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一种新型抗炎甾体药物:20-二氢泼尼松龙甲酯的全身活性

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

作者信息

Lee H J, Nathoo Z M

出版信息

Steroids. 1983 May;41(5):609-15. doi: 10.1016/0039-128x(83)90026-0.

Abstract

The systemic activities of methyl 20-dihydroprednisolonate (1), a new local anti-inflammatory steroid synthesized by modifying the 17 beta-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 dose-related 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.

摘要

通过修饰泼尼松龙的17β - 酮醇侧链合成的新型局部抗炎甾体20 - 二氢泼尼松龙甲酯(1)对大鼠垂体 - 肾上腺功能和肝糖原含量的全身活性进行了研究。母化合物泼尼松龙经肌肉注射给药后,大鼠血浆皮质酮、促肾上腺皮质激素(ACTH)水平及肝糖原含量均出现显著的剂量相关下降。相比之下,20 - 二氢泼尼松龙甲酯仅在高剂量时才引起轻度的垂体 - 肾上腺抑制和肝糖原消耗。与泼尼松龙不同,该甾体酸酯在肾上腺切除的大鼠中不具有糖原生成活性。

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