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E-17-[¹²⁵I]Iodovinylestradiol: An Estrogen-Receptor-Seeking Radiopharmaceutical

Northeastern University and Harvard Medical School, Boston, Massachusetts

Correspondence: For reprints contact: Robert N. Hanson, Dept. of Medicinal Chemistry, College of Pharmacy and Allied Health Professions, Northeastern University, Boston, MA 02115.

ABSTRACT

Through the use of radioiododestannylation, the specifically labeled E-17-[¹²⁵I]iodovinylestradiol [(I-125)VE₂] was synthesized rapidly and in high yield from the stable precursor E-17-tributylstannylvinylestradiol (SnVE₂), and its blodistribution was determined in immature female rats. The agent accumulated in the uterus, achieving a peak uptake of 0.465% ID-kg/g at 2 hr. Uterus-to-blood ratios of 19 and 16 occurred at 1 and 2 hr, respectively, declining to 7 by 4 hr after injection. The uptake of (I-125)VE₂ by the uterus at 2 hr was reduced 58–65% by pretreatment of the immature rats with estradiol (5 µg) or tamoxifen (100 µg), and compared with 16-[¹²⁵I]iodoestradiol, (I-125)VE₂ showed greater uterine uptake and similar uterus-to-blood ratios. The ease of preparation of the radioligand represents an advantage over the synthetic procedures for other estrogen-receptor-seeking agents.