The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs.

@article{Kogushi2011TheNA,
  title={The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs.},
  author={Motoji Kogushi and Toshiyuki Matsuoka and Tsutomu Kawata and Hiroko Kuramochi and Shinki Kawaguchi and Kimiyo Murakami and Hironobu Hiyoshi and Shuichi Suzuki and Tetsuya Kawahara and Akiharu Kajiwara and Ieharu Hishinuma},
  journal={European journal of pharmacology},
  year={2011},
  volume={657 1-3},
  pages={131-7}
}
Thrombin is a powerful agonist for platelets, the action of which is mediated by the thrombin receptor protease-activated receptor-1 (PAR-1). Recently, we discovered that E5555 (1-(3-tert-butyl-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-2H-isoindol-2-yl) ethanone hydrobromide) is a potent thrombin receptor antagonist. We evaluated the anti-platelet and anti-thrombotic effects of E5555. E5555 inhibited the binding of a high-affinity thrombin receptor-activating… CONTINUE READING

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