A glucocorticoid and mineralocorticoid receptor agonist
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)
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