Prednisolone-d₇

Prednisolone-d₇ is intended for use as an internal standard for the quantification of prednisolone (Item No. 20866) by GC- or LC-MS. Prednisolone is a glucocorticoid and mineralocorticoid receptor agonist and an active metabolite of the prodrugs and synthetic glucocorticoids prednisolone phosphate (Item No. 15933) and prednisone (Item No. 20677).^1,2,3 It selectively binds to the glucocorticoid and mineralocorticoid receptors over the progesterone, androgen, and estrogen receptors (K_is = 2.4, 37, >5,000, 2,762, and >1,000 nM, respectively) and induces transactivation in reporter assays using CV-1 cells expressing the human glucocorticoid receptor or human mineralocorticoid receptor (EC₅₀s = 6.9 and 3.78 nM, respectively).^2,3 Prednisolone reduces pulmonary eosinophil infiltration in a rat model of sephadex-induced asthma (ED₅₀ = 1.2 mg/kg).² Formulations containing prednisolone have been used as anti-inflammatory or immunosuppressive agents.

WARNING This product is not for human or veterinary use.

1. Frey, B.M., Seeberger, M., and Frey, F.J. Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejection. Transplantation 39(3), 270-274 (1985).

2. Coghlan, M.J., Kym, P.R., Elmore, S.W., et al. Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: Selective quinoline derivatives with prednisolone-equivalent functional activity. J. Med. Chem. 44(18), 2879-2885 (2001).

3. 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 properties. Eur. J. Endocrinol. 151(3), 397-406 (2004).