• Corpus ID: 19367004

Mespirenone and other 15,16-methylene-17-spirolactones, a new type of steroidal aldosterone antagonists.

@article{Losert1986MespirenoneAO,
  title={Mespirenone and other 15,16-methylene-17-spirolactones, a new type of steroidal aldosterone antagonists.},
  author={Wolfgang Losert and Dieter Bittler and Maria Gordon Buse and Jorge Casals-stenzel and Martin Haberey and Henry Laurent and Klaus Nickisch and Ekkehardt Schillinger and Rudolf Prof. Dr. Wiechert},
  journal={Arzneimittel-Forschung},
  year={1986},
  volume={36 11},
  pages={
          1583-600
        }
}
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, glucocorticoid-treated rats. The standard procedure involved continuous i.v. infusion with an isotonic solution of low sodium content (0.05% NaCl + 5.2% glucose, 3 ml/rat/h) supplemented with d-aldosterone [1 micrograms/(kg X h)] resulting in a long-lasting reduction of renal sodium excretion, increase of renal… 
Effect of a new mineralocorticoid antagonist mespirenone on aldosterone-induced hypertension.
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In vivo administration of mespirenone to Sprague-Dawley rats effectively prevents the aldosterone-induced hypertension and reversed the hypertension caused by ald testosterone in a dose-dependent manner.
Pharmacokinetics and metabolism of mespirenone, a new aldosterone antagonist, in rat and cynomolgus monkey.
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The pharmacokinetics and metabolism of mespirenone were examined in rat and cynomolgus monkey using the tritiated drug and after oral administration the unchanged compound was not detectable; thus, mespire None has to be considered a pro-drug.
Steroidal spirooxetanes. I. Synthesis and antiandrogenic properties of some 17-spirooxetanoandrostanes
A large number of steroidal 17-spirolactones is known at the present time. The widely known antimineralocorticoid preparations spironolactone, spirorenone, and prorenone pertain to them [1, 2]. Less
Electrogenic Na+ transport in rat late distal colon by natural and synthetic glucocorticosteroids.
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The potency of in vitro-added corticosteroids to stimulate electrogenic Na+absorption and the need for high concentrations of the mineralocorticoid antagonist mespirenone to block this response indicated that J Na in a native mammalian epithelium can be mediated by the glucocortioid receptor.
Antimineralocorticoid 11beta-substituted spirolactones exhibit androgen receptor agonistic activity: a structure function study.
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It is demonstrated here that synthetic mineralocorticoid antagonists bearing hydrophobic C-11beta substituents and C-17gamma-lactone are potent hAR agonists in vitro.
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