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Lysophosphatidic acid (radyl-glycerol-phosphate, LPA) has captured the interest of lipid biochemists, cell biologists, physiologists, and physicians alike due to its myriad biological effects. Since it was first identified in 1957 as the active ingredient of Darmstoff (smooth muscle-stimulating substance)[1, 2], our knowledge of LPA biology has steadily increased. In spite of hundreds of publications, we still lack a clear understanding of the role of LPA in disease or even its physiological role. Since the last comprehensive review on LPA in this journal by Tokumura in 1995 [3] major advances have occurred with regard to the production and breakdown, as well as the identification of plasma membrane and intracellular receptors for LPA. The present review is focused on these two aspects of LPA biology with a strong commitment to the physiological and pathophysiological context of these fundamental discoveries.