The renin-angiotensin system is a coordinated hormonal cascade of crucial importance in cardiovascular and renal function. The primary effector peptide angiotensin II functions at two major receptors, the AT1 and AT2 receptors. AT2 receptors mediate vasodilation and natriuresis. Regarding vasodilator actions, AT2 receptors oppose the AT1 receptor-mediated vasoconstrictor action of angiotensin II. Regarding the natriuretic actions of AT2 receptors, des-aspartyl 1-angiotensin II, rather than angiotensin II, is the preferred agonist. Regarding both the vasodilator and natriuretic properties of AT2 receptors, the beneficial blood pressure reduction and natriuretic responses to AT1 receptor blockade are mediated, at least in part, by AT2 receptor activation. In addition, AT2 receptor activation suppresses renin biosynthesis and release at renal juxtaglomerular cells. Therefore, AT2 receptors are potential therapeutic targets in hypertension.