References of "Plenevaux, Alain"
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See detailRadiosynthesis of 7-[18F]fluoroindole derivatives.
Otabashi, Muhammad ULg; Giacomelli, Fabrice ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2003), 46

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See detailSimple device for the radiosynthesis of [carbonyl-11C]amides, esters and ketones using carbon-11 monoxide.
Brichard, L.; Del Fiore, G.; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2003), 46

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See detailSynthesis of [18F]fluorinated a-methyl-a-amino acids by phase transfer catalysis for potential PET application.
Wouters, L.; Lemaire, Christian ULg; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2003), 46

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See detailDevelopment and evaluation of an automated atlas-based image analysis method for microPET studies of the rat brain.
Rubins, Daniel J.; Melega, William P.; Lacan, Goran et al

in NeuroImage (2003), 20(4), 2100-18

An automated method for placement of 3D rat brain atlas-derived volumes of interest (VOIs) onto PET studies has been designed and evaluated. VOIs representing major structures of the rat brain were ... [more ▼]

An automated method for placement of 3D rat brain atlas-derived volumes of interest (VOIs) onto PET studies has been designed and evaluated. VOIs representing major structures of the rat brain were defined on a set of digitized cryosectioned images of the rat brain. For VOI placement, each PET study was registered with a synthetic PET target constructed from the VOI template. Registration was accomplished with an automated algorithm that maximized the mutual information content of the image volumes. The accuracy and precision of this method for VOI placement was determined using datasets from PET studies of the striatal dopamine and hippocampal serotonin systems. Each evaluated PET study could be registered to at least one synthetic PET target without obvious failure. Registration was critically dependent upon the initial position of the PET study relative to the synthetic PET target, but not dependent on the amount of synthetic PET target smoothing. An evaluation algorithm showed that resultant radioactivity concentration measurements of selected brain structures had errors=2% due to misalignment with the corresponding VOI. Further, radioligand binding values calculated from these measurements were found to be more precise than those calculated from measurements obtained with manually drawn regions of interest (ROIs). Overall, evaluation results demonstrated that this atlas-derived VOI method can be used to obtain unbiased measurements of radioactivity concentration from PET studies. Its automated features, and applicability to different radioligands and brain regions, will facilitate quantitative rat brain PET assessment procedures. [less ▲]

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See detailThe potential of the beta-Microprobe, an intracerebral radiosensitive probe, to monitor the [(18)F]MPPF binding in the rat dorsal raphe nucleus.
Zimmer, L.; Pain, F.; Mauger, G. et al

in European Journal of Nuclear Medicine and Molecular Imaging (2002), 29(9), 1237-47

The aim of this study was to demonstrate the ability of a recently developed beta(+)-range sensitive intracerebral probe (beta-Microprobe) to measure the binding kinetics of [(18)F]MPPF, a well-documented ... [more ▼]

The aim of this study was to demonstrate the ability of a recently developed beta(+)-range sensitive intracerebral probe (beta-Microprobe) to measure the binding kinetics of [(18)F]MPPF, a well-documented 5-HT(1A) serotoninergic receptor ligand, in the dorsal raphe nucleus (DRN) of the anaesthetised rat. This midbrain nucleus presents a high concentration of 5-HT(1A) receptors known to be implicated in the effects of antidepressants. The difficulty confronting this study lay in the fact that the dimensions of the DRN are smaller than the detection volume of the beta-Microprobe. In the first part of the study, we studied the feasibility of this measurement from a theoretical point of view by autoradiography and a Monte Carlo simulation. We determined the optimal beta-Microprobe location close to the DRN and verified that this configuration allowed accurate determination of [(18)F]MPPF specific binding in the nucleus. In the second part of our study, we measured the in vivo time-concentration curves of [(18)F]MPPF binding in the DRN in comparison with the cerebellum. The specificity of [(18)F]MPPF binding in the DRN was confirmed by its displacement after non-labelled 5-HT(1A)antagonist injection (MPPF or WAY-100635). Moreover, we verified the feasibility of using beta-Microprobe monitoring and simultaneous validation by microdialysis to study the effect of an increase in extracellular serotonin, induced by fenfluramine injection, on [(18)F]MPPF binding in the DRN. Our theoretical simulations, confirmed by our experimental results, demonstrate the ability of this new device to monitor in vivo the binding of [(18)F]MPPF in the DRN of anaesthetised rodents. [less ▲]

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See detail18F-MPPF Pharmacokinetics in rat hippocampus imaged with MicroPet.
Rubin, D. J.; Way, B.; Lacan, G. et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (2002), 43(S1), 209

