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[Influence of the structure of synthetic gestagens on their binding to progesteron receptors in the endometrium].

Authors :
Kareva EN
Grinenko GS
Gasparian ND
Ovchinnikova EV
Gorenkova OS
Source :
Eksperimental'naia i klinicheskaia farmakologiia [Eksp Klin Farmakol] 2006 Jul-Aug; Vol. 69 (4), pp. 36-8.
Publication Year :
2006

Abstract

Chemical modification of progesterone molecule leads to changes both in the gestagenic activity of new derivatives and in their specific binding with progesterone receptors. The passage from esters (acetomepregenole, butagest) to the corresponding OH-forms such as 17a-acetoxy-3b-hydroxy-6-methyl-pregna-4,6-dien-20-one (ABMP)is accompanied by an increase in the binding with progesterone receptors in vitro. The translocation of a double bond from endocyclic (N6-N7) to exocyclic position (methylene group at N6 in ABMP) has no significant effect on the ability to binding with progesterone receptors.

Details

Language :
Russian
ISSN :
0869-2092
Volume :
69
Issue :
4
Database :
MEDLINE
Journal :
Eksperimental'naia i klinicheskaia farmakologiia
Publication Type :
Academic Journal
Accession number :
16995436