抗雌激素CI - 628与雌二醇对雌性大鼠血浆促黄体生成素及下丘脑促性腺激素释放激素的相互作用。

Interaction of the anti-estrogen CI-628 and estradiol on plasma LH and hypothalamic LH-RH in the female rat.

作者信息

Gogan F, Rotsztejn W H, Couturier L, Chazal G, Beattie I, Kordon C

出版信息

Brain Res. 1980 Feb 17;184(1):109-18. doi: 10.1016/0006-8993(80)90590-9.

Abstract

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]E2 retention in the hypothalamus and the pituitary. Incresing doses of CI-628 induced a dose-dependent inhibition of [3H]E2 retention in both cytosolic and nuclear fractions of the pituitary. In contrast, hypothalamic retention of [3H]E2 is 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.

摘要

已对去卵巢大鼠或去卵巢并植入雌二醇（E2）的大鼠，检测了抗雌激素Ci-628对血浆促黄体激素（LH）和下丘脑促性腺激素释放激素（LH-RH）含量的影响，以便将这些参数与下丘脑和垂体中[3H]E2的潴留情况相关联。Ci-628剂量增加时，垂体胞质和核部分中[3H]E2的潴留呈剂量依赖性抑制。相反，仅在更高剂量的Ci-628（2.4和24mg/kg）作用下，下丘脑[3H]E2的潴留才受到显著抑制。在去卵巢大鼠中，只有高剂量的Ci-628（24mg/kg）能够降低去势后升高的LH水平。在有E2存在的情况下，Ci-628对LH分泌具有雌激素和抗雌激素特性。Ci-628作用于垂体水平，降低组织对LH-RH的敏感性，但对下丘脑中间基底部（MBH）的LH-RH含量没有影响。