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  • 标题:Inhibitory Effects of TA-993 and Its Metabolite MB3 on Platelet Activation Induced by Collagen and U-46619 in Human Platelets
  • 本地全文:下载
  • 作者:Makoto KATOH ; Tadashi KARASAWA ; Ayako WATANABE
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2001
  • 卷号:24
  • 期号:5
  • 页码:501-504
  • DOI:10.1248/bpb.24.501
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:In the present study, we investigated the effects of TA-993 and its metabolite MB3 on platelet activation in vitro. TA-993 and MB3 concentration-dependently inhibited platelet aggregation and ATP release induced by collagen in human platelets. Thromboxane (Tx) A2 formation, as determined by the production of TxB2, and the increase in intracellular Ca2+ concentration ([Ca2+]i) were also suppressed by TA-993 and MB3. TA-993 and MB3 did not inhibit TxA2 formation caused by arachidonic acid. These results suggest that the inhibition of platelet activation by TA-993 and MB3 is partly mediated by an inhibition of TxA2 formation at a step prior to cyclooxygenase. Furthermore, TA-993 and MB3 inhibited U-46619-induced platelet aggregation without blockade of the increase in [Ca2+]i, suggesting that they are likely to exert some additional effects on the intracellular events induced by Ca2+.
  • 关键词:TA-993;platelet aggregation;thromboxane;collagen;ATP release;intracellular calcium
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