Hanson R N, Franke L A
J Nucl Med. 1984 Sep;25(9):998-1002.
The moxestrol analog 17 alpha-[125I]iodovinyl-11 beta-methoxyestradiol was prepared in 95% radiochemical yield from the corresponding 17 alpha-(tributylstannyl) vinyl compound and no-carrier-added sodium [125I]iodide. The new radioligand was evaluated in immature female rats to determine the uptake in and selectivity for tissues containing estrogen receptors. At 1, 2, and 6 hr after injection, the agent demonstrates both high selectivity (uterus to blood ratio) and a high concentration in the target tissue. These values are considerably better than those previously reported for IVE2 or for the 16 alpha-radiohalogenated estradiols. The compound's biologic properties and its ease of preparation suggest that it would be a likely candidate for clinical use as an estrogen-receptor-seeking radiopharmaceutical.
莫昔雌醇类似物17α-[¹²⁵I]碘乙烯基-11β-甲氧基雌二醇由相应的17α-(三丁基锡烷基)乙烯基化合物和无载体添加的[¹²⁵I]碘化钠制备而成，放射化学产率为95%。在未成熟雌性大鼠中对这种新的放射性配体进行了评估，以确定其在含有雌激素受体的组织中的摄取情况和选择性。注射后1小时、2小时和6小时，该药物表现出高选择性（子宫与血液的比值）以及在靶组织中的高浓度。这些数值比之前报道的IVE2或16α-放射性卤代雌二醇的数值要好得多。该化合物的生物学特性及其易于制备表明，它可能是一种有望用作寻找雌激素受体的放射性药物的临床候选物。
