Angiotensin (Ang II) is an octapeptide hormone that plays a crucial role in the maintenance of electrolyte homeostasis and cardiovascular function. The hemodynamic and cardiovascular effects o f Ang II are mediated by high-affinity cell-surface receptors of the AT(1) pharmacologic class. The mammalian AT(1) receptor has recently been cloned and found to encode a 359-amino-acid protein of 41,000 molecular weight. The AT, receptor belongs to the guanine nucleotide regulatory-proteincoupled receptor family and is coupled to the phospholipase C signal transduction pathway as evidenced by intracellular calcium mobilization and inositol trisphosphate production upon receptor activation. Cloning of the AT(1) receptor has facilitated the study of structure-function correlates and molecular mechanisms of receptor regulation, and will lead to substantial progress in elucidating the mechanisms governing Ang II actions.