Systemic activities of a new anti-inflammatory steroid: Methyl 20-dihydroprednisolonate

The systemic activities of methyl 20-dihydroprednisolonate (1), a new local anti-inflammatory steroid synthesized by modifying the 17β-ketol side-chain of prednisolone, on pituitary-adrenal function and liver glycogen content were investigated in rats. The parent compound, prednisolone, administered intramuscularly, caused a significant doserelated decrease in plasma levels of corticosterone, adrenocorticotropic hormone (ACTH), and liver glycogen content in rats. In contrast, methyl 20-dihydroprednisolonate caused mild PA suppression and liver glycogen depletion only at high doses. The steroid acid ester did not exert glycogenic activity, unlike prednisolone, in the adrenalectomized rats.