Preparation and evaluation of 17α-[125I]iodovinyl-11β-methoxyestradiol as a highly selective radioligand for tissues containing estrogen receptors: concise communication

The moxestrol analog 17α-[125I]iodovinyl-11β-methoxyestradiol was prepared in 95% radiochemical yield from the corresponding 17α-(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 largest tissue. The compounds'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