Gestrinone (R2323) Binding to Steroid Receptors in Human Uterine Endometrial Cytosol

@article{Tamaya1986GestrinoneB,
  title={Gestrinone (R2323) Binding to Steroid Receptors in Human Uterine Endometrial Cytosol},
  author={Teruhiko Tamaya and Jiro Fujimoto and Y. Watanabe and Keiko Arahori and Hiroji Okada},
  journal={Acta Obstetricia et Gynecologica Scandinavica},
  year={1986},
  volume={65}
}
To understand the mechanism of biological action of gestrinone (R2323), which has a therapeutic effect against endometriosis, the binding of gestrinone to numerous classes of intracellular steroid binding proteins was studied in the human uterine endometrium. Gestrinone bound to endometrial receptors for estrogen, progesterone and androgen, but seemed not to bind to endometrial intracellular corticosteroid‐binding globulin and sex hormone‐binding globulin. Gestrinone occupies all specific… Expand
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Tetrahydrogestrinone is a potent androgen and progestin.
TLDR
It is demonstrated that THG is a highly potent androgen and progestin in a yeast-based in vitro bioassay system expressing human androgens and progesterone receptors and has no estrogenic activity, antagonism for any of the three steroid receptor classes. Expand
Rationale for frequency and dose of administration in gestrinone therapy for pelvic endometriosis in the experimental model of rabbit uterus.
TLDR
Gestrinone dose of 60 micrograms (2.5 mg of clinical dose) every 3 days is considered to be effective for anti-steroid action in sex steroid receptor dynamics in the rabbit uterus, contributing to the rationale for gestrinone treatment of pelvic endometriosis. Expand
Multicentre study of gestrinone in cyclical breast pain FRIEDOLF PETERS
TLDR
Gestrinone was very effective in the treatment of cyclical mastalgia and was well tolerated and serum concentrations of oestradiol, progesterone, and tri-iodothyronine were significantly lower than baseline after 3 months of gestrinone. Expand
Medical Treatments for Endometriosis-Associated Pelvic Pain
TLDR
The first-line treatment for endometriosis associated pain is still represented by oral contraceptives used continuously, butgestins represent an acceptable alternative and norethisterone acetate at low dosage should be preferred. Expand
Preparation and Chromatographic Characterization of Tetrahydrogestrinone, a New “Designer” Anabolic Steroid
Tetrahydrogestrinone (THG, (17α)-13β-ethyl-17β-hydroxy-18,19-dinorpregna-4,9,11-trien-3-one, C21H28O2, 312 m.w.) is a synthetic 19-norsteroid closely related to gestrinone… Expand
Determination and excretion study of gestrinone in human urine by high performance liquid chromatography and gas chromatography/mass spectrometry.
TLDR
The reproducibility of the derivatization method was stable and recoveries were over 87% when spiked into blank urine. Expand
Designer Androgens in Sport: When Too Much Is Never Enough
The recent identification of tetrahydrogestrinone (THG), the first true "designer androgen," as a sports doping agent reflects both an alarmingly sophisticated illicit manufacturing facility and an… Expand
Treatment of pelvic endometriosis with gestrinone--report on 9 cases.
Nine patients with pelvic endometriosis were treated with gestrinone in a dose of 2.5 mg twice weekl- for 6 to 7 months. All patients became anovulator- with sporadic episodes of painless uterine… Expand
Determination of the metabolites of gestrinone in human urine by high performance liquid chromatography, liquid chromatography/mass spectrometry and gas chromatography/mass spectrometry.
TLDR
The trimethylsilyl (TMS)-enol-TMS ether derivative of gestrinone displayed three peaks in its GC/MS chromatogram, formed by tautomerism. Expand
History of Endometriosis : A 20 th-Century Disease
A reconstruction of the history of progress made in identifying, describing, and treating the condition we call endometriosis is neither simple nor easy because for almost 90 years endometriosis and… Expand
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