The biological functions of angiotensin (Ang) II are mediated by two Ang II receptors, designated type 1 receptor (AT1R) and type 2 receptor (AT2R). Most of the cardiovascular effects of Ang II are mediated by AT1R that is expressed widely in the body. The expression of AT1R is up-regulated in cardiovascular lesions, and is regulated by many endogenous bioactive substances and drugs. The AT2R is generally considered to antagonize the effects of AT1R, but its precise function remains enigmatic and controversial, particularly in humans. The expression of AT2R is low in normal adult animals, but AT2R expression is up-regulated in cardiovascular lesions. The dynamic regulation of AT1R and AT2R expression suggests an active involvement of Ang II receptors in the development of cardiovascular diseases such as atherosclerosis, heart failure, chronic kidney diseases and cerebrovascular diseases. Further clarification of gene regulatory mechanisms of Ang II receptors may identify potential targets for the development of novel therapeutics for cardiovascular diseases.