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Comparison of the Distribution of Bromine-77-Bromovinyl Steroidal and Triphenylethylene Estrogens in the Immature Rat

Ben May Institute, Department of Radiology, University of Chicago, Chicago, Illinois
Argonne National Laboratory, Argonne, Illinois

Correspondence: For reprints contact: Eugene R. DeSombre, Ben May institute, University of Chicago, 5841 S. Maryland Ave., Chicago, IL 60637.

ABSTRACT

The specific uptake and distribution of steroidal and nonsteroidal [⁷⁷Br]bromovinylestrogens were studied in immature female rats to assess the potential of these radioligands for imaging or therapy of estrogen receptor (ER) positive cancers. E-17[⁷⁷Br] bromovinylestradiol, its 3 methyl ether and 11ß-methoxy derivative, as well as the triphenylethylene estrogen, 1,1-bis[4-hydroxy-phenyl]-2- [⁷⁷Br]bromo-2-phenylethylene all showed diethylstilbestrol inhibitable, specific uptake of radiobromine between 2 and 16 hr after i.p. administration. The highest concentrations in the estrogen target tissues and the highest target tissue to-blood ratios were found with E-17-[⁷⁷Br]bromovinyl- 11ß-methoxyestradiol, but it also had rather high nonspecific uptake in all tissues. The triphenylethylene estrogen showed comparable specific uptake in estrogen target tissues to 17[⁷⁷Br]bromovinylestradiol at 2 hr but better apparent retention, indicated by higher specific target tissue levels at the later time points. Thus, [⁷⁷Br]bromovinyl-11ß-methoxyestradiol and 1,1-bis[4-hydroxyphenyl]-2- [⁷⁷Br]bromo-2-phenylethylene appear most favorable for these applications.

FOOTNOTES

^* Present address: Medical Division, Brookhaven National Laboratory, Associated Universities, Inc., Upton, NY 11973.