Kimball F A, Wyngarden L J
Prostaglandins. 1977 Mar;13(3):553-64. doi: 10.1016/0090-6980(77)90032-6.
Preliminary studies indicate the presence of PGF2alpha specific binding sites in membrane fractions prepared from equine corpora lutea. The equilibrium binding data indicate an apparent dissociation constant of 3.2 X 10(-9)M and the concentration of binding sites of -0.1 pmoles/mg membrane protein. Competition of several natural prostaglandins for equine luteal PGF2alpha specific binding sites indicates specificity for the 9alpha-hydroxyl moiety and the 5,6-cis doublebond. Significant increases in relative binding affinities were demonstrated for PGF2alpha analogs with a phenyl ring introduced at carbons 16 or 17. Specific PGF2alpha binding was demonstrated in corpora lutea collected at known stages of the estrous cycle. There was no pattern in these values based on the stage of the cycle. While specific 3H-PGE1 binding could be demonstrated, no high affinity sites could be quantitated. 3H-PGE1 binding appeared unaffected by changes in temperature or time of incubation, whereas PGF2alpha specific binding was significantly modified by both these factors.
初步研究表明，从马黄体制备的膜组分中存在前列腺素F2α特异性结合位点。平衡结合数据表明，表观解离常数为3.2×10⁻⁹M，结合位点浓度为-0.1皮摩尔/毫克膜蛋白。几种天然前列腺素对马黄体前列腺素F2α特异性结合位点的竞争表明，其对9α-羟基部分和5,6-顺式双键具有特异性。在碳16或17处引入苯环的前列腺素F2α类似物的相对结合亲和力显著增加。在发情周期的已知阶段收集的黄体中证明了特异性前列腺素F2α结合。基于周期阶段，这些值没有规律。虽然可以证明特异性³H-前列腺素E1结合，但无法定量高亲和力位点。³H-前列腺素E1结合似乎不受温度或孵育时间变化的影响，而前列腺素F2α特异性结合则受到这两个因素的显著影响。
