Effect of PP1D-1, a Synthetic Antiplatelet Compound, on Rabbit Platelets

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Author(s)

Abstract

The antiplatelet mechanism of a synthetic compound, 2-chloro-3-methoxycarbonylpropionamido-1, 4-naphthoquinone (PP1D-1), was studied by employing washed rabbit platelets in vitro. PP1D-1 concentration-dependently inhibited thrombin (0.1 U/ml)-, platelet-activating factor (2 ng/ml)-, collagen (10 μg/ml)-, arachidonic acid (100 μM)- and U46619 (1 μM)-induced aggregation and ATP release in washed rabbit platelets. The IC<SUB>50</SUB> values of PP1D-1 for aggregation induced by the above inducers are 17.9±1.7, 9.8±1.1, 3.9±0.4, 1.8±0.3 and 1.7±0.3 μM, respectively. PP1D-1 did not affect platelet thromboxane B<SUB>2</SUB> or prostaglandin D<SUB>2</SUB> formation induced by arachidonic acid, indicating that it did not affect cyclooxygenase and thromboxane synthase activities. PP1D-1 significantly inhibited the formation of inositol 1, 4, 5-trisphosphate caused by these five platelet stimulators. Moreover, PP1D-1 inhibited the increase in intracellular calcium concentration induced by these agents. On the contrary, PP1D-1 did not inhibit thapsigargin-elevated intracellular calcium concentration in indomethacin-pretreated platelets, indicating it did not influence the effect of thapsigargin. According to these data, PP1D-1 exerts antiplatelet effects mainly by inhibiting phosphoinositide turnover.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 76(2), 141-148, 1998-02

    The Japanese Pharmacological Society

References:  28

Codes

  • NII Article ID (NAID)
    10008191395
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    ART
  • ISSN
    00215198
  • NDL Article ID
    4416239
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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