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  • 标题:Antagonism of the Human Thromboxane A2 Receptor by an Anti-asthmatic Agent AA-2414
  • 本地全文:下载
  • 作者:Tomofumi KUROKAWA ; Tatsumi MATSUMOTO ; Yasuko ASHIDA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1994
  • 卷号:17
  • 期号:3
  • 页码:383-385
  • DOI:10.1248/bpb.17.383
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The human thromboxane A2 receptor (TXA2-R)-coding gene was introduced into Chinese hamster ovary cells and a cell line (TCHO-25) stably expressing TXA2-R, at a level of 3×105/cell, was obtained. An anti-asthmatic agent AA-2414 [(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid] competitively inhibited the specific binding of a TXA2 mimic ([3H] U-46619) to the TCHO-25 cells, with an IC50 of 6.0×10-8M, indicating that the drug is an antagonist of human TXA2-R. The TCHO-25 cells offer a tool for the screening and characterization of human TXA2-R antagonists.
  • 关键词:thromboxane A2 receptor antagonist;anti-asthmatic agent;AA-2414;(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid
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