Comparison of the distribution of bromine-77-bromovinyl steroidal and triphenylethylene estrogens in the immature rat

E. R. DeSombre, A. Hughes, R. C. Mease, P. V. Harper

Research output: Contribution to journalArticlepeer-review

Abstract

The specific uptake and distribution of steroidal and non-steroidal [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-17α[77Br]bromovinylestradiol, its 3 methyl ether and 11β-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-17α-[77Br]bromovinyl-11β-methoxyestradiol, but it also had rather high nonspecific uptake in all tissues. The triphenylethylene estrogen showed comparable specific uptake in estrogen target tissues to 17α[77Br]bromovinylestradiol at 2 hr but better apparent retention, indicated by higher specific target tissue levels at the later time points. Thus, [77Br]bromovinyl-11β-methoxyestradiol and 1,1-bis[4-hydroxyphenyl]-2-[77Br]bromo-2-phenylethylene appear most favorable for these applications.

Original languageEnglish (US)
Pages (from-to)1534-1542
Number of pages9
JournalJournal of Nuclear Medicine
Volume31
Issue number9
StatePublished - 1990
Externally publishedYes

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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