Epithioandrostanol (10275-S), an Estrogen Antagonist
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概要
- 論文の詳細を見る
2α, 3α-Epithio-5α-androstan-17β-ol (10275-S) has been known to possess a potent and long-acting anti-estrogenic activity in rodents. In this experiment, 1.25mg 10275-S injected once subcutaneously into the ovariectomized and estradiol-treated mice caused a complete block of vaginal cornification for 24.3 days in spite of the successive treatment with estrogen. Pre-treatment with 10275-S in ovariectomized mice either 4 or 24 hr before tritiated estradiol injection caused significant inhibition of accumulation of radioactivity in the uterus. Pre-incubation of uterine cytosol from immature rat with 10275-S competitively suppressed the formation of estradiol-macromolecule complex maximally around the 8S region, and 50% suppression was obtained at 4.4×10<SUP>-7</SUP><I>M</I>, about 70-fold over the estradiol. Under the same conditions, 10<SUP>-5</SUP><I>M</I> progesterone or testosterone gave no effect on estradiol binding at the 8S region. The relation of these <I>in vitro</I> results to the <I>in vivo</I> activities of this steroid was discussed.
- 社団法人 日本内分泌学会の論文
著者
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MIYAKE TAMOTSU
Shionogi Research Laboratory, Shionogi & Co., Ltd.
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HORI TAKASHI
Shionogi Research Laboratory, Shionogi and Co., Ltd.
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SUZUKI TETSURO
Shionogi Research Laboratory, Shionogi & Co., Ltd.
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HORI TAKASHI
Shionogi Research Laboratory, Shionogi & Co., Ltd.
関連論文
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- Further Studies on the Luteotropic Action of Estrogen in Rats
- Effects of Exogenous Progesterone on the Ovarian Progestin Secretion and Plasma LH and Prolactin Levels in Cyclic Rats
- Effects of Estradiol, Dietary Cholesterol and 1-Thyroxine on Biliary Bile Acid Composition and Secretory Rate, and on Plasma, Liver and Bile Cholesterol Levels in Rats
- Further Studies on the Effect of Exogenous Progesterone and Related Compounds on the Preovulatory Progesterone Secretion in the Rat
- Luteotrophic Action of Estrogen and Prolactin in Rats
- Relationship between Ovarian Progestin Secretion and Corpora Lutea Function in Pregnat Rats
- Acute Effects of Various Gonadotropins and Other Pituitary Hormones on Preovulatory Ovarian Progestin Secretion in Hypophysectomized Rats
- Ovarian Secretion of Progesterone and 20α-Hydroxypregn-4-en-3-one during Rat Estrous Cycle in Chronological Relation to Pituitary Release of Luteinizing Hormone
- Biphasic Effect of Estrogen on Rat Plasma Cholesterol Level and its Interaction by Androgen
- Effect of Exogenous Progesterone on the Preovulatory Progesterone Secretion in the Rat
- THE ESTROGEN-STIMULATION OF MAMMARY GROWTH IN OVARIECTOMIZED IMMATURE MICE AND THEIR INHIBITION BY STEROIDS
- Acute Effects of Ovarian Steroids upon Follicular Growth in the Cycling Rat
- Relation between Estrogen Secretion and Follicular Morphology in the Rat Ovary under the Influence of Ovulating Hormone or Exogenous Gonadotropins
- Pituitary Regulation of Preovulatory Estrogen Secretion in the Rat
- OVARIAN ESTROGEN SECRETION DURING THE ESTROUS CYCLE AND UNDER THE INFLUENCE OF EXOGENOUS CONADOTROPINS IN RATS
- 2α, 3α-EPITHIO-5α-ANDROSTAN-17β-YL 1-METHOXY CYCLOPENTYL ETHER (10364-S), A NEW ORALLY ACTIVE ANABOLIC-ANDROGENIC STEROID
- Acute Effect of Hypothalamic Deafferentation on Progesterone-Induced Ovulating Hormone Release in the Rats
- Induction of Delayed or Advanced Ovulation by Estrogen in 4-Day Cyclic Rat
- THE USE OF IN VIVO VAGINAL TTC REDUCTION OF SPAYED MICE FOR THE STUDY OF MODE OF ACTION OF ANTI-ESTROGENS
- Facilitation of Luteinizing Hormone Release by Progesterone in Proestrous Rats
- Delayed Implantation Induced by Anti-Estrogenic Compounds in Rats
- Epithioandrostanol (10275-S), an Estrogen Antagonist