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-123I] Iodoestradiol and Its Interaction with the Estrogen Receptor In Vivo and In Vitro
Departments of Obstetrics and Gynecology and Diagnostic Radiology, Yale University School of Medicine, New Haven, Connecticut
Correspondence: For reprints contact: Richard B. Hochberg, PhD, Yale University School of Medicine, PO Box 3333, New Haven, CT 06510.
ABSTRACT
In order to produce an estrogen receptor mediated imaging agent, we have synthesized 11ß-methoxy-16
-iodoestradiol labeled with 123I, and have studied its interaction with the estrogen receptor and its distribution in rats and rabbits. This 123I-labeled steroid, 11ß-methoxy-16
-[123I]iodoestradiol, binds with high affinity, Ka = 6 x 109 M1, and specificity to the estrogen receptor in uterine cytosol. When tested in vivo, this radiolabeled steroid concentrates by a receptor mediated mechanism, in the estrogen target tissue, the uterus, producing very high target to nontarget tissue ratios. The results of these experiments indicate that 11ß-methoxy-16
-[123I]iodoestradiol may be a useful imaging agent for clinically monitoring and detecting estrogen receptor containing tumors.
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