Abstract: Selective activation or inhibition of the angiotensin Ⅱ type 2 (AT₂) receptor can cause vasodilation, decrease cell proliferation, promote neurite outgrowth and block neuronal excitability. The AT₂ receptor can be used as a potential drug target for the treatment of cardiovascular diseases, fibrosis, inflammation, neuronal diseases and tumors. Research and development of new drugs that selectively act on the AT₂ receptor and the mechanism of intracellular signal transduction involving the AT₂ receptor is a challenging but worthy endeavor. We review research progress on the AT₂ receptor and compounds that act on the AT₂ receptor, along with structure-activity relationship analysis, to provide reference and guidance for further research in this field.