Prodrug conversion: terlipressin is a prodrug for lysine-vasopressin, which also activates vasopressin receptors.

03

Biological functions

VasoconstrictionSignal transductionRegulation of blood pressureRegulation of renal perfusion
04

Disease associations

Cardiovascular diseaseRenal diseaseLiver diseaseOther
05

Safety considerations

Respiratory failure/hypoxiaIschemiaPotential for fetal harmBlue skin/lip discoloration, numbness, and pain
06

Interacting drugs

Terlipressin

4 more in the full profile.

07

Biomarkers

Serum creatinineMean arterial pressure (MAP)Signs of portal hypertension

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