References of "Aerts, Joël"
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See detailFully Automated Preparation and Conjugation of N-Succinimidyl 4-[(18)F]Fluorobenzoate ([ (18)F]SFB) with RGD Peptide Using a GE FASTlab Synthesizer.
Thonon, David ULg; Goblet, D.; Goukens, Eve ULg et al

in Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging (2011)

PURPOSE: The aim of this work was to automate the radiosynthesis of [(18)F]SFB, a widely used reagent for the labeling of biomolecules with (18)F on a new generation commercial synthesis module (FASTLab ... [more ▼]

PURPOSE: The aim of this work was to automate the radiosynthesis of [(18)F]SFB, a widely used reagent for the labeling of biomolecules with (18)F on a new generation commercial synthesis module (FASTLab, GE Healthcare). PROCEDURES: Two synthesis approaches were implemented on this module: the classical "two-pot radiosynthesis" and the more recently described "one-pot" method. RESULTS: The "two-pot" approach affords [(18)F]SFB with a 42% decay-corrected yield in 57 min (n = 24) with a chemical purity sufficient to avoid an intermediate HPLC purification. The recently established "one-pot" method, afforded a product with a lower chemical purity, in the conditions used in this report. The lower d.c. yield obtained (32% (n = 15)) was related to the low (18)F labeling yields obtained in MeCN compared with DMSO. The subsequent conjugation step with a RGD (PRGD2) peptide was also successfully automated. CONCLUSIONS: The formulated [(18)F]FPRGD2 was obtained without any operator manipulation with a d.c. yield of 13% +/- 3% (n = 13) in 130 min, a radiochemical purity >98% and a specific activity of 140 +/- 40 TBq/mmol. [less ▲]

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See detailControlled Memory Processes in Questionable Alzheimer's Disease: A View from Neuroimaging Research
Bastin, Christine ULg; Kerrouche N; Lekeu, Françoise ULg et al

in Journal of Alzheimer's Disease [=JAD] (2010), 20(2), 547-560

Alzheimer's disease (AD) is characterized by a progressive loss of controlled cognitive processes, and neuroimaging studies at early stages of AD provide an opportunity to tease out the neural correlates ... [more ▼]

Alzheimer's disease (AD) is characterized by a progressive loss of controlled cognitive processes, and neuroimaging studies at early stages of AD provide an opportunity to tease out the neural correlates of controlled processes. Accordingly, controlled and automatic memory performance was assessed with the Process Dissociation Procedure in 50 patients diagnosed with questionable Alzheimer's disease (QAD). The patients' brain glucose metabolism was measured using FDG-PET. After a follow-up period of 36 months, 27 patients had converted to AD, while 23 remained stable. Both groups showed a similar decrease in controlled memory processes but preserved automatic processes at entry into the study. Voxel-based cognitive and metabolic correlations showed that a decrease in controlled memory processes was preferentially correlated with lower activity in the dorsomedial prefrontal and posterior cingulate cortices in very early AD patients. In stable QAD patients, reduced controlled performance in verbal memory correlated with impaired activity in the left anterior hippocampal structure. The results demonstrated the central role of a medial frontal-posterior cingulate network for controlled processing of episodic memory in the early stages of AD. [less ▲]

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See detailFast Production of Highly Reactive No-Carrier-Added [18F]Fluoride for the Labeling of Radiopharmaceuticals
Lemaire, Christian ULg; Aerts, Joël ULg; Voccia, Samuel et al

in Angewandte Chemie (International ed. in English) (2010), 49

The 18F labeling of radiopharmaceuticals requires nearly anhydrous solutions of [18F]fluoride. Aqueous K2CO3 is generally used to elute [18F]fluoride from an anion-exchange resin. Replacing aqueous K2CO3 ... [more ▼]

The 18F labeling of radiopharmaceuticals requires nearly anhydrous solutions of [18F]fluoride. Aqueous K2CO3 is generally used to elute [18F]fluoride from an anion-exchange resin. Replacing aqueous K2CO3 with strong organic bases, such as the phosphazene base P2Et enabled the recovery of highly reactive [18F]fluoride and avoided the azeotropic evaporation of water, which is very difficult on a microchip device. [less ▲]

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See detailFast production of highly concentrated reactive [18F] fluoride for aliphatic and aromatic nucleophilic radiolabelling
Aerts, Joël ULg; Voccia, Samuel; Lemaire, Christian ULg et al

in Tetrahedron Letters (2010), 51

The use of a polymeric solid support loaded with a long alkyl chain quaternary ammonium allows the rapid and efficient recovery of cyclotron produced [18F]F- from [18O]water to a low water content organic ... [more ▼]

The use of a polymeric solid support loaded with a long alkyl chain quaternary ammonium allows the rapid and efficient recovery of cyclotron produced [18F]F- from [18O]water to a low water content organic solution compatible with fast nucleophilic labelling of most precursors for PET radiopharmaceuticals in high yield. [less ▲]

