Isoflupredone

Isoflupredone is an agonist of glucocorticoid and mineralocorticoid receptors (EC₅₀s = 0.877 and 0.007 nM, respectively, in transactivation assays).¹ It inhibits LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages (IC₅₀ = 25.5 nM).² Topical application of a solution containing isoflupredone inhibits croton oil-induced ear edema in rats (ED₅₀ = 51.9 nM). Isoflupredone (0.6 mg/day) increases mean arterial pressure (MAP) and decreases the levels of potassium and sodium in the plasma and urine, respectively, in sheep.³ It reduces tumor levels of uridine incorporation into 18S and 28S rRNA in a P1798 murine lymphoma model when administered at a dose of 25 mg/kg.⁴

1.Grossmann, C., Scholz, T., Rochel, M., et al.Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: A comparison of their glucocorticoid and mineralocorticoid propertiesEur. J. Endocrinol.151(3)397-406(2004) 2.Park, K.-K., Ko, D.-H., You, Z., et al.Synthesis and pharmacological evaluations of new steroidal anti-inflammatory antedrugs: 9α-Fluoro-11β,17α,21-trihydroxy-3,20-dioxo-pregna-1,4-diene-16α-carboxylate (FP16CM) and its derivativesSteroids71(1)83-89(2006) 3.Coghlan, J.P., Denton, D.A., Mills, E.H., et al.Steroid antagonism of the ’hypertensinogenic’ activity of 9α-fluoroprednisoloneLife Sci.35(26)2609-2612(1984) 4.Stevens, J., Mashburn, L.T., and Hollander, V.P.Effect of 9α-fluoroprednisolone and ?-asparaginase on uridine incorporation into ribosomal RNA of P1798 lymphosarcomaBiochim. Biophys. Acta186(2)332-339(1969)