Anti-inflammatory effect of theophylline in rats and its involvement of the glucocorticoid-glucocorticoid receptor system

Shigekazu Watanabe, Jun Yamakami, Masao Tsuchiya, Tomoko Terajima, Junko Kizu, Seiji Hori

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Although theophylline has been suggested to have an anti-inflammatory effect, there have been few reports to show the in vivo effect and the mechanism of anti-inflammatory activity of theophylline experimentally. To reveal the anti-inflammatory activity of theophylline, we studied the effect of theophylline and its metabolites on carrageenan-induced edema in rat foot pad. Subcutaneous injection of theophylline (5-100 mg/kg) inhibited carrageenan-induced edema dose-dependently. Theophylline metabolites, that is, 1-methylxanthine, 3-methylxanthine, 1-methyluric acid, and 1,3-dimethyluric acid (equimolar dose to 50 mg/kg of theophylline), did not inhibit the edema significantly. The inhibitory effect of theophylline on carrageenan-induced edema disappeared by pretreatment with aminoglutethimide, an inhibitor of glucocorticoid synthesis and with mefepristone, an antagonist of the glucocorticoid receptor. These results suggest that theophylline itself has anti-inflammatory activity and the glucocorticoid-glucocorticoid receptor system is involved in the anti-inflammatory activity of theophylline.

Original languageEnglish
Pages (from-to)566-570
Number of pages5
JournalJournal of Pharmacological Sciences
Issue number4
Publication statusPublished - 2008 Apr 24



  • Anti-inflammation
  • Carrageenan
  • Glucocorticoid
  • Theophylline

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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