Background:

Prednisolone is a glucocorticoid with the general properties of the corticosteroids.Target: Glucocorticoid ReceptorPrednisolone is a glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. Prednisolone, 5 or 50 mg/kg, was administered intravenously to adrenalectomized rats. Total plasma, free plasma, CBG-free plasma, and liver prednisolone concentrations were measured simultaneously with free hepatic cytosolic glucocorticoid receptor concentrations and tyrosine aminotransferase (TAT) activity of the liver as a function of time. prednisolone pharmacokinetics were dose-dependent, parameters describing receptor kinetics and TAT activity were constant at each prednisolone dose. The major determinants of receptor-mediated glucocorticoid activity are confirmed to be the availability of the receptor, drug-receptor dissociation rate, and corticosteroid persistence in the biophase [1, 2].

参考文献:
[1]. Boudinot, F.D., R. D'Ambrosio, and W.J. Jusko, Receptor-mediated pharmacodynamics of prednisolone in the rat. J Pharmacokinet Biopharm, 1986. 14(5): p. 469-93.
[2]. Czock, D., et al., Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clinical pharmacokinetics, 2005. 44(1): p. 61-98.