(2R*, 3S*)-1- [18fluoro-2, 3-bis (4-hydroxyphenyl) pentane ([18F]fluoronorhexestrol), A positron-emitting estrogen that shows highly-selective, receptor-mediated uptake by target tissues in vivo

Scott W. Landvatter, Dale O. Kiesewetter, Michael R. Kilbourn, John A. Katzenellenbogen, Michael J. Welch

Research output: Contribution to journalArticlepeer-review

Abstract

The positron-emitting, non-steroidal estrogen (2R*, 3S*)-1-[18F]fluoro-2, 3-bis (4-hydroxyphenyl) pentane ([18F]-fluoronor-hexestrol), has been prepared by fluoride ion displacement on a labile trifluoromethanesulfonate (triflate) derivative of a suitably protected precursor, followed by removal of the aryl triflate groups with lithium aluminum hydride and purification by HPLC. In immature female rats, this compound is taken up selectively by the uterus and is retained for prolonged periods, due to its binding to the estrogen receptor. This compound and related 18F-labeled estrogens thus appear to be promising agents for imaging estrogen receptor-positive breast tumors in humans.

Original languageEnglish (US)
Pages (from-to)1933-1938
Number of pages6
JournalLife Sciences
Volume33
Issue number19
DOIs
StatePublished - Nov 7 1983

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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