Inhibition of platelet function by KB-2796.

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  • ＫＢ‐２７９６のＩｎ　ｖｉｔｒｏおよびＩｎ　ｖｉｖｏにおける抗血小板作用
  • KB-2796 ノ In vitro オヨビ In vivo ニ オケル コウ

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The anti-platelet activity of KB-2796, 1-Cbis (4-fluorophenyl) methyl)-4-(2, 3, 4-trimethoxybenzyl) piperazine dihydrochloride, was studied in guinea pigs and mice. When guinea pig platelet-rich plasma (PRP) was employed, platelet function was inhibited at high doses of KB-2796. The IC50 value for (3H) 5-HT release was 940 pM, and the IC50 values for collagen and ADP-induced platelet aggregation were 210 and 390 μM, respectively. Oral administration of KB-2796 at 10 ?? 100 mg/kg dose-dependently inhibited the transient thrombocytopenia induced by collagen, but not that caused by ADP. KB-2796 protected mice from death after intravenous injection of collagen plus epinephrine, with an ED50 value of 9.5 mg/kg, p.o. Oral administration of KB-2796 at 10 ?? 100 mg/kg dose-dependently reduced guinea pig platelet retention in glass bead columns and reduced the leakage of ADP and ATP from erythrocytes passing through similar columns. KB-2796, at a concentration of 1 ?? 10 μM, produced a stabilizing effect on guinea pig erythrocytes against hypotonic hemolysis. These results suggest that KB-2796 is an inhibitor of platelet function and that its inhibition is related mainly to the inhibition of leakage of ADP and ATP from erythrocytes.

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