High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635.; Lemaire, Christian ; et alin Nuclear Medicine & Biology (1998), 25(4), 343-50 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 ... [more ▼] 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. [less ▲] Detailed reference viewed: 38 (6 ULg)![]() Métabolisme du p-[18]MPPF (antagoniste 5-HT1A) chez le ratPlenevaux, Alain ; Aerts, Joël ; Lemaire, Christian et alPoster (1997, May 29) Detailed reference viewed: 8 (0 ULg) Le p-[18F]MPPF: un nouveau ligand pour l'étude par TEP des récepteurs 5-HT1A; ; Lemaire, Christian et alPoster (1997, May 25) Detailed reference viewed: 10 (0 ULg)![]() Microwave improved synthesis of p-[18F]MPPF, 5-HT1A antagonist and PET sudies on cat brain.; ; Lemaire, Christian et alin Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40 Detailed reference viewed: 6 (0 ULg)![]() Tissue distribution, autoradiography and metabolism in rats of p-[18F]MPPF: 5-HT1A antagonist.Plenevaux, Alain ; Aerts, Joël ; Lemaire, Christian et alin Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40 Detailed reference viewed: 4 (0 ULg) Evaluation of p-[18F]MPPF, 5-HT1A antagonist, a potential radiopharmaceutical for PET: tissue distribution, autoradiography and metabolism in rats.Plenevaux, Alain ; Aerts, Joël ; Lemaire, Christian et alin Society for Neuroscience / Abstracts (1997), 23 Detailed reference viewed: 5 (1 ULg)![]() Evaluation of p-[F-18]MPPF, 5-HT1A antagonist, in rats: tissue distribution, autoradiography and metabolism.Plenevaux, Alain ; Aerts, Joël ; Lemaire, Christian et alin Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1997), 38 Detailed reference viewed: 8 (1 ULg) |
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