Budesonide-d8

Budesonide-d₈ is intended for use as an internal standard for the quantification of budesonide by GC- or LC-MS. 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.

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.Millan, D.S., Ballard, S.A., Chunn, S., et al.Design and synthesis of long acting inhaled corticosteroids for the treatment of asthmaBioorg. Med. Chem. Lett.21(19)5826-5830(2011) 3.Birrell, M.A., Hardaker, E., Wong, S., et al.IκB kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthmaAm. J. Respir. Crit. Care Med.172(8)962-971(2005) 4.EkstrÖm, G.M.Oxazolone-induced colitis in rats: effects of budesonide, cyclosporin A, and 5-aminosalicylic acidScand. J. Gastroenterol.33(2)174-179(1998)