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Target intelligence / Profile preview
Angiotensin II Receptor Type 1 (AT1)
- Target
- AT1
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
Angiotensin II receptor type 1 (AT1) is a G protein-coupled receptor (GPCR), specifically coupled to the Gq/11 family of G proteins. It mediates most of the known physiological and pathophysiological effects of angiotensin II, a key peptide hormone in cardiovascular regulation. Excessive activation contributes to hypertension, cardiac hypertrophy, vascular remodeling, inflammation, and fibrosis. Drugs that block AT1 receptors—known as Angiotensin Receptor Blockers (ARBs)—are widely used for treating hypertension, heart failure, diabetic nephropathy, and related conditions.
- Other names
- AGTR1Angiotensin receptor type 1
02
Mechanism of action
Angiotensin Receptor Blockers (ARBs) block AT1 receptors, preventing angiotensin II from binding and activating the receptor, thus inhibiting downstream signaling pathways such as vasoconstriction, aldosterone release, and cardiac remodeling.
03
Biological functions
VasoconstrictionAldosterone synthesis/secretionIncreased vasopressin secretionCardiac hypertrophy/remodelingVascular smooth muscle cell proliferationRenal renin inhibitionRenal tubular sodium reuptakeModulation of central sympathetic nervous system activityCardiac contractility enhancementCentral osmocontrolExtracellular matrix formationSignal transduction
04
Disease associations
HypertensionHeart failureDiabetic nephropathyCardiovascular diseaseInflammationFibrosis
05
Safety considerations
Low blood pressureHigh circulating renin levels
06
Interacting drugs
Losartan
2 more in the full profile.
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