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Estrogen Derivatives for the External Localization of Estrogen-Dependent Malignancy

George Washington University, Washington, D.C.
National Naval Medical Center, Bethesda, Maryland

Correspondence: For reprints contact: William C. Eckelman, Div. of Nuclear Medicine, George Washington University, Washington, DC 20037.

ABSTRACT

Four radioiodinated estrogen derivatives were studied to determine their affinity for the estrogen-binding protein found in the cytosol of rabbit and rat uteri. In vitro determination of the binding properties by competitive-binding experiments and by sucrose-gradient centrifugation indicates that one of the derivatives, iodohexestrol, binds to the cytosol estrogen binding protein. This in vitro behavior was related to in vivo distribution. Studies in immature female rats showed high uterine uptake of iodohexestrol at 2 hr (1.69% dose/gm). Iodohexestrol also has a high nonspecific binding in both the blood and the uterine cytosol. Thyroxine can diminish the nonspecific binding in vitro; in vivo the prior injection of thyroxine increased the 2-hr uterus-to-blood ratio from 1.9 to 10.4. The in vitro receptor-assay system was helpful in predicting in vivo distribution.

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				R. Hochberg Iodine-125--labeled estradiol: a gamma-emitting analog of estradiol that binds to the estrogen receptor Science, September 14, 1979; 205(4411): 1138 - 1140. [Abstract] [PDF]