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达那唑与大鼠雄激素、糖皮质激素、孕激素及雌激素受体的结合:与生物活性的相关性。

Danazol binding to rat androgen, glucocorticoid, progesterone, and estrogen receptors: correlation with biologic activity.

作者信息

Barbieri R L, Lee H, Ryan K J

出版信息

Fertil Steril. 1979 Feb;31(2):182-6. doi: 10.1016/s0015-0282(16)43820-3.

DOI:10.1016/s0015-0282(16)43820-3
PMID:761680
Abstract

Danazol was found to possess androgenic and glucocorticoid activity in rat bioassays. In contrast, danazol displayed no significant estrogenic activity. In support of these findings, danazol bound to the 8 S androgen receptor of rat prostate cytosol and to the glucocorticoid receptor of rat liver cytosol, but danazol did not bind well to the estrogen receptor of the rat uterus. Finally, danazol bound to the progesterone receptor of the rat uterus, but controversy continues as the whether danazol possesses progestational, antiprogestational, or no progestational effects.

摘要

在大鼠生物测定中发现达那唑具有雄激素和糖皮质激素活性。相比之下,达那唑没有显著的雌激素活性。为支持这些发现,达那唑与大鼠前列腺细胞质的8S雄激素受体以及大鼠肝脏细胞质的糖皮质激素受体结合,但达那唑与大鼠子宫的雌激素受体结合不佳。最后,达那唑与大鼠子宫的孕激素受体结合,但关于达那唑是否具有孕激素、抗孕激素或无孕激素作用仍存在争议。

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1
Danazol binding to rat androgen, glucocorticoid, progesterone, and estrogen receptors: correlation with biologic activity.达那唑与大鼠雄激素、糖皮质激素、孕激素及雌激素受体的结合:与生物活性的相关性。
Fertil Steril. 1979 Feb;31(2):182-6. doi: 10.1016/s0015-0282(16)43820-3.
2
Danazol binding to steroid receptors in human uterine endometrium.达那唑与人子宫内膜中甾体受体的结合。
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Danazol binding and translocation of steroid receptors.达那唑与类固醇受体的结合及转位
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The interaction of human endometrial and myometrial steroid receptors with danazol.人子宫内膜和子宫肌层甾体受体与达那唑的相互作用。
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Evidence of a possible direct action of Danazol on the human ovary.达那唑对人类卵巢可能存在直接作用的证据。
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Danazol binds to progesterone receptors and inhibits the growth of human endometrial cancer cells in vitro.达那唑与孕酮受体结合,并在体外抑制人子宫内膜癌细胞的生长。
Am J Obstet Gynecol. 1986 Oct;155(4):857-61. doi: 10.1016/s0002-9378(86)80039-4.
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Nestorone: a progestin with a unique pharmacological profile.孕诺酮:一种具有独特药理学特性的孕激素。
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Mechanism of activation of steroid receptors: involvement of low molecular weight inhibitor in activation of androgen, glucocorticoid, and estrogen receptor systems.类固醇受体激活机制:低分子量抑制剂参与雄激素、糖皮质激素和雌激素受体系统的激活
Endocrinology. 1980 Apr;106(4):1142-8. doi: 10.1210/endo-106-4-1142.
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Cytoplasmic and nuclear estrogen binding capacity in the rat uterus during treatment with danazol and testosterone.达那唑和睾酮治疗期间大鼠子宫的细胞质和细胞核雌激素结合能力
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Progestin-like effects of danazol on rabbit uterus.达那唑对兔子宫的孕激素样作用。
Endocrinology. 1983 Mar;112(3):1110-4. doi: 10.1210/endo-112-3-1110.

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Effect of progestins, androgens, estrogens and antiestrogens on 3H-thymidine uptake by human endometrial and endosalpinx cells in vitro.孕激素、雄激素、雌激素及抗雌激素对人子宫内膜和输卵管内膜细胞体外摄取³H-胸腺嘧啶核苷的影响。
Arch Gynecol. 1987;240(4):225-32. doi: 10.1007/BF02134072.
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Endometriosis 1990. Current treatment approaches.子宫内膜异位症1990。当前的治疗方法。
Drugs. 1990 Apr;39(4):502-10. doi: 10.2165/00003495-199039040-00003.
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