0100488857

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EFFECT OF A POTENT THROMBIN INHIBITOR, NO.407, ON PLATELET FUNCTION IN VITRO AND IN VIVO

English (英語)

The Kobe journal of the medical sciences

26(1)

47-60

1980-03

No. 407 (Nα-(6,7-dimethoxynaphthalene-2-sulfonyl)-L-ArginylN-(2-methoxyethyl) glycine) is a new thrombin inhibitor that shows a potent and highly selective inhibitory effect. The effect of No. 407 on platelet function was studied in vitro and in vivo. No.407 showed a potent inhibitory action on thrombin-induced platelet aggregation with 150 of 0.2 μM. On collagen-induced platelet aggregation and secondary aggregation of guinea-pig platelets, No.407 was found to be a weak inhibitor, but no inhibition was observed on ADP- or arachidonate-induced platelet aggregation. No.407 showed a weak inhibition of platelet adhesiveness to glass beads and clot retraction. At doses of 12.5 mg/kg s.c. and above, the micropuncture bleeding time in mice was prolonged significantly, and the prolongation was also observed at oral doses of 300 mg/kg and above. No. 407 prevented the decrease in platelet count potently in the experimental DIC caused by thrombin infusion. Its effective plasma level was about 0.2 μM. These findings imply that No. 407 may be a useful antithrombotic drug and, especially, in DIC.

DIC

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