| 应用于抗血栓治疗的新凝血酶受体抑制剂SCH-530348 |
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| 引用本文： | 李琴,王宇.应用于抗血栓治疗的新凝血酶受体抑制剂SCH-530348[J].中国新药杂志,2011(13). |
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| 作者姓名： | 李琴 王宇 |
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| 作者单位： | 南京海陵中药制药工艺技术研究有限公司; |
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| 摘 要： | 喜巴辛衍生物SCH-530348是蛋白酶激活受体1(PAR-1)的抑制剂,PAR-1是人血小板凝血酶最主要的一种受体。SCH-530348是第一种能抑制凝血酶诱导的血小板聚集而不影响凝血酶对胶原酶原活化能力的化合物。文中综述了SCH-530348的临床前和Ⅰ～Ⅲ期临床试验结果。这些研究表明SCH-530348具有降低缺血性事件发生风险的几率,同时不会明显增加机体出血的风险,临床上可应用于急性冠脉综合征的治疗和缺血性心血管事件的预防。
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| 关 键 词： | SCH-530348 蛋白酶激活受体1 凝血酶受体抑制剂 抗血栓治疗 |
SCH-530348,a new thrombin receptor antagonist in antithrombotic therapy |
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| LI Qin,WANG Yu.SCH-530348,a new thrombin receptor antagonist in antithrombotic therapy[J].Chinese Journal of New Drugs,2011(13). |
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| Authors: | LI Qin WANG Yu |
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| Institution: | LI Qin,WANG Yu(Nanjing Hailing R&D for Chinese Traditional Medicine,Nanjing 210049,China) |
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| Abstract: | SCH-530348,a himbacine derivative,is an antagonist of the protease-activated receptor-1(PAR-1) that is the primary receptor for thrombin on platelets in humans.SCH-530348 is the first agent in a new class of compounds that inhibit thrombin-mediated platelet aggregation without affecting the enzymatic activity of thrombin on fibrinogen.Preclinical and initial clinical studies have indicated that SCH-530348 has a potential to reduce the risk of ischemic events without significantly increasing the rate of blee... |
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| Keywords: | SCH-530348 protease-activated receptor-1 thrombin receptor antagonist antithrombotic therapy |
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