The physiology of adipose tissue has a key role in the pathogenesis of the metabolic syndrome and related cardiovascular disorders. Three main functions of adipocytes have been proposed to explain this role: the secretion of adipocyte-derived hormones (so-called adipokines), energy dissipation/thermogenesis, and energy storage. There is mounting evidence that this repertoire of actions and reactions contributes to whole-body glucose and energy homeostasis, the control of blood pressure, immune-system function, haemostasis and atherosclerosis. In this article we highlight the most recent examples of adipocyte-based therapies and discuss future pharmacological options for exploiting this triad of adipocyte functions.