In vitro and in vivo anti-inflammatory activity of the new glucocorticoid ciclesonide.

  title={In vitro and in vivo anti-inflammatory activity of the new glucocorticoid ciclesonide.},
  author={Michael Stoeck and Richard Riedel and Guenther Hochhaus and Dietrich H{\"a}fner and Jose Felix Marti Masso and Beate Schmidt and Armin Hatzelmann and Degenhard Marx and Daniela S. Bundschuh},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={309 1},
The glucocorticoid ciclesonide is the 2'R-epimer of 2'-cyclohexyl-11beta-hydroxy-21-isobutyryloxy-16bH-dioxolo[5',4':16,17]pregna-1,4-diene-3,20-dione. The active metabolite desisobutyryl-ciclesonide (des-CIC) is derived from ciclesonide by esterase cleavage of isobutyrate at the C21 position. The relative binding affinities at the rat glucocorticoid receptor were dexamethasone, 100; ciclesonide, 12; des-CIC, 1212; and budesonide, 905. Des-CIC potently inhibited the activation of murine and… CONTINUE READING


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