Difference of in vivo and in vitro antimineralocorticoid potency of progesterone.

Abstract:

:Progesterone (P) given intramuscularly increases renal sodium excretion. We tested the in vitro capacity of P to bind to the human mineralocorticoid receptor (MR) with a reticulocyte lysate system and Ps transactivation potency in transfected CV-1 cells. Progesterone binds with higher affinity to the MR than aldosterone, but shows only low transactivation activity. This results in a very strong anti-mineralocorticoid (MC) potency of P in vitro. To test the in vivo anti-MC potency of P we infused aldosterone intravenously to hypo-MC Addison's patients, followed by increasing P infusions. During the study we measured normal aldosterone plasma concentrations and high P concentrations similar to the third trimester of pregnancy. Despite the 1000-fold higher plasma P concentrations, the in vivo anti-MC effect of P (increase of urinary sodium/potassium ratio) was rather small. We suggest that this may be due to effective MR protection mechanisms, such as conversion of P to inactive metabolites.

journal_name

Endocr Res

journal_title

Endocrine research

authors

Quinkler M,Diederich S

doi

10.1081/erc-120016824

subject

Has Abstract

pub_date

2002-11-01 00:00:00

pages

465-70

issue

4

eissn

0743-5800

issn

1532-4206

journal_volume

28

pub_type

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