226915-92-0Relevant academic research and scientific papers
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide
Liu, Jun,Sun, Bin,Zhao, Xiaoyu,Xing, Jie,Gao, Yanhui,Chang, Wenqiang,Ji, Jianbo,Zheng, Hongbo,Cui, Changyi,Ji, Aiguo,Lou, Hongxiang
, p. 7166 - 7185 (2017/09/07)
Protease-activated receptor-1 (PAR1), a G-protein-coupled receptor, plays a critical role in thrombin-mediated platelet aggregation. It is regarded as a promising antithrombosis target that is unlikely to result in bleeding. Here, we describe the synthesi
Metabolism-based identification of a potent thrombin receptor antagonist
Clasby, Martin C.,Chackalamannil, Samuel,Czarniecki, Michael,Doller, Dario,Eagen, Keith,Greenlee, William,Kao, Grace,Lin, Yan,Tsai, Hsingan,Xia, Yan,Ahn, Ho-Sam,Agans-Fantuzzi, Jacqueline,Boykow, George,Chintala, Madhu,Foster, Carolyn,Smith-Torhan, April,Alton, Kevin,Bryant, Matthew,Hsieh, Yunsheng,Lau, Janice,Palamanda, Jairam
, p. 129 - 138 (2008/02/03)
The metabolism of our prototypical thrombin receptor antagonist 1, K i = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites were verified independently by synthesis. Compound 4 was shown
THROMBIN RECEPTOR ANTAGONISTS
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Page 80, (2010/11/30)
Heterocyclic-substituted tricyclics of formula (I) or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally subs
