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Budesonide is a glucocorticoid and an agonist of glucocorticoid receptors (EC50 = 45.7 pM in a transactivation assay).1 It is selective for glucocorticoid over mineralocorticoid receptors (EC50 = 7,620 pM). Budesonide inhibits LPS-induced TNF-α release from human peripheral blood mononuclear cells (PBMCs; IC50 = 0.96 nM).2 It reduces levels of IL-1β and eotaxin in the lungs and the number of eosinophils and neutrophils in bronchoalveolar lavage fluid (BALF) in a rat model of ovalbumin-induced airway inflammation when administered at a dose of 3 mg/kg.3 Intracolonic administration of budesonide decreases colon wet weight and colonic myeloperoxidase (MPO) activity in a rat model of oxazolone-induced colitis.4 Formulations containing budesonide have been used in the treatment of Crohn's disease, ulcerative colitis, allergic rhinitis, and asthma.
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1. Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-
2. Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma. Bioorg. Med. Chem. Lett. 21(19), 5826-5830 (2011).
3. IκB kinase-
4. Oxazolone-