Gatley S J, Shaughnessy W J, Inhorn L, Leiberman L M
J Nucl Med. 1981 May;22(5):459-64.
We have studied the distribution of 17 beta(16 alpha-[125I]iodo)-estradiol (I-E2) in tumor-bearing and normal rats. High early adrenal-to-blood ratios (up to 22 at 5 min) were seen in all groups, but this fell to six at 1 hr. Uterus-to-blood ratios of 15 were found, and these were fairly constant up to 2 hr after administration. Uptake of label in the uterus, but not in the adrenals, was sensitive to excess diethylstilbestrol, which competes with I-E2 for estrogen receptors. Mean tumor-to-blood ratios of 1.4, 5.5, and 8.7 were seen at 1 hr in rats with transplanted, spontaneous, and N-nitrosomethylurea-induced tumors, respectively. Diethylstilbestrol was shown to reduce uptake of label by spontaneous tumors. Most of the radioactivity was excreted in the bile by 1 hr. Better estrogen-receptor-binding radiopharmaceuticals can probably be designed.
我们研究了17β(16α-[¹²⁵I]碘)-雌二醇（I-E2）在荷瘤大鼠和正常大鼠体内的分布情况。所有组在早期均出现较高的肾上腺与血液比值（5分钟时高达22），但1小时后降至6。子宫与血液的比值为15，给药后2小时内该比值相当恒定。子宫对标记物的摄取对过量己烯雌酚敏感，而肾上腺对标记物的摄取则不敏感，己烯雌酚与I-E2竞争雌激素受体。在移植瘤、自发瘤和N-亚硝基甲基脲诱导瘤的大鼠中，1小时时肿瘤与血液的平均比值分别为1.4、5.5和8.7。己烯雌酚可减少自发瘤对标记物的摄取。大部分放射性在1小时内通过胆汁排出。或许可以设计出更好的雌激素受体结合放射性药物。
