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

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

1. 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.

兔子宫雌三醇特异性结合位点抗雌激素作用的可能性。
1. 本研究旨在探讨克罗米芬或他莫昔芬与兔子宫雌二醇-17 β (E2R)和雌三醇(E3R)受体位点的结合。2. 这些所谓的抗雌激素化合物倾向于同样抑制E2-E2R和E3-E3R结合。3.在给定的情况下,克罗米芬对E2R的抑制剂常数在4℃时约为3.8 × 10(-8) M,对E3R的抑制剂常数在4℃时约为1.8 × 10(-8) M。4. 这表明,抗雌激素化合物在与E2R或E3R结合后显示其作用。5. E2R和E3R在组织中含量存在一定差异。例如,子宫和皮质含有E2R,垂体含有E3R。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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