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The protease-activated receptor (PAR) is the family of G protein-coupled, seven transmembrane domain receptors, currently consisting of four members, PARs 1-4. The activation of PARs occurs by proteolytic unmasking of the N-terminal cryptic receptor-activating tethered ligand. In the past decade since the cloning of PAR-1, physiological roles that PARs play have been gradually understood and are now considered extremely extensive and important. This review describes physiological and/or pathophysiological roles of PARs in the circulatory, digestive, respiratory and central nervous systems, on the basis of our works and of those achieved by other research groups. The future perspective of studies on PARs is also discussed, focusing on the possibility of clinical application of PAR-targeted drugs.

The G Protein-Coupled Protease Receptor PAR (Protease-Activated Receptor) as a Novel Target for Drug Development