Feenstra A, Vaalburg W, Nolten G M, Reiffers S, Talma A G, Wiegman T, van der Molen H D, Woldring M G
J Nucl Med. 1983 Jun;24(6):522-8.
Tritiated 17 alpha-methylestradiol was synthesized to investigate the potential of the carbon-11-labeled analog as an estrogen-receptor-binding radiopharmaceutical. In vitro, 17 alpha-methylestradiol is bound with high affinity to the cytoplasmic estrogen receptor from rabbit uterus (Kd = 1.96 x 10(-10)M), and it sediments as an 8S hormone-receptor complex in sucrose gradients. The compound shows specific uptake in the uterus of the adult rat, within 1 hr after injection. After 30 min the uterine uptake was 1.73% dose/g. In female rats bearing DMBA-induced tumors, specific uterine and tumor uptakes were observed, although at 30 min the tumor uptake was only 23-30% of the uptake in the uterus. Tritiated 17 alpha-methylestradiol with a specific activity of 6 Ci/mmole showed a similar tissue distribution. Our results indicate that 17 alpha-methylestradiol is promising as an estrogen-receptor-binding radiopharmaceutical.
合成了氚标记的17α-甲基雌二醇，以研究碳-11标记类似物作为雌激素受体结合放射性药物的潜力。在体外，17α-甲基雌二醇与兔子宫细胞质雌激素受体具有高亲和力结合（解离常数Kd = 1.96×10⁻¹⁰M），并且在蔗糖梯度中以8S激素-受体复合物形式沉降。该化合物在成年大鼠注射后1小时内显示出在子宫中的特异性摄取。30分钟后子宫摄取量为1.73%剂量/克。在患有DMBA诱导肿瘤的雌性大鼠中，观察到子宫和肿瘤的特异性摄取，尽管在30分钟时肿瘤摄取量仅为子宫摄取量的23 - 30%。比活度为6居里/毫摩尔的氚标记17α-甲基雌二醇显示出相似的组织分布。我们的结果表明，17α-甲基雌二醇作为雌激素受体结合放射性药物具有前景。
