Description and references

Non-peptide proteolytic enzyme inhibitor which also inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, trypsin but not chymotrypsin; cf. aprotinin. Prepn as the p-toluenesulfonate salt: S. Fujii, T. Watanabe, DE 2050484; eidem, US 3751447 (1971, 1973 both to Ono). Enzyme inhibition: M. Muramatu, S. Fujii, Biochim. Biophys. Acta 268, 221 (1972); S. Tamura et al., ibid. 484, 417 (1977). Pharmacology: T. Okegada et al., Nippon Yakurigaku Zasshi 71, 71 (1975), C.A. 84, 218m (1976). Metabolism: M. Sugiyama et al., Oyo Yakuri 9, 733 (1975), C.A. 83, 188145s (1975). Metabolism of inhibitory effect on platelet aggregation: G. Kosaki et al., Thromb. Res. 20, 587 (1980). Beneficial action in traumatic shock: A. M. Lefer et al., IRCS Med. Sci. Libr. Compend. 8, 278 (1980); in exptl acute pancreatitis: J. R. Wisner et al., Pancreas 2, 181 (1987). Comparative clinical study in acute pancreatitis: N. Tanaka et al., Adv. Exp. Med. Biol. 120, 367 (1979). Teratology and toxicity study: T. Fujita et al., Oyo Yakuri 9, 743 (1975), C.A. 83, 188322x (1975).

Derivative