PAR-2 (protease-activated receptor 2), a G-protein-coupled receptor activated by certain serine proteases such as trypsin and tryptase, is now considered a physiologically important molecule and also a novel target for drug development. PAR-2 is widely distributed in the mammalian body, especially throughout the alimentary system. PAR-2 plays various roles in the alimentary, circulatory, respiratory and neuronal systems. In the gastric mucosa, PAR-2 modulates multiple functions and exerts mucosal cytoprotection mainly by activating sensory neurons. Thus, PAR-2 would appear to be a therapeutic target for treatment of gastric mucosal injury. Agonists and/or antagonists for PAR-2 might also be applicable to the clinical treatment of patients with inflammatory diseases in other organs.