Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity |
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| Authors: | J Sakaki T Murata Y Yuumoto I Nakamura T Trueh T Pitterna G Iwasaki K Oda T Yamamura K Hayakawa |
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| Affiliation: | Takarazuka Research Institute, Novartis Pharma K.K., Japan. |
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| 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, mouse, and guinea pig plasmas. |
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