Reference : High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro...
Scientific journals : Article
Human health sciences : Radiology, nuclear medicine & imaging
High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.
Le Bars, Didier [Centre d'Exploration et de Recherche Médicales par Émission de Positons - CERMEP (Lyon) >]
Lemaire, Christian mailto [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
Ginovart, N. [> > > >]
Plenevaux, Alain mailto [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
Aerts, Joël mailto [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
Brihaye, C. [> > > >]
Hassoun, W. [> > > >]
Leviel, V. [> > > >]
Mekhsian, P. [> > > >]
Weissmann, D. [> > > >]
Pujol, J. F. [> > > >]
Luxen, André mailto [Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron >]
Comar, Dominique [> > > >]
Nuclear Medicine & Biology
Pergamon Press
Yes (verified by ORBi)
United Kingdom
[en] Animals ; Brain/metabolism ; Cats ; Chromatography, High Pressure Liquid ; Female ; Fluorine Radioisotopes/diagnostic use/pharmacokinetics ; Molecular Structure ; Piperazines/chemical synthesis/diagnostic use/pharmacokinetics ; Pyridines/chemical synthesis/diagnostic use/pharmacokinetics ; Quality Control ; Radioligand Assay ; Radiopharmaceuticals/chemical synthesis/diagnostic use/pharmacokinetics ; Serotonin Antagonists/chemical synthesis/diagnostic use/pharmacokinetics ; Tomography, Emission-Computed
[en] 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.
Centre de Recherches du Cyclotron - CRC ; CERMEP Lyon
Fonds de la Recherche Scientifique (Communauté française de Belgique) - F.R.S.-FNRS
Researchers ; Professionals ; Students

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