...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Biochemical Pharmacology >Evidence for separate effects of U73122 on phospholipase C and calcium channels in human platelets.
【24h】

Evidence for separate effects of U73122 on phospholipase C and calcium channels in human platelets.

机译：U73122对人血小板中磷脂酶C和钙通道的单独作用的证据。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

U73122 ((1-[6-(( 17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)exyl]-1H-p yrrole-2,5-dione)) is generally used as a selective inhibitor of phospholipase C (PLC) and the related rise in cytosolic Ca2+. Recently, by using hepatocytes, it was suggested that its action sites are different for PLC activation and increase in Ca2+ concentration. To verify whether U73122 has different sites for inhibiting PLC activation and calcium responses in human platelets, aggregation, Mn2+ influx, cytosolic Ca2+ increase and PLC activation were studied in response to thrombin and the synthetic agonist of the thromboxane receptor U46619 (9,11-dideoxy-9alpha,11alpha-methanoepoxyprostaglandin F2alpha). With both agonists, U73122 inhibited aggregation, Mn2+ influx and the enhancement of cytosolic calcium at concentrations of 2 microM or lower, while 10 microM was necessary to inhibit PLC activation. Our results suggested that U73122 is much more active in antagonizing Ca2+ channels, both the intracellular ones, which are activated by formation of inositol 1,4,5 P3 and those present on plasma membrane, than in reducing the activation of PLC.
机译：U73122（（1- [6-（（17β-3-甲氧基-1,3,5（10）-三烯-17-基）氨基）己基] -1H-p吡咯-2,5-二酮））用作磷脂酶C（PLC）的选择性抑制剂以及胞质Ca2 +的相关升高。近来，有人建议通过使用肝细胞，其作用部位对于PLC活化和Ca2 +浓度增加是不同的。为了验证U73122是否具有抑制人血小板中PLC活化和钙反应的不同位点，研究了对凝血酶和血栓烷受体U46619（9,11-dideoxy的合成激动剂）的聚集，Mn2 +内流，胞质Ca2 +的增加和PLC活化-9alpha，11alpha-methanoepoxyprostaglandin F2alpha）。对于这两种激动剂，U73122在2 microM或更低的浓度下均能抑制聚集，Mn2 +内流和胞质钙的增加，而抑制PLC激活则需要10 microM。我们的研究结果表明，U73122在拮抗Ca2 +通道（无论是胞内通道）（与肌醇1,4,5 P3的形成以及质膜上存在的那些通道激活）相比，在抑制PLC激活方面更具活性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号