Matches in SemOpenAlex for { <https://semopenalex.org/work/W1968853879> ?p ?o ?g. }
- W1968853879 endingPage "418" @default.
- W1968853879 startingPage "375" @default.
- W1968853879 abstract "In our studies, designed to synthesize an active center-directed plasmin (PL) inhibitor, N-(4-aminomethylbenzoyl)-4-(3-picolyloxy)-L-phenylalanine n-hexylamide dihydrochloride (PASI-535) was found. We characterized PASI-535 and analyzed the actions of PL, comparing with those of PASI-535 and tranexamic acid (t-AMCHA). (1) PASI-535 strongly inhibited not only fibrinolysis (IC50: 2.9 × 10−6 M) but also amidolysis (Ki value: 2.9 × 10−6 M) and fibrinogenolysis (IC50: 4.5 × 10−6 M) induced by PL. While t-AMCHA which strongly inhibited fibrinolysis (IC50: 6.0 × 10−5 M), rarely inhibited amidolysis (Ki value: 4.0 × 10−2 M) and fibrinogenolysis (IC50: 1.0 × 10−2 M). (2) PL is able to liberate kinins by degrading kininogen. This kinin-generation by PL was inhibited by 2 × 10−5 M PASI-535. However, it was little inhibited even by 1 × 10−3 M t-AMCHA. (3) The inhibitory effect of PASI-535 and t-AMCHA on tumor growth was studied. In sarcoma-180 bearing mice, ascites retention and the increase of tumor cells were markedly suppressed by subcutaneous injection of PASI-535, either 30 mg/kg/day or 50 mg/kg/day, for 5 days, and the inhibitory effect was dosedependent. Although t-AMCHA also reduced both ascites retention and the increase of tumor cells, it needed approximately 40 times (2 g/kg/day) the amount of PASI-535 to exert these effects. PASI-535 may be a useful tool in analyzing the multiplicity of PL actions. Moreover, PASI-535 can be used as an antifibrinolytic drug which has a mechanism of function different from that of t-AMCHA." @default.
- W1968853879 created "2016-06-24" @default.
- W1968853879 creator A5025546575 @default.
- W1968853879 creator A5052044688 @default.
- W1968853879 date "1982-12-01" @default.
- W1968853879 modified "2023-10-17" @default.
- W1968853879 title "Complex carbohydrates of the extracellular matrix structures, interactions and biological roles" @default.
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