Jordan V C, Koch R, Mittal S, Schneider M R
Br J Pharmacol. 1986 Jan;87(1):217-23. doi: 10.1111/j.1476-5381.1986.tb10174.x.
The oestrogenic and antioestrogenic activities of a series of substituted derivatives of 1,1,2 triphenylbut-1-ene have been determined using primary cultures of rat pituitary gland cells to monitor prolactin synthesis in vitro. The relative binding affinity of the agonists for the oestrogen receptor was consistent with their oestrogenic potency. Bis para substitution at C1 of 1,1,2 triphenylbut-1-ene with either phenolic or acetoxy groups produced partial agonists. The antioestrogenic properties were reversible by the incubation of cells with increasing concentrations of oestradiol. The results lend support to a hypothetical single binding site model of oestrogen action, based upon an adaptation of Belleau's macromolecular perturbation theory.
利用大鼠垂体腺细胞原代培养物来监测体外催乳素的合成，已测定了一系列1,1,2-三苯基丁-1-烯取代衍生物的雌激素活性和抗雌激素活性。这些激动剂对雌激素受体的相对结合亲和力与它们的雌激素效力一致。在1,1,2-三苯基丁-1-烯的C1位进行双对位取代，用酚基或乙酰氧基取代会产生部分激动剂。通过用浓度递增的雌二醇孵育细胞，抗雌激素特性是可逆的。基于对贝洛大分子扰动理论的改编，这些结果支持了雌激素作用的假设单结合位点模型。
