rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
4
|
pubmed:dateCreated |
1998-9-17
|
pubmed:abstractText |
No-carrier-added 4-[18F]fluoro-N-[2-[1-(2-methoxyphenyl)-1 piperazinyl]ethyl-N-2-pyridinyl-benzamide (p-[18F]MPPF) was synthesized by nucleophilic substitution of the corresponding nitro compound in the presence of Kryptofix 222 and K2CO3 by microwave heating (3 min, 500 W) using a remotely controlled radiosynthesis. Baseline separation of p-[18F]MPPF from the nitro derivative was performed on a semipreparative HPLC C18 column. After Sep-Pak formulation, the radiopharmaceutical was obtained with a radiochemical yield of 25% (EOS) in about 70 min. Specific radioactivity averaged between 1-5 Ci/micromol EOS. Labelling of the ortho and meta derivatives was also attempted. Brain uptake of p-[18F]MPPF was studied with PET on fluothane-anesthetized cats. Following intravenous injection of p-[18F]MPPF, high accumulation of radioactivity was observed in the hippocampus and cerebral cortex. Low levels of radioactivity were observed in cerebellum. At 30 min, the mean hippocampus/cerebellum and cortex/cerebellum ratios were 5 and 3.8, respectively. The accumulation of the tracer was blocked by prior administration of reference WAY-100635, demonstrating the specificity of the ligand.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0969-8051
|
pubmed:author |
pubmed-author:BENYOE AEA,
pubmed-author:BrihayeCC,
pubmed-author:ComarDD,
pubmed-author:GinovartNN,
pubmed-author:HassounWW,
pubmed-author:Le BarsDD,
pubmed-author:LemaireCC,
pubmed-author:LevielVV,
pubmed-author:LuxenAA,
pubmed-author:MekhsianPP,
pubmed-author:PlenevauxAA,
pubmed-author:PujolJ FJF,
pubmed-author:WeissmannDD
|
pubmed:issnType |
Print
|
pubmed:volume |
25
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
343-50
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:9639295-Animals,
pubmed-meshheading:9639295-Brain,
pubmed-meshheading:9639295-Cats,
pubmed-meshheading:9639295-Chromatography, High Pressure Liquid,
pubmed-meshheading:9639295-Female,
pubmed-meshheading:9639295-Fluorine Radioisotopes,
pubmed-meshheading:9639295-Molecular Structure,
pubmed-meshheading:9639295-Piperazines,
pubmed-meshheading:9639295-Pyridines,
pubmed-meshheading:9639295-Quality Control,
pubmed-meshheading:9639295-Radioligand Assay,
pubmed-meshheading:9639295-Radiopharmaceuticals,
pubmed-meshheading:9639295-Serotonin Antagonists,
pubmed-meshheading:9639295-Tomography, Emission-Computed
|
pubmed:year |
1998
|
pubmed:articleTitle |
High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.
|
pubmed:affiliation |
CERMEP, Lyon, France. lebars@univ-lyon1.fr
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|