The renin-angiotensin system (RAS) has a wide range of actions in biological processes ranging from development and reproduction to cardiovascular and renal functions. Most of these actions are mediated by the octapeptide hormone angiotensin II. The identified family of angiotensin II receptors is divided into two pharmacological classes: type 1 (AT1) and type 2 (AT2). The classically recognized actions of the RAS are primarily mediated by the AT1 subtype of angiotensin receptors, and these receptors are the targets of a new class of anti-hypertensive agents. In recent years, our understanding of the physiological functions of AT1 receptors has been advanced through the use of gene-targeting technology. In this review, we will summarize the emerging picture of AT1 receptor functions that has been provided by gene-targeting experiments.