Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ET A receptor antagonist through the modification of Bosentan ( HY-A0013 ). Nebentan inhibits [ 125 I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K i of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
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