RWJ-58259: a selective antagonist of protease activated receptor-1.

  title={RWJ-58259: a selective antagonist of protease activated receptor-1.},
  author={Bruce P Damiano and Claudia K. Derian and Bruce E Maryanoff and Han Cheng Zhang and Patricia Andrade Gordon},
  journal={Cardiovascular drug reviews},
  volume={21 4},
Protease activated receptor-1 (PAR-1) is a key mediator of the cellular actions of alpha-thrombin. Thus, antagonism of this unique G-protein coupled receptor with a small molecule represents a means of selectively inhibiting thrombin's cellular actions without inhibiting its proteolytic activity. RWJ-58259 (alphaS)-N-[(1S)-3-amino-1-[[(phenylmethyl)- amino]carbonyl]propyl]-alpha-[[[[[1-(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indazol-6-yl]amino]carbonyl]amino]-3,4… CONTINUE READING


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