Angiotensin receptors are a class of G protein-coupled receptors with angiotensin II as their ligands. They are important in the renin-angiotensin system: they are responsible for the signal transduction of the vasoconstricting stimulus of the main effector hormone, angiotensin II. The AT1 and AT2 receptors have a similar affinity for angiotensin II, which is their main ligand. The AT1 receptor is the best elucidated angiotensin receptor. AT2 receptors are more plentiful in the fetus and neonate. Other poorly characterized subtypes include the AT3 and AT4 receptors.
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TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP); produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension, does not increase TPE at antihypertensive doses in rat tracheal plasma extravasation (TPE) models.
BIBS-39 is a selective nonpeptide angiotensin II receptor antagonist with Ki of 29 nM and 480 nM for AT1 and AT2 respectively; shows no high affinity for other receptors, shifts the AII concentration-contractile response curves in isolated rabbit aorta with pA2 of 8.14 and a slope of 1.06; shows effective antihypertensives in the model of the renal hypertensive rat.
Angiotensin II 5-valine
Angiotensin II 5-valine is an angiotensin II analog that is an agonist of AT1 angiotensin receptor.
Losartan (DuP-753) is a selective, competitive angiotensin II receptor type 1 (AT1) antagonist (IC50=20 nM) for treatment of high blood pressure (hypertension).
Losartan potassium (DuP-753 potassium) is a selective, competitive angiotensin II receptor type 1 (AT1) antagonist (IC50=20 nM) for treatment of high blood pressure (hypertension).
Valsartan (CGP-48933) is an angiotensin II receptor antagonist for treatment of high blood pressure and heart failure.
Candesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
Olmesartan(RNH 6270;CS 088) is an angiotensin II receptor antagonist which has been used for the treatment of high blood pressure.
Olmesartan medoxomil (CS-866) is an angiotensin II receptor antagonist which has been used for the treatment of high blood pressure.
Candesartan cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
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