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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
1988-8-5
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pubmed:abstractText |
We have synthesized 21-[18F]fluoro-16 alpha-ethyl-19-norprogesterone (FENP), a high affinity ligand for the progesterone receptor, labeled with the positron-emitting radionuclide fluorine-18 (t1/2 = 110 min). The synthesis proceeds in two steps from 21-hydroxy-16 alpha-ethyl-19-norprogesterone and involves [18F]fluoride ion displacement of the 21-trifluoromethanesulfonate (21-triflate). This material is purified by HPLC and is obtained in 4-30% overall yield (decay corrected) within 40 min after the end of bombardment to produce [18F]fluoride ion. The effective specific activity, determined by competitive radioreceptor binding assays, is 700-1400 Ci/mmol. In vivo, [18F]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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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/16...,
http://linkedlifedata.com/resource/pubmed/chemical/Estrogens,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Norpregnenes,
http://linkedlifedata.com/resource/pubmed/chemical/Norprogesterones,
http://linkedlifedata.com/resource/pubmed/chemical/Pregnenediones,
http://linkedlifedata.com/resource/pubmed/chemical/Progesterone,
http://linkedlifedata.com/resource/pubmed/chemical/Progesterone Congeners,
http://linkedlifedata.com/resource/pubmed/chemical/Promegestone,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Progesterone
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
31
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1360-3
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:3260285-Animals,
pubmed-meshheading:3260285-Binding, Competitive,
pubmed-meshheading:3260285-Chemical Phenomena,
pubmed-meshheading:3260285-Chemistry,
pubmed-meshheading:3260285-Chromatography, High Pressure Liquid,
pubmed-meshheading:3260285-Estrogens,
pubmed-meshheading:3260285-Female,
pubmed-meshheading:3260285-Fluorine Radioisotopes,
pubmed-meshheading:3260285-Norpregnenes,
pubmed-meshheading:3260285-Norprogesterones,
pubmed-meshheading:3260285-Pregnenediones,
pubmed-meshheading:3260285-Progesterone,
pubmed-meshheading:3260285-Progesterone Congeners,
pubmed-meshheading:3260285-Promegestone,
pubmed-meshheading:3260285-Rats,
pubmed-meshheading:3260285-Rats, Inbred Strains,
pubmed-meshheading:3260285-Receptors, Progesterone,
pubmed-meshheading:3260285-Tomography, Emission-Computed,
pubmed-meshheading:3260285-Uterus
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pubmed:year |
1988
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pubmed:articleTitle |
21-[18F]fluoro-16 alpha-ethyl-19-norprogesterone: synthesis and target tissue selective uptake of a progestin receptor based radiotracer for positron emission tomography.
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pubmed:affiliation |
Department of Chemistry, University of Illinois, Urbana 61801.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.
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