MolPharm

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Vicent, G. P.
Right arrow Articles by Galigniana, M. D.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Vicent, G. P.
Right arrow Articles by Galigniana, M. D.

0026-895X/97/040749-05$3.00/0
Copyright © by The American Society for Pharmacology and Experimental Therapeutics
All rights of reproduction in any form reserved.
MOLECULAR PHARMACOLOGY 52:749-753 (1997).

21-Hydroxy-6,19-oxidoprogesterone: A Novel Synthetic Steroid with Specific Antiglucocorticoid Properties in the Rat

G. P. Vicent, M. C. Monteserín, A. S. Veleiro, G. Burton, C. P. Lantos, and M. D. Galigniana1

Departamentos de Química Biológica (G.P.V., C.P.L., M.D.G) and Química Orgánica (M.C.M., A.S.V., G.B.), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires and PRHOM-Consejo Nacional de Investigaciones Científicas y Técnicas (G.P.V., C.P.L., M.D.G.), Ciudad Universitaria, (1428) Buenos Aires, Argentina

In the rat, the conformationally highly bent steroid 21-hydroxy-6,19-oxidoprogesterone efficiently displaces [3H]corticosterone from thymus-glucocorticoid receptors and blocks type II receptors in kidney cytosols but competes with neither [3H]aldosterone for kidney-mineralocorticoid receptors nor [3H]progesterone for uterus-progesterone receptors. It evokes Na+ retention only at very high doses (~100 µg/100 g of rat weight) and is unable to induce tyrosine aminotransferase or to increase glycogen deposits in rat liver. When coincubated with corticosterone or dexamethasone, 2.5 µM 21OH-6OP inhibits 80% of tyrosine aminotransferase induction. It may therefore be used experimentally as an antiglucocorticoid virtually lacking mineralocorticoid or glucocorticoid properties as well as affinity for mineralocorticoid or progesterone receptors.

Copyright © by The American Society for Pharmacology and Experimental Therapeutics


This article has been cited by other articles:


Home page
 J Mol EndocrinolHome page
J. Zhang, F. T F Tsai, and D. S Geller
Differential interaction of RU486 with the progesterone and glucocorticoid receptors.
J. Mol. Endocrinol., August 1, 2006; 37(1): 163 - 173.
[Abstract] [Full Text] [PDF]

Home page
 J. Clin. Endocrinol. Metab.Home page
F. A. Patel, J. W. Funder, and J. R. G. Challis
Mechanism of Cortisol/Progesterone Antagonism in the Regulation of 15-Hydroxyprostaglandin Dehydrogenase Activity and Messenger Ribonucleic Acid Levels in Human Chorion and Placental Trophoblast Cells at Term
J. Clin. Endocrinol. Metab., June 1, 2003; 88(6): 2922 - 2933.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
M. D. Galigniana, G. P. Vicent, G. Piwien-Pilipuk, G. Burton, and C. P. Lantos
Mechanism of Action of the Potent Sodium-Retaining Steroid 11,19-Oxidoprogesterone
Mol. Pharmacol., July 1, 2000; 58(1): 58 - 70.
[Abstract] [Full Text]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1997 by the American Society for Pharmacology and Experimental Therapeutics