Article (Scientific journals)
High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.
Le Bars, Didier; Lemaire, Christian; Ginovart, N. et al.
1998In Nuclear Medicine and Biology, 25 (4), p. 343-50
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Keywords :
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
Abstract :
[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.
Research center :
GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège
CERMEP Lyon
Disciplines :
Radiology, nuclear medicine & imaging
Author, co-author :
Le Bars, Didier;  Centre d'Exploration et de Recherche Médicales par Émission de Positons - CERMEP (Lyon)
Lemaire, Christian ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Ginovart, N.
Plenevaux, Alain  ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Aerts, Joël ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Brihaye, C.
Hassoun, W.
Leviel, V.
Mekhsian, P.
Weissmann, D.
Pujol, J. F.
Luxen, André ;  Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron
Comar, Dominique
More authors (3 more) Less
Language :
English
Title :
High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.
Publication date :
1998
Journal title :
Nuclear Medicine and Biology
ISSN :
0969-8051
Publisher :
Pergamon Press, Oxford, United Kingdom
Volume :
25
Issue :
4
Pages :
343-50
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
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