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The Journal of Nuclear Medicine Vol. 30 No. 2 209-215
© 1989 by Society of Nuclear Medicine
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The Synthesis of 11ß-Methoxy-[16{alpha}-123I] Iodoestradiol and Its Interaction with the Estrogen Receptor In Vivo and In Vitro

Jan E. Zielinski, Janice M. Larner, Paul B. Hoffer and Richard B. Hochberg

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{alpha}-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{alpha}-[123I]iodoestradiol, binds with high affinity, Ka = 6 x 109 M–1, 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{alpha}-[123I]iodoestradiol may be a useful imaging agent for clinically monitoring and detecting estrogen receptor containing tumors.




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D. A. Mankoff, J. M. Link, H. M. Linden, L. Sundararajan, and K. A. Krohn
Tumor Receptor Imaging
J. Nucl. Med., June 1, 2008; 49(Suppl_2): 149S - 163S.
[Abstract] [Full Text] [PDF]




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Copyright © 1989 by the Society of Nuclear Medicine.