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Preparation and Evaluation of 17-[¹²⁵I]Iodovinyl-11ß-Methoxyestradiol as a Highly Selective Radioligand for Tissues Containing Estrogen Receptors: Concise Communication

Northeastern University, Harvard Medical School, and Children's Hospital Corporation, Boston, Massachusetts

Correspondence: For reprints contact: R. N. Hanson, PhD, College of Pharmacy and Allied Health Professions, Northeastern University, Boston, MA 02115.

ABSTRACT

The moxestrol analog 17-[¹²⁵I]iodovinyl-11ß-methoxyestradiol was prepared in 95% radiochemical yield from the corresponding 17-(tributyistannyl)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-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.