Bioorganic and Medicinal Chemistry Letters p. 2241 - 2246 (1998)
Update date:2022-08-05
Topics:
Sakaki, Junichi
Murata, Toshiki
Yuumoto, Yoko
Nakamura, Ikushi
Frueh, Thomas
Pitterna, Thomas
Iwasaki, Genji
Oda, Kyoko
Yamamura, Takaki
Hayakawa, Kenji
IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5- isoxazolyl)-phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ET(A) + ET(B)) [Ki(ET(A))=1.8 nM, Ki(ET(B))=1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ET(B) selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.
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