Highly selective angiotensin II (Ang II) type 1 (AT(1)) receptor blockers (ARBs) are now available. The AT(1) receptor is a member of the G protein-coupled receptor (GPCR) superfamily and block the diverse effects of Ang II. Several ARBs are available for clinical use. Most ARBs have common molecular structures (biphenyl-tetrazol and imidazole groups) and it is clear that ARBs have 'class effects'. On the other hand, recent clinical studies have demonstrated that not all ARBs have the same effects, and some benefits conferred by ARBs may not be class effects, and instead may be 'molecular effects'. In addition, each ARB has been clearly shown to have specific molecular effects in basic experimental studies, and these effects may be due to small differences in the molecular structure of each ARB. However, it is controversial whether ARBs have molecular effects in a clinical setting. Although the presence of molecular effects for each ARB based on experimental studies may not directly influence the clinical outcome, this possibility has not been adequately evaluated. This review focuses on the class effects versus molecular effects of ARBs from bench to bedside.