Interaction of the anti-estrogen CI-628 and estradiol on plasma LH and hypothalamic LH-RH in the female rat
Interaction of the anti-estrogen CI-628 and estradiol on plasma LH and hypothalamic LH-RH in the female rat
复制标题
抗雌激素 CI-628 和雌二醇对雌性大鼠血浆 LH 和下丘脑 LH-RH 的相互作用
DOI：
10.1016/0006-8993(80)90590-9
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发表时间：
1980
期刊：
影响因子：
2.9
通讯作者：
C. Kordon
中科院分区：
文献类型：
--
作者：
F. Gogan;W. Rotsztejn;L. Couturier;G. Chazal;I. Beattie;C. Kordon
在切除卵巢或植入雌二醇（E2）的大鼠中，测试了抗雌激素CI-628对血浆LH和下丘脑LH-RH含量的影响，以将这些参数与下丘脑和垂体中的[3 H] E2滞留相关联。增加剂量的CI-628诱导剂量依赖性抑制[3 H] E2滞留在细胞质和核组分的垂体。相反，[3 H] E2的下丘脑保留仅在较高剂量的CI-628（2.4和24 mg/kg）下才被显著抑制。在卵巢切除大鼠中，仅高剂量的CI-628（24 mg/kg）能够降低去势后观察到的升高的LH水平。在E2存在下，CI-628对LH分泌具有雌激素和抗雌激素性质。CI-628作用于垂体水平，降低组织对LH-RH的敏感性，但对下丘脑内侧基底（MBH）LH-RH含量无影响。
The effects of the anti-estrogen CI-628 have been tested on both plasma LH and hypothalamic LH-RH content in ovariectomized or ovariectomized, estradiol (E2)-implanted rats, in order to correlate those parameters with the [3H]E2retention in the hypothalamus and the pituitary. Increasing doses of CI-628 induced a dose-dependent inhibition of [3H]E2retention in both cytosolic and nuclear fractions of the pituitary. In contrast, hypothalamic retention of [3H]E2is only inhibited significantly with higher doses of CI-628 (2.4 and 24 mg/kg). In ovariectomized rats, only a high dose of CI-628 (24 mg/kg) is able to decrease elevated LH levels observed following castration. In the presence of E2, CI-628 has both estrogenic and anti-estrogenic properties on LH secretion. CI-628 acts at the pituitary level to decrease the tissue sensitivity to LH-RH, but has no effect on mediobasal hypothalamic (MBH) LH-RH content.