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16-[⁷⁷Br]Bromoestradiol-17ß: A High Specific-Activity, Gamma-Emitting Tracer with Uptake in Rat Uterus and Induced Mammary Tumors

University of Illinois, Urbana, Illinois
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri
Los Alamos Scientific Laboratory, Los Alamos, New Mexico

Correspondence: For reprints contact: John A. Katzenellenbogen, School of Chemical Sciences, Univ. of Illinois, Urbana, IL 61801.

ABSTRACT

16-[⁷⁷Br]Bromoestradiol-17ß (Compound 1) has been synthesized by radiobromination of estrone enoldiacetate. Tissue uptake studies performed 1 hr after administration of Compound 1 to immature or mature female rats showed uterus-to-blood ratios of 13, with nontarget tissue-to-blood ratios ranging from 0.6 to 2. Co-administration of unlabeled estradiol caused a selective depression in the uterine uptake with no effect on nontarget tissue uptake. In adult animals bearing adenocarcinomas induced by DMBA (7,12-dimethylbenz(a)anthracene), tumor-to-blood ratios of 6.3 were obtained, this uptake also being depressed in animals treated with unlabeled estradiol. The studies demonstrate that Compound 1 has suitable binding properties and sufficiently high specific activity so that its uptake in estrogen target tissues in vivo is mediated primarily by the estrogen receptor. Furthermore, they suggest that this compound may be suitable for imaging human breast tumors that contain estrogen receptors.

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