The role of plasma proteases in inflammation. The study by using FUT-175, a selective serine-protease inhibitor.:—The study by using FUT-175, a selective serine-protease inhibitor—

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Out of numerous factors relating to the pathogenesis and development of inflammation, the roles of plasma serine-proteases including, kallikrein, Clr, Cls, trypsin and plasmin are not thoroughly elucidated. To investigate the role of an enzyme, it is effective to use the selective inhibitor on it. In the present studies, authors used two pharmacological tools, i.e., FUT-175 (nafamostat mesilate), a selective inhibitor on serine-proteases and indomethacin, a selective inhibitor on cyclooxygenase and investigated the participation of serine-proteases in inflammation. At first, the pharmacological profile of FUT-175 was investigated in comparison with indomethacin. It was made clear that FUT-175 had selective inhibitory activities only on serine-proteases and no indomethacin-like activities. In the second, FUT-175 had significant suppressive effects on the representative models of inflammation including carrageenin-induced pleurisy and foot edema and adjuvant-arthritis in rats. These results suggest that plasma serine-proteases, especially complement system and kallikrein-kinin system play an important part in the processes of either acute or chronic inflammatory reactions.
日本炎症・再生医学会の論文