兔子宫中雌三醇特异性结合位点产生抗雌激素作用的可能性。

Possibility of anti-estrogen action from estriol specific binding sites in rabbit uterus.

Tamaya T, Kawabata I, Wada K, Iida K, Imai A

Department of Obstetrics and Gynecology, Gifu University School of Medicine, Japan.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1990;96(2):241-4.

Abstract

This study was designed to investigate the clomiphene or tamoxifen binding to receptor sites for estradiol-17 beta (E2R) and estriol (E3R) in the rabbit uterus. 2. Those so-called anti-estrogenic compounds tended to inhibit E2-E2R and E3-E3R bindings equally. 3. The inhibitor constant of clomiphene for E2R was approximately 3.8 x 10(-8) M at 4 degrees C and that for E3R approximately 1.8 x 10(-8) M at 4 degrees C in a given case, determined by charcoal assay. 4. It is suggested that the anti-estrogenic compounds demonstrate their effects after binding either to E2R or to E3R. 5. There were some tissue differences of the contents between E2R and E3R. For example, the uterus and the cortex contained E2R, and the pituitary E3R more than the other.

摘要

本研究旨在探讨氯米芬或他莫昔芬与兔子宫中雌二醇-17β（E2R）和雌三醇（E3R）受体位点的结合情况。2. 那些所谓的抗雌激素化合物倾向于同等程度地抑制E2-E2R和E3-E3R的结合。3. 在给定情况下，通过活性炭测定法，氯米芬在4℃时对E2R的抑制常数约为3.8×10⁻⁸M，对E3R的抑制常数在4℃时约为1.8×10⁻⁸M。4. 提示抗雌激素化合物在与E2R或E3R结合后发挥其作用。5. E2R和E3R的含量存在一些组织差异。例如，子宫和皮质含有E2R，而垂体中E3R的含量比其他组织更多。