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See detailMethod for the direct elution of reactive 18F fluoride from an anion exchange resin in an organic medium suitable for radiolabeling without any evaporation step by the use of strong organic bases
Lemaire, Christian ULg; Voccia, Samuel; Aerts, Joël ULg et al

Patent (2009)

The present invention relates to a method to extract out of an aqueous solution, concentrate and/or reformulate [18F] fluorides without any evaporation step characterised in that the eluting solution is a ... [more ▼]

The present invention relates to a method to extract out of an aqueous solution, concentrate and/or reformulate [18F] fluorides without any evaporation step characterised in that the eluting solution is a organic solution having a water content <3%, containing at least: an organic solvent suitable for the subsequent radiolabelling reaction; a first compound (A) which is a molecule containing at least one acidic hydrogen and a second compound (B) which is an organic base sufficiently strong to be able to tear off the acidic hydrogen of first compound (A) in an acid-base reaction leading to the formation of an organic salt (S). [less ▲]

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See detailModified Non-Ionic Solid Supports: a Way to High Activity Fluorine-18 Radiochemistry in Microfluidic Devices
Aerts, Joël ULg; Voccia, Samuel; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 12

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See detailTertiary Alcohols to Avoid Evaporation in Fluorine-18 Labeling
Aerts, Joël ULg; Voccia, Samuel; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 204

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See detailNew Improvements in the Enantioselective Synthesis of 2-[18F]Fluoro-L-Tyrosine and 6-[18F]Fluoro-L-Dopa
Libert, Lionel ULg; Lemaire, Christian ULg; Denoël, Thibaut ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 196

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See detailAre Ionic Liquid Useful for Fluorine-18 Labeling?
Aerts, Joël ULg; Lemaire, Christian ULg; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 193

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See detailUse of Organic Bases for 18F-Fluoride Anion Exchange Elution avoiding the Classical Azeotropic drying Step Before Labeling
Lemaire, Christian ULg; Aerts, Joël ULg; Voccia, Samuel et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 198

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See detailMultivariate analysis of cognitive profiles in Alzheimer's disease
Bastin, Christine ULg; Leclercq, Yves ULg; Collette, Fabienne ULg et al

in Proceedings of the 8th bi-annual Meeting of the Belgian Society for Neuroscience (2009)

The neuropsychological profiles of patients with early Alzheimer’s disease (AD) appear to be heterogeneous. In this study, we examined whether this heterogeneity corresponds to the existence of ... [more ▼]

The neuropsychological profiles of patients with early Alzheimer’s disease (AD) appear to be heterogeneous. In this study, we examined whether this heterogeneity corresponds to the existence of cognitively distinct subtypes of AD or rather to impairments along a continuum of performances in different cognitive domains. A large group of 187 AD patients recruited in the European project NEST-DD performed a neuropsychological battery. A factor analysis of cognitive performance identified three factors, which respectively reflected attentional/instrumental function, declarative memory and executive function. Three clustering methods were applied on the factor scores in order to explore the existence of separate groups. The clustering methods indicated that cognitive profiles among the patients were sufficiently variable to identify clusters, but there was continuity between clusters rather than clear-cut subtypes. Moreover, clusters corresponded to various combinations of relatively impaired and preserved functions, suggesting multidimensional distribution within a large population of patients. Finally, clusters of cognitive profiles were characterized by different levels of metabolism in brain regions commonly (but variably) involved or relatively preserved in AD. [less ▲]

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See detailCombiner les mesures métaboliques cérébrales et neuropsychologiques permet une meilleure prédiction de la conversion vers une maladie d’Alzheimer chez les patients MCI
Bastin, Christine ULg; Adam, Stéphane ULg; LEKEU, Françoise ULg et al

in Revue Neurologique (2009), 165

Introduction. Une voie de recherche neurologique importante concerne la capacité de prédire sur base de l’évaluation initiale des patients avec Mild Cognitive Impairment (MCI) ceux qui vont développer une ... [more ▼]

