Title of article
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity
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 ,
Issue Information
روزنامه با شماره پیاپی سال 1998
Pages
6
From page
2241
To page
2246
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1998
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
789605
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