(S)-N-{3-[1-Cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: A Potent, Nonsteroidal, Functional Antagonist of the Mineralocorticoid Receptor
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- 作者：Michael G. Bell ; Douglas L. Gernert ; Timothy A. Grese ; Matthew D. Belvo ; Peter S. Borromeo ; Sally A. Kelley ; Joseph H. Kennedy ; Stanley P. Kolis ; Peter A. Lander ; Rachel Richey ; V. Scott Sharp ; Gregor
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：December 27, 2007
- 年：2007
- 卷：50
- 期：26
- 页码：6443 - 6445
- 全文大小：226K
- 年卷期：v.50,no.26(December 27, 2007)
- ISSN：1520-4804
文摘
A novel, potent series of indole analogs were recently developed as MR antagonists, culminating in 14. This compound represents the first MR antagonist in this class of molecules, exhibiting picomolar binding affinity and in vivo blood pressure lowering at pharmaceutically relevant doses.