Author/Authors :
Junichi Sakaki، نويسنده , , Toshiki Murata، نويسنده , , Yoko Yuumoto، نويسنده , , Ikushi Nakamura، نويسنده , , Thomas Frueh، نويسنده , , Thomas Pitterna، نويسنده , , Genji Iwasaki، نويسنده , , Kyoko Oda، نويسنده , , Takaki Yamamura، نويسنده , , Kenji Hayakawa، نويسنده ,
Abstract :
IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-isoxazolyl)-phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ETA+ETB) [Ki(ETA)=1.8 nM, Ki(ETB)=1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ETB selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mous, and guinea pig plasmas.
