There has been recent interest in the role of α-adrenoreceptor manipulation and the prevention of renal dysfunction. α2-Agonists have been used in the prevention of renal dysfunction after extracorporeal circulation. In the setting of sepsis and hypotension, α1-agonists have also been shown to be beneficial to renal function. Accordingly, we review the renal effects of α2-agonists as studied in animal models and present currently available evidence from controlled and uncontrolled human studies. Although the pathophysiology of the interaction between α-adrenoreceptor manipulation and renal function is complex, the balance of evidence suggests that central α-receptor agonists may be useful in preventing renal dysfunction as prophylactic agents before a state of α-receptor over-stimulation. α-Receptor agonists administered peripherally also appear useful in states of hyperdynamic hypotension, in which α-receptors may be dysfunctional. In both cases, restoration of α-adrenoreceptor homeostasis appears to be the key to the achievement of renal protection.