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7α-卤代取代对皮质类固醇活性的选择性影响:Sch 22219和Sch 23409。

Selective effects of 7 alpha-halogeno substitution on corticosteroid activity: Sch 22219 and Sch 23409.

作者信息

Lutsky B N, Berkenkopf J, Fernandez X, Monahan M, Watnick A S

出版信息

Arzneimittelforschung. 1979;29(7):992-8.

PMID:583002
Abstract

Two 7 alpha-halogeno substituted corticosteroids, 7 alpha-chloro-16 alpha-methylprednisolone-17,21 dipropionate (Sch 22219) and 7 alpha-bromo-16 alpha-methylprednisolone-17-benzoate-21-acetate (Sch 23409) were compared to other clinically utilized topical corticosteroids for local and parenteral antiinflammatory and glucocorticosteroid activity. Both compounds were at least equivalent to the most potent comparison corticosteroids in topical antiinflammatory activity, and exhibited favorable ratios of local to systemic effects. In mice, Sch 22219 showed a greater dissociation of antiinflammatory activity from side effects than Sch 23409, although the reverse was true in rats. On the basis of the data available, both compounds possess enhanced topical antiinflammatory potency, with the potential for reduced side effects in man.

摘要

将两种7α-卤代取代的皮质类固醇,即7α-氯-16α-甲基泼尼松龙-17,21-二丙酸酯(Sch 22219)和7α-溴-16α-甲基泼尼松龙-17-苯甲酸酯-21-乙酸酯(Sch 23409)与其他临床使用的局部皮质类固醇进行比较,以评估其局部和全身抗炎及糖皮质激素活性。这两种化合物在局部抗炎活性方面至少与最有效的对照皮质类固醇相当,并且表现出有利的局部与全身效应比。在小鼠中,Sch 22219显示出抗炎活性与副作用的解离程度比Sch 23409更大,尽管在大鼠中情况相反。根据现有数据,这两种化合物均具有增强的局部抗炎效力,且在人体中有可能减少副作用。

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Development of glucocorticosteroids with enhanced ratio between topical and systemic effects.
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