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Mespirenone and other 15,16-methylene-17-spirolactones, a new type of steroidal aldosterone antagonists.
The ability of a series of 15,16-methylene-spirolactones in comparison to known antimineralocorticoids to inhibit the renal actions of aldosterone was tested in adrenalectomized, glucocortioid-treated rats to obtain preliminary information on potential antiandrogenic and progestogenic (side-)effects.
New biologically active pregnan-21-oic acid esters.
Several pregnan-21-oic acid esters possess the unique activity that they are topical anti-inflammatory agents with no side effects and even when administered at high dosages, the usual systemic activity associated with corticosteroid treatment could not be observed.
Prodrugs of Gestodene for Matrix-Type Transdermal Drug Delivery Systems
Designing prodrugs to the requirements of matrix TDDS is an efficient way of enhancing the transdermal drug flux rate.
Development of Progestogens
The development of progestogens is one of the most fascinating chapters in the history of steroid chemistry and biology. When in 1934 the structure of progesterone was elucidated [1], no one could
Synthesis and activities of anti-aldosterones.
The bis-methylene derivative was found to reverse the strong depression of the urinary Na/K ratio induced by the mineralocorticoid effect of aldosterone in a dose-dependent manner and had more than five times the potency of spironolactone.
Aldosterone antagonists. 2. New 7 alpha-(acetylthio)-15,16-methylene spirolactones.
In animal studies mespirenone exhibited a threefold-greater antialdosterone potency and less than 10% of the antiandrogenic activity of spironolactone.
Aldosterone antagonists. 1. Synthesis and activities of 6 beta,7 beta:15 beta,16 beta-dimethylene steroidal spirolactones.
The 1 alpha,2 alpha-methylene derivative 20 has a similar aldosterone antagonistic potency compared to that of spirorenone but does not show decreased endocrinological side effects, while other substituents as in compounds 4-11, 15-19, and 21 sharply decreased the ald testosterone antagonistic activity of 2 or 3, respectively.