Over the past decade, the paradigm shift of adipose tissue as being far beyond its pivotal role in lipid and energy homeostasis has been increasingly recognized. Arguably, adipocytes as well as other adipose cells are at present considered bona fide secretory cell types, using pleiocrine pathways for delivery of multiple signaling proteins designated adipokines. Transcriptomic and proteomic studies "upregulate" more than hundred adipokines that are synthesized, stored, and released by adipose tissue cells. However, the functional description of adipose-secreted proteins look like an incomplete puzzle. Here we describe only adipsin, adiponectin, leptin, resistin, visfatin, tumor necrosis factor-alpha, interleukin-6, plasminogen activator inhibitor type 1, nerve growth factor, brain-derived neurotrophic factor, and metallothioneins, and focus on their implications for the pathogenesis of various diseases besides obesity and related disorders. Accordingly, a horizon of the adipopharmacology of disease is outlined. Biomed Rev 2007; 18: 27-43.