| Literature DB >> 147913 |
F Di Carlo, G Conti, C Reboani.
Abstract
The inhibitory effect of some gestagens and calusterone on the binding of oestradiol-17beta to its specific uterine receptors has been investigated in intact rats. Progesterone, medrogestone, clogestone, medroxyprogesterone acetate and calusterone reduce the specific oestradiol-receptor interaction in vitro; this effect is dose-dependent and does not differ significantly from one drug to the other. A more relevant decrease in the amount of oestradiol-17beta bound to specific receptors has been observed with calusterone. Progesterone, clogestone, medrogestone, medroxyprogesterone acetate and calusterone given orally induce a marked decrease (between 30 and 70% depending on the dose) in the binding capacity of oestradiol-17beta to specific uterine receptors in vivo. Results from a Scatchard plot analysis suggest that the interference with the binding of oestradiol-17beta caused by both progestogens and calusterone is due to a non-competitive interaction.Entities:
Keywords: Animals, Laboratory; Biology; Clinical Research; Contraception; Contraceptive Agents, Female--side effects; Contraceptive Agents, Progestin--side effects; Contraceptive Agents--side effects; Endocrine System; Estradiol; Estrogens; Examinations And Diagnoses; Family Planning; Genitalia; Genitalia, Female; Hormone Receptors--analysis; Hormones; In Vitro; Laboratory Examinations And Diagnoses; Laboratory Procedures; Medroxyprogesterone Acetate--side effects; Membrane Proteins; Physiology; Progestational Hormones; Progesterone--side effects; Research Methodology; Urogenital System; Uterus
Mesh：
Substances：
Year: 1978 PMID： 147913 DOI： 10.1677/joe.0.0770049
Source DB: PubMed Journal: J Endocrinol ISSN： 0022-0795 Impact factor: 4.286