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[Influence of the structure of synthetic gestagens on their binding to progesteron receptors in the endometrium].
- 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.
- Subjects :
- 17-alpha-Hydroxyprogesterone analogs & derivatives
17-alpha-Hydroxyprogesterone chemistry
17-alpha-Hydroxyprogesterone metabolism
Adult
Endometrial Hyperplasia metabolism
Endometrial Hyperplasia prevention & control
Female
Humans
Hydroxyprogesterones chemistry
Hydroxyprogesterones metabolism
Middle Aged
Pregnadienediols chemistry
Pregnadienediols metabolism
Pregnenes chemistry
Pregnenes metabolism
Progesterone Congeners chemistry
Progestins chemistry
Structure-Activity Relationship
Endometrium metabolism
Progesterone Congeners metabolism
Progestins metabolism
Receptors, Progesterone metabolism
Subjects
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