雌激素受体在脑、垂体和子宫中的特异性。
The specificity of oestrogen receptor in brain, pituitary and uterus.
作者信息
Ginsburg M, Maclusky N J, Morris I D, Thomas P J
出版信息
Br J Pharmacol. 1977 Mar;59(3):397-402. doi: 10.1111/j.1476-5381.1977.tb08392.x.
Abstract
1 The specificity of oestrogen receptor in rat brain regions (hypothalamus, amygdala and cortex), pituitary and uterus was studied by measurement of the inhibition of 17beta-oestradiol high affinity binding in cytosol, in the presence of unlabelled putative inhibitors of binding. 2 Binding was inhibited only by those of the compounds tested that possessed oestrogen agonist or antagonist activity. The affinities were estimated and the ranking order of the compounds was the same in all tissue sources of cytosol and corresponded to the ranking order of agonist or antagonist potency. 3 There were some significant differences between some of the estimated affinities in different tissues, these being seen most commonly between pituitary and hypothalamus on one hand and uterus on the other. 4 The possibility of heterogeneity of oestrogen receptor is discussed.
摘要
- 通过在存在未标记的假定结合抑制剂的情况下测量细胞溶胶中17β - 雌二醇高亲和力结合的抑制作用，研究了大鼠脑区（下丘脑、杏仁核和皮层）、垂体和子宫中雌激素受体的特异性。2. 仅具有雌激素激动剂或拮抗剂活性的测试化合物能抑制结合。估计了亲和力，并且这些化合物的排序在所有细胞溶胶组织来源中是相同的，并且与激动剂或拮抗剂效力的排序相对应。3. 不同组织中一些估计的亲和力之间存在一些显著差异，最常见的是一方面垂体和下丘脑之间，另一方面子宫与它们之间的差异。4. 讨论了雌激素受体异质性的可能性。
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