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N-丙基20-表二氢泼尼松龙酰胺差向异构体的抗炎活性

Anti-inflammatory activity of the epimers of N-propyl 20 xi-dihydroprednisolonamide.

作者信息

Lee J W, Kim H P, Bird J, Lee H J

出版信息

Steroids. 1984 Dec;44(6):511-8. doi: 10.1016/s0039-128x(84)80032-x.

Abstract

The epimers of a steroid carboxamide, N-propyl 20 alpha- and 20 beta -dihydroprednisolonamide, were evaluated for their local and systemic effects on granuloma formation, pituitary-adrenal function and liver glycogen content in rats. When the carboxamides were administered locally, the 20 beta-epimer exhibited greater activity than the 20 alpha-epimer in suppressing cotton pellet granuloma formation. Neither epimer had suppressive effects on thymus weight and plasma corticosterone levels at the dose level used. When the carboxamides were administered systemically, they were pharmacologically inactive. Furthermore, in acute pharmacological studies, the carboxamides neither increased tyrosine aminotransferase activity and glycogen deposition in the liver nor decreased plasma corticosterone levels and relative thymus weight.

摘要

对一种甾体羧酰胺(N-丙基20α-和20β-二氢泼尼松龙酰胺)的差向异构体进行了评估,以研究它们对大鼠肉芽肿形成、垂体-肾上腺功能及肝糖原含量的局部和全身影响。当局部给予羧酰胺时,在抑制棉球肉芽肿形成方面,20β-差向异构体比20α-差向异构体表现出更强的活性。在所使用的剂量水平下,两种差向异构体对胸腺重量和血浆皮质酮水平均无抑制作用。当全身给予羧酰胺时,它们在药理上无活性。此外,在急性药理学研究中,羧酰胺既未增加肝脏中酪氨酸转氨酶活性和糖原沉积,也未降低血浆皮质酮水平及相对胸腺重量。

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