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

Abstract:

: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.

journal_name

Endocrinology

journal_title

Endocrinology

authors

Ulick S,Marver D,Adam WR,Funder JW

doi

10.1210/endo-104-5-1352

subject

Has Abstract

pub_date

1979-05-01 00:00:00

pages

1352-6

issue

5

eissn

0013-7227

issn

1945-7170

journal_volume

104

pub_type

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