Magnesium is the second most abundant cation within the cell after potassium and plays an important role in numerous biological functions. Several pieces of experimental evidence indicate that mammalian cells tightly regulate Mg(2+) content by precise control mechanisms operating at the level of Mg(2+) entry and efflux across the cell membrane, as well as at the level of intracellular Mg(2+) buffering and organelle compartmentation under resting conditions and following hormonal stimuli. This review will attempt to elucidate the mechanisms involved in hormonal-mediated Mg(2+) extrusion and accumulation, as well as the physiological implications of changes in cellular Mg(2+) content following hormonal stimuli.