• Corpus ID: 19367004

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

  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},
  volume={36 11},
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.
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.
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.
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.
It is demonstrated here that synthetic mineralocorticoid antagonists bearing hydrophobic C-11beta substituents and C-17gamma-lactone are potent hAR agonists in vitro.