| Literature DB >> 9873521 |
J Sakaki1, T Murata, Y Yuumoto, I Nakamura, T Trueh, T Pitterna, G Iwasaki, K Oda, T Yamamura, K Hayakawa.
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.Entities:
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Year: 1998 PMID： 9873521 DOI： 10.1016/s0960-894x(98)00387-4
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823