Related Experiment Video

Updated: Oct 2, 2026

Performing Vaginal Lavage, Crystal Violet Staining, and Vaginal Cytological Evaluation for Mouse Estrous Cycle Staging Identification
09:01

Performing Vaginal Lavage, Crystal Violet Staining, and Vaginal Cytological Evaluation for Mouse Estrous Cycle Staging Identification

Published on: September 15, 2012

Interference of gestagens and androgens with rat uterine oestrogen receptors

F Di Carlo, G Conti, C Reboani

    The Journal of Endocrinology
    |April 1, 1978
    PubMed

    Insights

    Gestagens and calusterone inhibit oestradiol-17beta binding to uterine receptors. This non-competitive interaction occurs both in vitro and in vivo, with calusterone showing a notable effect.

    Area of Science:

    • Endocrinology
    • Pharmacology
    • Molecular Biology

    Background:

    • Oestradiol-17beta is a key hormone regulating reproductive functions.
    • Gestagens are synthetic or natural steroids that mimic progesterone's effects.
    • Understanding steroid-receptor interactions is crucial for reproductive health and drug development.

    Purpose of the Study:

    • To investigate the inhibitory effects of specific gestagens and calusterone on oestradiol-17beta binding to uterine receptors.
    • To compare the efficacy of different gestagens and calusterone in blocking oestradiol-17beta receptor interaction.
    • To elucidate the mechanism of interaction between these compounds and oestradiol-17beta receptors.

    Main Methods:

    • In vitro and in vivo experiments using intact rats.
    • Assessing the binding of oestradiol-17beta to specific uterine receptors.
    • Dose-response analysis and Scatchard plot analysis to determine interaction type.

    Main Results:

    • Progesterone, medrogestone, clogestone, medroxyprogesterone acetate, and calusterone all reduced oestradiol-17beta-receptor binding in a dose-dependent manner.
    • Calusterone exhibited a more significant decrease in binding compared to other gestagens.
    • Oral administration of these compounds in vivo resulted in a 30-70% decrease in oestradiol-17beta binding capacity.
    • Scatchard plot analysis indicated a non-competitive interaction mechanism.

    Conclusions:

    • Gestagens and calusterone effectively inhibit oestradiol-17beta binding to uterine receptors.
    • The observed inhibition is mediated through a non-competitive interaction.
    • These findings have implications for understanding hormonal regulation and potential therapeutic interventions.
    Keywords:
    Animals, LaboratoryBiologyClinical ResearchContraceptionContraceptive Agents, Female--side effectsContraceptive Agents, Progestin--side effectsContraceptive Agents--side effectsEndocrine SystemEstradiolEstrogensExaminations And DiagnosesFamily PlanningGenitaliaGenitalia, FemaleHormone Receptors--analysisHormonesIn VitroLaboratory Examinations And DiagnosesLaboratory ProceduresMedroxyprogesterone Acetate--side effectsMembrane ProteinsPhysiologyProgestational HormonesProgesterone--side effectsResearch MethodologyUrogenital SystemUterus

    More Related Videos

    Ultrasonography in Experimental Reproductive Investigations on Rats07:59

    Ultrasonography in Experimental Reproductive Investigations on Rats

    Published on: December 2, 2017

    Establishment of Rat Models Mimicking Gender-affirming Hormone Therapies06:24

    Establishment of Rat Models Mimicking Gender-affirming Hormone Therapies

    Published on: January 10, 2025

    Related Concept Videos

    Oogenesis02:07

    Oogenesis

    In human women, oogenesis produces one mature egg cell or ovum for every precursor cell that enters meiosis. This process differs in two unique ways from the equivalent procedure of spermatogenesis in males. First, meiotic divisions during oogenesis are asymmetric, meaning that a large oocyte (containing most of the cytoplasm) and minor polar body are produced as a result of meiosis I, and again following meiosis II. Since only oocytes will go on to form embryos if fertilized, this unequal...
    Teratogenicity01:07

    Teratogenicity

    The ability of a drug to produce structural deformations and functional abnormalities in the developing embryo or the fetus is called teratogenicity, and the drug producing this effect is known as a teratogen. Teratogenic effects include stillbirth, miscarriage, intrauterine growth restriction, and neurocognitive delay. A teratogen may affect the embryo at different stages of development, which is important in determining the type and extent of the damage. During blastocyst formation, the early...
    Hormonal Regulation of the Menstrual Cycle01:22

    Hormonal Regulation of the Menstrual Cycle

    The ovarian cycle regulates endometrial changes throughout a single menstrual cycle via the coordinated action of gonadotrophin-releasing hormone (GnRH) and gonadotrophins.
    At puberty, GnRH begins a pulsatile release pattern, which triggers the anterior pituitary gland to secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH). The frequency and amplitude of GnRH pulses vary across the menstrual cycle, with faster pulses favoring LH release and slower pulses favoring FSH release.
    Hormonal Control of the Ovarian Cycle01:30

    Hormonal Control of the Ovarian Cycle

    The ovarian cycle is meticulously regulated by the hypothalamic-pituitary-gonadal axis. This cycle orchestrates the release of a mature oocyte, essential for reproduction.
    Before puberty, the hypothalamus releases GnRH in a low frequency, low amplitude pulsatile manner. This along with the immature hypothalamic-pituitary-gonadal axis activity, results in low estrogen levels and the absence of a fully functional ovarian cycle.  At puberty, GnRH secretion increases in both frequency and...