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See detailInfluence of P-glycoprotein on the tissue distribution in rats of the 5-HT1A antagonist p-[18F]MPPF.
Plenevaux, Alain ULg; Lacan, G.; Defraiteur, C. et al

in Society for Neuroscience / Abstracts (2002)

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See detailFast F-18 FDG synthesis by alkaline hydrolysis on a low polarity solid phase supports
Lemaire, Christian ULg; Damhaut, P.; Lauricella, Benjamino ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2002), 45(5), 435-447

The synthesis of 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) has been simplified by the use of a tC18 Sep Pak cartridge to effect purification and hydrolysis of the tetraacetylated [18F]fluoro-glucose ... [more ▼]

The synthesis of 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG) has been simplified by the use of a tC18 Sep Pak cartridge to effect purification and hydrolysis of the tetraacetylated [18F]fluoro-glucose compound ([18F]TAG). After radiolabelling, this derivative was trapped on a solid phase extraction (SPE) cartridge and the residual reaction solvent (CH3CN), reagents (K222, K2CO3,) and by-products removed by washing the support with water. After this cleaning step, the acetyl groups were cleaved on the same tC18 column using 2N sodium hydroxide. This fast reaction proceeded near quantitatively (>98%) at room temperature in less than 2 min. The [18F]FDG was then recovered with a small amount of water, neutralized with a slight excess of 2N hydrochloric acid, buffered for pH with a citrate solution and finally purified on a neutral alumina oxide and a second tC18 column. After filtration, the radiochemical yield of this [18F]FDG isotonic solution after more than 100 production runs was found to be very reliable and reproducible (70±6% decay corrected). The synthesis time was about 22 min. Quality controls showed that the radiochemical purity was higher than 98% and in any case no [18F]FDM was detected. Only traces of 2-chloro-2-deoxy-glucose (ClDG) were found in the final sample (64±9 g/ batch of 16 ml). [18F]FDG specific activity averaged between 1 and 20 Ci/µmol (EOS). No evaporation and use of ion retardation resin (AG11A8) are required. Moreover, this new approach is suitable for complete remote operation using available single use medical components. Copyright © 2002 John Wiley [less ▲]

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See detailEnantioselective synthesis of 2-[18F]fluoro-L-Tyrosine by catalytic phase-transfer alkylation.
Lemaire, Christian ULg; Gillet, S.; Ooi, T. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2001), 44

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See detailModeling p-18FMPPF pet kinetics for the detremination of local 5-HT1A receptor concentration.
Costes, N.; Le Bars, D.; Merlet, I. et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (2001), 42(S1), 209

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See detail[(18)F]p-MPPF: A radiolabeled antagonist for the study of 5-HT(1A) receptors with PET
Plenevaux, Alain ULg; Lemaire, Christian ULg; Aerts, Joël ULg et al

in Nuclear Medicine & Biology (2000), 27(5), 467-71

This paper summarizes the present status of the researches conducted with [(18)F]4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p-fluorobenzamido ]ethyl]-piperazine known as [(18)F]p-MPPF, a new 5-HT(1A ... [more ▼]

This paper summarizes the present status of the researches conducted with [(18)F]4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p-fluorobenzamido ]ethyl]-piperazine known as [(18)F]p-MPPF, a new 5-HT(1A) antagonist for the study of the serotonergic neurotransmission with positron emission tomography (PET). This includes chemistry, radiochemistry, animal data (rats, cats, and monkeys) with autoradiography and PET, human data with PET, toxicity, and metabolism. [less ▲]

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See detailSynthèse du 6-fluoro-a-méthyl-L-tryptophane et de ses principaux métabolites
Lambin, D.; Tadino, V.; Olynyk, Ch et al

Poster (2000, May 12)

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See detailTissue distribution, autoradiography, and metabolism of 4-(2'-methoxyphenyl)-1-[2' -[N-2"-pyridinyl)-p-[(18)F]fluorobenzamido]ethyl]piperazine (p-[(18)F]MPPF), a new serotonin 5-HT(1A) antagonist for positron emission tomography: An In vivo study in rats.
Plenevaux, Alain ULg; Weissmann, D.; Aerts, Joël ULg et al

in Journal of Neurochemistry (2000), 75(2), 803-11

The in vivo behavior of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p-[(18)F]fluorobenzamido ]ethyl]-piperazine (p-[(18)F]MPPF), a new serotonin 5-HT(1A) antagonist, was studied in awake, freely moving ... [more ▼]

