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  • 标题:NQ-Y15 Inhibits the Calcium Mobilization by Elevation of Cyclic AMP in Rat Platelets
  • 本地全文:下载
  • 作者:Tong-Shin CHANG ; Ki-Seon LEE ; Gwi-Yeop LEE
  • 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:480-483
  • DOI:10.1248/bpb.24.480
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:2-[(4-Cyanophenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15) is a dual action drug which acts as a thromboxane A2 (TXA2) synthase inhibitor and TXA2/PGH2 receptor antagonist. In the present study, we examined the effects of NQ-Y15 on Ca2+ mobilization, which is the common event in various types of platelet activation, in arachidonic acid (AA)-stimulated rat platelets. The elevation of cytosolic Ca2+ concentration ([Ca2+]i) induced by AA was inhibited by NQ-Y15 in a concentration-dependent manner. This inhibition-effect of NQ-Y15 was found to be based on the suppression of the rise in [Ca2+]i by the inhibition of both Ca2+ release from internal stores and Ca2+ influx from the extracellular space. Our successive trial was focused on the role of cyclic AMP (cAMP) in the action of NQ-Y15, because cAMP was reported to be increased by dual action drugs such as picotamide and to inhibit the increase in [Ca2+]i. NQ-Y15 was confirmed to increase cAMP in AA-stimulated rat platelets. These results suggested that NQ-Y15 might inhibit the rise in [Ca2+]i in AA-treated rat platelets by increasing cAMP, which is involved in the inhibition of platelet activation.
  • 关键词:2-[(4-cyanophenyl)amino]-3-chloro-1,4-naphthalenedione;platelet;calcium mobilization;cyclic AMP
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