去甲基屈洛昔芬（3-羟基他莫昔芬）后雌激素或抗雌激素活性无损失。

No loss of estrogenic or anti-estrogenic activity after demethylation of droloxifene (3-OH-tamoxifen).

作者信息

Löser R, Seibel K, Eppenberger U

出版信息

Int J Cancer. 1985 Dec 15;36(6):701-3. doi: 10.1002/ijc.2910360614.

Abstract

The binding affinity of 3-OH-Tamoxifen (Droloxifene or DROL) and N-demethyl-droloxifene (ND-DROL) to the cystosolic estrogen receptor of rabbit uteri was 10 times higher than that of Tamoxifen. Both compounds exhibited similar stimulation (estrogenic effect) and inhibition (anti-estrogenic effect) of uterine growth of immature female rats. 3H-Uridine incorporation into the RNA of MCF-7 and ZR-75 cells as a measure of anti-estrogenic activity was equally inhibited by concentrations of 0.05-1.0 mumol/l of both compounds. Thus, the pharmacological properties of DROL were not changed by N-demethylation.

摘要

3-羟基他莫昔芬（屈洛昔芬或DROL）和N-去甲基屈洛昔芬（ND-DROL）与兔子宫胞质雌激素受体的结合亲和力比他莫昔芬高10倍。两种化合物对未成熟雌性大鼠子宫生长均表现出相似的刺激（雌激素效应）和抑制（抗雌激素效应）。作为抗雌激素活性的一种衡量指标，两种化合物浓度为0.05 - 1.0 μmol/L时，均能同等程度地抑制3H-尿苷掺入MCF-7和ZR-75细胞的RNA中。因此，N-去甲基化并未改变DROL的药理特性。