Publication | Open Access
(<i>S</i>)-<i>N</i>-{3-[1-Cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1<i>H</i>-indol-7-yl}-methanesulfonamide: A Potent, Nonsteroidal, Functional Antagonist of the Mineralocorticoid Receptor
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2007
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HypertensionFunctional AntagonistPharmacotherapyChemical BiologyIndole AnalogsChemical DerivativePharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryPotent SeriesBiochemistryAntihypertensive TherapyMechanism Of ActionFirst Mr AntagonistPharmacological AgentPharmacologyNatural SciencesMedicineDrug Discovery
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.
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