An antithrombotic agent, NQ301, inhibits thromboxane $A_2$ synthase activity and blocks thromboxane $A_2$ receptor in rabbit platelets

  • Jin, Yong-Ri (College of Pharmacy, Chungbuk National University) ;
  • Ryu, Chung-Kiu (College of Pharmacy, Ewha Womans University) ;
  • Cho, Mi-Ra (Division of Life Science, College of Natural Sciences, Konkuk University) ;
  • Shin, Hwa-Sup (Division of Life Science, College of Natural Sciences, Konkuk University) ;
  • Yoo, Hwan-Soo (Division of Life Science, College of Natural Sciences, Konkuk University) ;
  • Yun, Yeo-Pyo (Division of Life Science, College of Natural Sciences, Konkuk University)
  • Published : 2003.10.01

Abstract

In the previous studies, we have reported that NQ30l, a synthetic l,4-naphthoquinone derivative, displayed a potent antithrombotic activity, and that this might be due to antiplatelet effect, which was mediated by inhibition of cytosolic $Ca^{2+}$ mobilization in activated platelets. In the present study, the effect of NQ301 on arachidonic acid cascade in activated platlets was examined. NQ301 concentration-dependently inhibited washed rabbit platelet aggregation induced by collagen (10 $\mu$g/ml), arachidonic acid (100 $\mu$M) and U46619 (1 $\mu$M), a thromboxane $A_2$receptor agonist, with $IC_50$ values of 0.60$\pm$0.02, 0.79$\pm$0.04 and 0.58$\pm$0.04 $\mu$M, respectively. (omitted)

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