Pharmacological studies of FUT-175, nafamostat mesilate. V. Effects on the pancreatic enzymes and experimental acute pancreatitis in rats.

@article{Iwaki1986PharmacologicalSO,
  title={Pharmacological studies of FUT-175, nafamostat mesilate. V. Effects on the pancreatic enzymes and experimental acute pancreatitis in rats.},
  author={Masahiro Iwaki and Yoshitaka Ino and A Motoyoshi and Masayuki Ozeki and Takayuki Sato and Masateru Kurumi and Takuo Aoyama},
  journal={Japanese journal of pharmacology},
  year={1986},
  volume={41 2},
  pages={
          155-62
        }
}
Effects of FUT-175 on the pancreatic enzymes in vitro and in vivo in the enterokinase-induced experimental acute pancreatitis were investigated, and they were compared with those of gabexate and aprotinin. In in vitro experiments, FUT-175 inhibited the pancreatic protease activities 10 to 100 times more potently than gabexate. Furthermore, FUT-175 inhibited the enterokinase activity. Unlike aprotinin, FUT-175 inhibited alpha 2-macroglobulin bound trypsin activity as well as free trypsin. In in… 
The effects of nafamostat mesilate (FUT-175) on caerulein-induced acute pancreatitis in the rat
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    International journal of pancreatology : official journal of the International Association of Pancreatology
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TLDR
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Fut-175 seems to be an effective inhitor of protease-mediated hypercoagulation and fibrinolysis in severe acute pancreatitis.
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TLDR
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References

SHOWING 1-10 OF 14 REFERENCES
[Pharmacological studies of FUT-175, nafamstat mesilate. II. Effects on experimental acute pancreatitis].
TLDR
FUT-175 infused i.v. at a dose range of 5-50 micrograms/kg/min inhibited the increase in plasmatrypsin activity and reduced the mortality of rabbits in trypsin-induced acute pancreatitis in a dose-dependent manner, suggesting that FUT- 175 is beneficial as a therapeutic agent of acute pancreatritis.
Pharmacological studies of FUT-175, nafamstat mesilate. I. Inhibition of protease activity in in vitro and in vivo experiments.
TLDR
FUT-175 was highly effective in that, for example, intravenous dosing at 3 mg/kg could completely protect guinea pigs from the lethal Forssman shock and was also found to be effective in trypsin-induced shock in mice, in lethality due to thrombin-thrombosis in mice and in kinin formation in the inflammatory process in rats.
[Therapeutic effects of human urinary trypsin inhibitor on acute experimental pancreatitis].
TLDR
Results suggest that MTI may suppress pathogenesis and development of pancreatitis in several ways, for example, by directly inhibiting trypsin and by inhibiting tissue-damaging enzymes released from the pancreas by stimulation withtrypsin.
Inhibitory effect of aprotinin and gabexate mesilate on human plasma kallikrein.
  • M. Nakahara
  • Chemistry, Medicine
    Arzneimittel-Forschung
  • 1983
TLDR
It is concluded that a predominant effect of aprotinin in human plasma is due to its stability in contrast to instability of gabexate mesilate.
TRYPSIN RELEASE, KININ PRODUCTION, AND SHOCK; RELATIONSHIP IN EXPERIMENTAL AND HUMAN PANCREATITIS.
TLDR
The object of the present investigation is to measure the liberation of proteolytic enzymes in pancreatitis and to relate this to the release of substances affecting vascular smooth muscle and capillary permeability.
Measurement of the rate of plasmin action on synthetic substrates.
  • P. S. Roberts
  • Medicine, Biology
    The Journal of biological chemistry
  • 1958
TLDR
The Hestrin method is modified so that enzyme rates at optimal substrate concentrations of either TAME or LME can be determined by using the same standard reagents and procedures and the rate measurements are reproducible with an average deviation of 3 per cent of the rate.
On the physiological role of 2 -macroglobulin.
TLDR
Thrombin bound by α 2 -macroglobulin bound thrombin, contrary to earlier reports, was found to retain clotting activity although at a reduced rate and may play a role in the “hemostatic balance”.
The effects of Ca2+ on porcine enteropeptidase activity
Abstract The activity of porcine enteropeptidase was inhibited by low concentrations of EDTA suggesting a requirement for a divalent metal ion in the catalysis. The Group IIA metal ions, CA2+, Sr2+
New synthetic inhibitors of C1r, C1 esterase, thrombin, plasmin, kallikrein and trypsin.
TLDR
6'-amidino-2-naphthyl-4-guanidinobenzoate dihydrochloride, 4-(beta- amidinoethenyl)phenyl- 4-guAnidin Obenzoates dimethanesulfonate and 4-amidinos2-benzoylphenyl the most effective inhibitors of trypsin, plasmin, pancreatic kallikrein and thrombin.
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