Prednisolone-d7

Prednisolone-d₇ is intended for use as an internal standard for the quantification of prednisolone 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 and prednisone .^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.

References:
[1].Frey, B.M., Seeberger, M., and Frey, F.J.Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejectionTransplantation39(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 activityJ. 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 propertiesEur. J. Endocrinol.151(3)397-406(2004).