This review provides a systematic overview of the influence of the third generation beta-adrenoceptor antagonists on vascular and/or endothelial function at a cellular level as well as of the advantages of their application in hypertension, heart failure and coronary artery disease. Drugs antagonizing the beta-adrenoceptors have been in use for the treatment of hypertension for decades. In systolic heart failure and post-myocardial infarction, beta-adrenoceptor antagonists were proven to be effective in decreasing the number of deaths and improving morbidity. However, betaadrenoceptor antagonists are a heterogeneous drug group, consisting of agents with different selectivity for adrenoceptors and/or additional effects in heart and peripheral circulation. Beta-adrenoceptor antagonists comprise a multitude of different agents, which may have additional properties exceeding the pure receptor blockade. These features may provide additional benefit in the treatment of hypertension. The third generation drug nebivolol exerts a nitric oxide-mediated vasodilating activity which has positive effects on intima and media thickness and arterial rigidity, a major risk factor in cardiovascular disease. Moreover, anti-proliferative, anti-inflammatory, and anti-oxidative properties have been detected for carvedilol and nebivolol, contributing to their additional value in treatment of hypertension and heart failure.