Angiotensin II receptor type 1 (AGTR1) (AGTR1)

The Angiotensin II receptor type 1 (AGTR1) is a G protein-coupled receptor that mediates the primary cardiovascular and renal effects of Angiotensin II, the main effector of the renin-angiotensin-aldosterone system (RAAS) [1, 4]. Activation of AGTR1 leads to potent vasoconstriction, stimulation of aldosterone secretion, and increased renal sodium reabsorption, which collectively increase blood pressure and maintain fluid homeostasis [2, 3]. In pathological states, excessive AGTR1 signaling contributes to hypertension, cardiac remodeling, and the progression of chronic kidney disease [1, 2]. As a result, AGTR1 is a critical therapeutic target for Angiotensin II Receptor Blockers (ARBs), such as losartan and valsartan, which are standard treatments for hypertension and heart failure [2, 4]. These medications work by competitively inhibiting the binding of Angiotensin II to AGTR1, thereby reducing peripheral resistance and preventing organ damage [2, 3]. Blocking AGTR1 also leads to a compensatory increase in Angiotensin II levels, which may then act on the Angiotensin II receptor type 2 (AT2R), potentially providing additional vasoprotective effects [1, 2].

Other names

AT1 receptorAngiotensin II type-1 receptorAT1RAGTR1Angiotensin receptor 1

Competitive antagonism of the Angiotensin II receptor type 1, preventing the binding of Angiotensin II and inhibiting its downstream signaling pathways that lead to vasoconstriction and fluid retention [2, 3].