The in vivo behavior of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p-[(18)F]fluorobenzamido ]ethyl]-piperazine (p-[(18)F]MPPF), a new serotonin 5-HT(1A) antagonist, was studied in awake, freely moving rats. Biodistribution studies showed that the carbon-fluorine bond was stable in vivo, that this compound was able to cross the blood-brain barrier, and that a general diffusion equilibrium could account for the availability of the tracer. The great quantity of highly polar metabolites found in plasma did not contribute to the small amounts of metabolites found in hippocampus, frontal cortex, and cerebellum. Exvivo p-[(18)F]MPPF and in vitro 8-hydroxy-2-(di-n-[(3)H]propylamino)tetralin autoradiography were compared both qualitatively and quantitatively. Qualitative evaluation proved that the same brain regions were labeled and that the p-[(18)F]MPPF labeling is (a) in total agreement with the known distribution of 5-HT(1A) receptors in rats and (b) characterized by very low nonspecific binding. Quantitative comparison demonstrated that the in vivo labeling pattern obtained with p-[(18)F]MPPF cannot be explained by differences in regional blood flow, capillary density, or permeability. The 5-HT(1A) specificity of p-[(18)F]MPPF and binding reversibility were confirmed in vivo with displacement experiments. Thus, this compound can be used to evaluate parameters characterizing 5-HT(1A) binding sites in the brain. [less ▲]

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See detailSynthèse du 6-fluoro-a-méthyl-L-tryptophane et d'un de ses métabolites
Lambin, D.; Tadino, V.; Olynyk, Ch et al

Poster (1999, May 03)

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See detail5-HT1A Receptors visualization with p-[18F]MPPF in healthy volunteers.
Plenevaux, Alain ULg; Lemaire, Christian ULg; Salmon, Eric ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detailp-[18F]MPPF, a fluoro analog of WAY-100635 for visualisation of 5-HT1A receptors in cat.
Le Bars, D.; Ginovart, N.; Hassoun, W. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detailThe synthesis of 6-[18F]fluoro-L-dopa by chiral catalytic phase-transfer alkylation.
Lemaire, Christian ULg; Guillouet, S.; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detailIn vivo studies of p-[18F]MPPF metabolites in human.
Damhaut, Ph.; Plenevaux, Alain ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detail5-HT1A receptor distribution in the human brain: preliminary PET data with p-[18F]MPPF.
Fuchs, Sonia ULg; Plenevaux, Alain ULg; Degueldre, Christian ULg et al

in Society for Neuroscience / Abstracts (1999), 25

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See detailp-[18F]MPPF, 5-HT1A antagonist: comparison to [3H]8-OH-DPAT with autoradiography
Plenevaux, Alain ULg; Weissmann, D.; Lemaire, Christian ULg et al

in Society for Neuroscience / Abstracts (1999)

p-MPPF 4-(2’-methoxyphenyl)-1-[2’-[N-(2’’-pyridinyl)-p-fluorobenzamido] ethyl]piperazine is the para-fluorobenzoyl analog of the highly selective 5-HT1A antagonist WAY-100635. The one step procedure used ... [more ▼]

p-MPPF 4-(2’-methoxyphenyl)-1-[2’-[N-(2’’-pyridinyl)-p-fluorobenzamido] ethyl]piperazine is the para-fluorobenzoyl analog of the highly selective 5-HT1A antagonist WAY-100635. The one step procedure used to label p-MPPF with fluorine-18 (cyclotron produced positron emitter of 110 min half-life) leads to a radiopharmaceutical compound easily prepared on a large scale. The preliminary evaluations conducted in rats and cats are good reason to consider p-[18F]MPPF as an interesting reversible radioligand to study the 5-HT1A receptor family in humans with positron emission tomography (PET). In this paper we report a careful comparison between p-[18F]MPPF and [3H]8-OH-DPAT with autoradiography and quantitative densitometry in the same animal. All experiments were conducted in Sprague Dawley male rats. For p-[18F]MMPF, the results were obtained ex-vivo after an intravenous injection of high specific activity radioligand (0.8-1.5 Ci/µmol) in vigil (no anesthesia), free moving and unstressed animals. For the purpose, permanent cannulation of the posterior vena cava were realized at least four days in advance. The [3H]8-OH-DPAT results were obtained in vitro on adjacent coronal sections to the one used for the p-[18F]MPPF autoradiography. Quantitative densitometry was employed to compare the values obtained in relevant brain structures (frontal cortex, lateral septum, hippocampus, dorsal raphe, entorhinal cortex and cerebellum). The plot of the p-[18F]MPPF values obtained for each structure against the [3H]8-OH-DPAT results displayed a significant linear correlation. These results demonstrate that from a qualitative as well as quantitative point of view, the binding of p-[18F]MPPF is totally comparable to the one of [3H]8-OH-DPAT. Supported by grants from INSERM/CGRI and FNRS Belgium. [less ▲]

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