Molecular Classification
G protein-coupled receptor, Receptor
Other Names
Angiotensin II receptor type 1, AT1R, AGTR1
Disease Roles
HypertensionDiabetic nephropathyCongestive heart failure

A-type 1 Angiotensin II Receptor 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.

Mechanism of Action

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

Biological Functions

Vasoconstriction
Aldosterone synthesis/secretion
Fluid/salt homeostasis
Signal transduction
Regulation of blood pressure
Cardiac hypertrophy
Vascular smooth muscle cell proliferation
Thirst/osmocontrol

Disease Associations

Hypertension
Diabetic nephropathy
Congestive heart failure
Cardiovascular disease
Coronary heart disease

Safety Considerations

  • Potential for hypotension
  • Angioedema
  • Hyperkalemia
  • Renal dysfunction
  • Drug interactions

Interacting Drugs

Angiotensin II receptor blockers (ARBs)

Associated Biomarkers

Biomarker
AGTR1 polymorphisms
Expression levels of AT1R