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Endocrinology, Vol 104, 1352-1356, Copyright © 1979 by Endocrine Society


ARTICLES

The mineralocorticoid antagonist activity of an 11 beta,18- oxidopregnane

S Ulick, D Marver, WR Adam and JW Funder

Removal of the 18-hydroxy group of the hemiacetal form of aldosterone transforms its activity from that of pure agonist to predominant antagonist. The 18-deoxy derivative possesses one third of the binding affinity of aldosterone for the cytoplasmic mineralocorticoid receptor of rat kidney and exhibits an approximate 2:1 antagonist to agonist ratio in both toad bladder and adrenalectomized rat bioassay systems. The promising properties of the 11 beta,18-oxidopregnane tested included very low androgen receptor affinity and approximately equal effectiveness in vitro and in vivo in displacing aldosterone from mineralocorticoid-binding sites in the rat.





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Copyright © 1979 by The Endocrine Society