21-( super(18)F)fluoro-16 alpha -ethyl-19-norprogesterone: Synthesis and target tissue selective uptake of a progestin receptor based radiotracer for positron emission tomography

The authors have synthesized 21-( super(18)F)fluoro-16 alpha -ethyl-19-norprogesterone (FENP), a high affinity ligand for the progesterone receptor, labeled with the positron-emitting radionuclide fluorine-18. ( super(18)F)FENP demonstrates highly selective, receptor-mediated uptake by the uterus of...

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Published inJournal of medicinal chemistry Vol. 31; no. 7; pp. 1360 - 1363
Main Authors Pomper, M G, Katzenellenbogen, JA, Welch, MJ, Brodack, J W, Mathias, C J
Format Journal Article
LanguageEnglish
Published 01.01.1988
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Summary:The authors have synthesized 21-( super(18)F)fluoro-16 alpha -ethyl-19-norprogesterone (FENP), a high affinity ligand for the progesterone receptor, labeled with the positron-emitting radionuclide fluorine-18. ( super(18)F)FENP demonstrates highly selective, receptor-mediated uptake by the uterus of estrogen-primed rats; the uterus to blood and uterus to muscle ratios were respectively 26 and 16 at 1 h and 71 and 41 at 3 h after injection. The high target tissue selectivity of this uptake suggests that this compound may be useful for the in vivo imaging of progestin target tissues and receptor-rich tumors (such as human breast tumors) by positron emission tomography.
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ISSN:0022-2623