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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1997-1-7
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pubmed:abstractText |
We describe the 18F-radiolabelling synthesis (18F; T(1/2) = 109.8 min) of 2-beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane (also known as CFT or WIN 35,428) and the biodistribution of this compound in rats. 18F-labelled CFT has high chemical and radiochemical purity and relatively high specific radioactivity [specific radioactivity up to 14.8 GBq/mumol (400 mCi/mumol) at end of synthesis]. Striatum to cerebellum radioactivity uptake ratios were calculated from digitised images of rat brain slices recorded with a phosphoimaging device, the maximum ratio of about 10 was obtained at 2 h postinjection. Pretreatment of the rats with a specific dopamine transport inhibitor, GBR 12909, showed that CFT binding is specific in striatum. The highest accumulation of 18F-radioactivity was found in the liver, urine, striatum, and kidney of the rat. Clearance from blood was rapid. The uptake in bone was low, indicating that [18F]CFT is not defluorinated. The relatively long half-life of 18F makes it possible to study the uptake of [18F]CFT in the brain, as equilibrium between specific and non-specific binding is reached. This will improve the signal to noise ratio as compared to positron emission tomography (PET) studies with [11C]CFT (11C; T(1/2) = 20.4 min). CFT labelled with 18F is clearly a promising radioligand for PET studies of the dopamine transporter system in humans.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/(1R-(exo,exo))-3-(4-fluorophenyl)-8-...,
http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Cocaine,
http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Plasma Membrane Transport...,
http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Uptake Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Glycoproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Transport Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Nerve Tissue Proteins
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0887-4476
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
321-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8855517-Animals,
pubmed-meshheading:8855517-Brain,
pubmed-meshheading:8855517-Carrier Proteins,
pubmed-meshheading:8855517-Cocaine,
pubmed-meshheading:8855517-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:8855517-Dopamine Uptake Inhibitors,
pubmed-meshheading:8855517-Fluorine Radioisotopes,
pubmed-meshheading:8855517-Male,
pubmed-meshheading:8855517-Membrane Glycoproteins,
pubmed-meshheading:8855517-Membrane Transport Proteins,
pubmed-meshheading:8855517-Nerve Tissue Proteins,
pubmed-meshheading:8855517-Radioligand Assay,
pubmed-meshheading:8855517-Rats,
pubmed-meshheading:8855517-Rats, Sprague-Dawley,
pubmed-meshheading:8855517-Tissue Distribution,
pubmed-meshheading:8855517-Tomography, Emission-Computed
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pubmed:year |
1996
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pubmed:articleTitle |
[18F]CFT ([18F]WIN 35,428), a radioligand to study the dopamine transporter with PET: biodistribution in rats.
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pubmed:affiliation |
Medical Cyclotron/PET Center, University of Turku, Finland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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