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- W2883205142 abstract "Gabexate mesilate:[Ethyl p-(6-guanidinohexanoyloxy)benzoate]methanesulfonate, which is clinically used as a potent trypsin inhibitor in Japan, inhibits competitively the hydrolytic reactions with synthetic substrates by thrombin and factor Xa. However, its virtual anticoagulant effect in vivo remains to be evaluated, because of its short halflife due to the presence of plasma esterase. In the present study, the inhibitory effect of gabexate mesilate on experimental disseminated intravascular coagulation was investigated in comparison with those of heparin and aprotinin. 125I-Fibrinogen was injected into rats along with t-AMCHA to prevent lysis of fibrin formed. Five minutes after a infusion of gabexate mesilate, heparin, aprotinin or saline, intravascular cogulation was triggered by a continuous infusion of thrombin or tissue thromboplstin. The deposition of fibrin in kidney was continuously monitored by scintillation detector. Platelet count and 125I-fibrinogen in blood were determined. The formation of fibrin induced by thrombin and tissue thromboplastin was completely inhibited by continuous administration of 120 μmol gabexate mesilate/kg/h or 200 U heparin/kg/h. On the other hand, aprotinin failed to prevent the deposition of fibrin even at dose of 50,000 U/kg/h. Also, other parameters corroborated the same aspect. The naturally occuring lysis of the microthrombi previously formed by thrombin was not blocked by the infusion of 120 μmol gabexate mesilate/kg/h or 200 U heparin/kg/h. However, aprotinin, at 5,000 U/kg/h, completely blocked the lysis. Using clotting assay, the biological half life of gabexate mesilate in human plasma was found to be ten times longer than that in rat plasma, suggesting that much lower dose would be effective in human. In conclusion, gabexate mesilate is a relevant compound as an antithrombotic agent." @default.
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- W2883205142 date "1981-01-01" @default.
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- W2883205142 title "Inhibitory Effect Of Gabexate Mesilate On Experimental Disseminated Intravascular Coagulation" @default.
- W2883205142 doi "https://doi.org/10.1055/s-0038-1652081" @default.
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