NEW MINERALOCORTICOIDS-5-ALPHA-DIHYDROALDOSTERONE AND 5-ALPHA-DIHYDRO-11-DEOXYCORTICOSTERONE

被引：18

作者：

SEKIHARA, H ^{[1
]}

ISLAND, DP ^{[1
]}

LIDDLE, GW ^{[1
]}

机构：

[1] VANDERBILT UNIV, SCH MED,DEPT MED, NASHVILLE, TN 37232 USA

来源：

ENDOCRINOLOGY | 1978年 / 103卷 / 04期

关键词：

D O I：

10.1210/endo-103-4-1450

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Mineralocorticoid activity of several Δ4- 3-ketosteroids and their 5α-dihydro analogs were evaluated by bioassay using urinary Na:K ratio of adrenalectomized rats as an index of mineralocorticoid activity. Among Δ4-3-ketosteroids, aldosterone, 11-deoxycorticosterone, corticosterone, cortisol, 11-dehydrocorticosterone, and cortisone showed mineralocorticoid activity with aldosterone, the most potent of the series, showing virtually maximum activity at a dose of 0.25 μg/rat. 5α- Dihydroaldosterone and 5α-dihydro-11-deoxycorticosterone possessed distinct mineralocorticoid activity, albeit less than aldosterone and 11-deoxycorticosterone. 5α-Dihydrocorticosterone, 5α -dihydrocortisol, 5α-dihydro- 11-dehydrocorticosterone, and 5α-dihydrocortisone did not show mineralocorticoid activity in doses up to 100 μg/rat. It is concluded that reduction of the 4, 5 double bond diminishes mineralocorticoid activity of Δ4-3-ketosteroids. Nevertheless, 5α-dihydroaldosterone has distinct mineralocorticoid activity with potency of 1.8% of that of aldosterone and approximately the same as that of 11-deoxycorticosterone. © 1978 by The Endocrine Society.

引用

页码：1450 / 1452

页数：3

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