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Through the multiple actions of angiotensin II (AII), the renin‐angiotensin system (RAS) participates in cardiovascular homeostasis. Angiotensin II acts by binding to specific membrane‐bound receptors, which are coupled to one of several signal transduction pathways. These AII receptors exhibit heterogeneity, represented by AT₁ and AT₂ receptor subtypes. The AT₁ receptor mediates the major cardiovascular action of the RAS. This receptor has been cloned from multiple species, disclosing features consistent with a transmembrane, G‐protein‐linked receptor. Further AII receptor heterogeneity is evident by the cloning of isotypes of the AT₁ receptor. Blocking the interaction of AII with its receptor is the most direct site to inhibit the actions of the RAS. Many AII receptor antagonists, including peptide analogs of AII and antibodies directed against AII, possess unfavorable properties that have limited their clinical utility …