Pharmacological profile of T-0201, a highly potent and orally active endothelin receptor antagonist.

@article{Hoshino1998PharmacologicalPO,
  title={Pharmacological profile of T-0201, a highly potent and orally active endothelin receptor antagonist.},
  author={Takashi Hoshino and Rena Yamauchi and K. Kikkawa and Hideo Yabana and Satoshi Murata},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1998},
  volume={286 2},
  pages={643-9}
}
The authors studied the pharmacological properties of N-(6-(2-(5-bromopyrimidin-4-yl)-4-(2-hydroxy-1, 1-dimethylethyl)benzensulfonamide sodium salt sesquihydrate (T-0201), a new nonpeptide endothelin (ET) receptor antagonist, in vitro and in vivo. In binding studies, T-0201 competitively antagonized the specific binding of [125I]-ET-1 to human cloned ETA receptors (the Ki value was 0.015 +/- 0.004 nM). T-0201 weakly inhibited [125I]-ET-1-binding to human cloned ETB receptors; the Ki value was… CONTINUE READING

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