Target intelligence / Profile preview

A-type 1 Angiotensin II Receptor (AT1)

Target
AT1
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The A-type 1 angiotensin II receptor (AT1), encoded by the AGTR1 gene, is a G protein-coupled receptor (GPCR) that plays a central role in the renin-angiotensin system (RAS), which regulates blood pressure, fluid balance, and cardiovascular function. It is the primary mediator of angiotensin II's effects, including vasoconstriction, aldosterone secretion, and cardiac hypertrophy. AT1 is a major drug target for antihypertensive therapy, with angiotensin II receptor blockers (ARBs) being used to treat hypertension, diabetic nephropathy, and congestive heart failure.

Other names
Angiotensin II receptor type 1AT1RAGTR1
02

Mechanism of action

Selective inhibition of the AT1 receptor, blocking vasoconstrictive and volume-increasing effects mediated through AT1R activation.

03

Biological functions

VasoconstrictionAldosterone synthesis/secretionFluid/salt homeostasisSignal transductionRegulation of blood pressureCardiac hypertrophyVascular smooth muscle cell proliferationThirst/osmocontrol
04

Disease associations

HypertensionDiabetic nephropathyCongestive heart failureCardiovascular diseaseCoronary heart disease
05

Safety considerations

Potential for hypotensionAngioedemaHyperkalemiaRenal dysfunctionDrug interactions
06

Interacting drugs

Angiotensin II receptor blockers (ARBs)
07

Biomarkers

AGTR1 polymorphismsExpression levels of AT1R

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