The type 1 angiotensin receptor (AT1) mediates the important biological actions of the peptide hormone, angiotensin II (AngII), by activating an array of intracellular signaling pathways. The unique temporal arrangement and duration of AngII-stimulated signals suggests a hierarchy of post-AT1 receptor binding events that permits activation of selective effector pathways. Moreover, it predicts that the coupling of AT1 receptors is tightly regulated, allowing cells to differentiate acute responses from those requiring longer periods of stimulation. Recent studies have concentrated on delineating the molecular processes involved in modulating AT1 receptor activity. In addition to AT1 receptor modification (phosphorylation), trafficking (internalization and degradation) and interaction with regulatory intracellular proteins, other processes may include receptor dimerization, cross-regulation by other receptor systems, and receptor isomerization between activated and non-activated forms. This review focuses on recent advances in this area of research, highlighting directions for future investigation.