Interaction of [3H]nomegestrol acetate with cytosolic progesterone receptors from the rat uterus.
Steroids
; 56(6): 325-8, 1991 Jun.
Article
in En
| MEDLINE
| ID: mdl-1926229
ABSTRACT
The binding characteristics of the progestin 17 alpha-acetoxy-6-methyl-19-[3H]norpregna-4,6-diene-3,20-dione, nomegestrol acetate ([3H]NOM-Ac) to progesterone receptors (PgRs) of uterus were determined in the rat. Scatchard plot analysis of the equilibrium binding data showed that [3H]NOM-Ac binds to uterine PgR with a Kd of 5.44 +/- 1.27 nM and a Bmax of 1.51 +/- 0.11 pmol/mg protein. Analysis of dissociation kinetics showed that [3H]NOM-Ac dissociates slowly from the PgR, k - 1 = 4.9 +/- 0.5 10(-5) s-1. Competition experiments against [3H]NOM-Ac showed the specificity of the binding with a sequence in relative affinity as follows ORG 2058 greater than P greater than NOM-Ac greater than medroxyprogesterone acetate greater than megestrol acetate greater than cyproterone acetone greater than NOM.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Uterus
/
Receptors, Progesterone
/
Cytosol
/
Progesterone Congeners
/
Megestrol
/
Norpregnadienes
Limits:
Animals
Language:
En
Journal:
Steroids
Year:
1991
Document type:
Article