Introduction. Une voie de recherche neurologique importante concerne la capacité de prédire sur base de l’évaluation initiale des patients avec Mild Cognitive Impairment (MCI) ceux qui vont développer une maladie d’Alzheimer (MA). Parmi les tests neuropsychologiques, le rappel indicé avec indiçage congruent lors de l’encodage et du rappel (RI48) apparaît comme le meilleur prédicteur du devenir des patients MCI (Ivanoiu et al., 2005). D’autre part, on a montré que les mesures métaboliques cérébrales (TEP-FDG), plus particulièrement l’hypométabolisme du cortex temporopariétal, prédit le déclin cognitif global dans le MCI mieux que des mesures neuropsychologiques (Chételat et al., 2005). Le but de notre étude était d’évaluer le pouvoir de prédiction pour la conversion du MCI vers une MA de deux prédicteurs robustes (performance au RI48 et métabolisme cérébral) pris soit isolément soit ensemble. Méthode. 50 patients MCI ont subi un examen en TEP-FDG au repos et ont réalisé le test de rappel indicé RI48 et le MMSE. Au terme d’un suivi neuropsychologique de 36 mois, 28 patients ont évolué vers une MA et 22 sont restés stables. Le métabolisme cérébral et les performances cognitives ont été comparés entre « convertisseurs » et MCI-stables. Des analyses discriminantes ont ensuite permis d’évaluer la capacité de classification de l’âge, du MMSE et des mesures métaboliques et mnésiques considérés individuellement ou selon diverses combinaisons. Résultat. Par comparaison avec les MCI-stables, les « convertisseurs » montraient un hypométabolisme du cortex temporal moyen bilatéralement, du cortex pariétal inférieur droit et du précuneus droit, et de plus faibles performances initiales au RI48. Prises individuellement, les différentes mesures permettaient le même taux de classification correcte (métabolisme cérébral = 76%, RI48 = 76%). L’âge et le MMSE étaient de faibles prédicteurs (exactitude de classification = 62% et 66% respectivement). Par contre, la combinaison des mesures métaboliques et des scores au RI48 prédisaient le mieux la progression vers la MA (88%). Conclusion. Les résultats suggèrent que la stratégie optimale pour identifier quels patients MCI ont plus de risque de développer une MA est de combiner les mesures métaboliques cérébrales et la performance à un test de mémoire très sensible. [less ▲]

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See detailMetabolism of no-carrier-added 2-[18F]fluoro-L-tyrosine in rats
Aerts, Joël ULg; Plenevaux, Alain ULg; Lemaire, Christian ULg et al

in BMC Medical Physics (2008), 8

Background: Several fluorine-18 labelled fluoroamino acids have been evaluated as tracers for the quantitative assessment of cerebral protein synthesis in vivo by positron emission tomography (PET). Among ... [more ▼]

Background: Several fluorine-18 labelled fluoroamino acids have been evaluated as tracers for the quantitative assessment of cerebral protein synthesis in vivo by positron emission tomography (PET). Among these, 2-[18F]fluoro-L-tyrosine (2-[18F]Tyr) has been studied in mice at a low specific activity. Its incorporation into proteins is fast and metabolism via other pathways is limited. The present in vivo study was carried out in normal awake rats using no-carrier-added 2-[18F]Tyr. Under normal physiological conditions, we have studied the incorporation into proteins and the metabolism of the tracer in different brain areas. Methods: No-carrier-added 2-[18F]Tyr was administered to awake rats equipped with chronic arterial and venous catheters. The time course of the plasma activity was studied by arterial blood sampling. The biodistribution of the activity in the main organs was studied at the end of the experiment. The distribution of radioactive species in plasma and brain regions was studied by acidic precipitation of the proteins and HPLC analysis of the supernatant. Results: The absolute uptake of radioactivity in brain regions was homogenous. In awake rats, nocarrier-added 2-[18F]Tyr exhibits a fast and almost quantitative incorporation into the proteins fractions of cerebellum and cortex. In striatum, this incorporation into proteins and the unchanged fraction of the tracer detected by HPLC could be lower than in other brain regions. Conclusion: This study confirms the potential of 2-[18F]fluoro-L-tyrosine as a tracer for the assessment of the rate of protein synthesis by positron emission tomography. The observed metabolism suggests a need for a correction for the appearance of metabolites, at least in plasma. [less ▲]

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See detailMethod for the preparation of reactive [18F]fluoride
Voccia, Samuel; Aerts, Joël ULg; Lemaire, Christian ULg et al

Patent (2008)

The invention is related to a method to obtain reactive [18F] fluorides in an org. medium suitable for radiolabeling without any azeotropic evapn. step, using a solid phase extn. column contg. a modified ... [more ▼]

The invention is related to a method to obtain reactive [18F] fluorides in an org. medium suitable for radiolabeling without any azeotropic evapn. step, using a solid phase extn. column contg. a modified non- ionic solid support. The SS is selected from extn. resins and liq. chromatog. resins comprising polar and nonpolar phases functionalized with or made of alkyl chains comprising 1 to 30 carbon atoms, polystyrene, cyclohexyl, poly(divinylbenzene)​, poly(styrene-​5-​divinylbenzene)​, Ph, polyamide, aminopropyl (NH2)​, cyanopropyl (CN)​, alcs. or diols, carboxymethyl, hydroxylated poly(styrene-​divinylbenzene)​, diethylaminoethyl, quaternary aminoethyl or sulfopropyl. Said vinyl comonomer is selected from the group consisting of vinylpyrrolidone, vinyl acetate, (methacryloyloxymethyl)​naphthalene, 4,​4'-​bis(maleimido)​diphenylmethane, p,​p'-​dihydroxydiphenylmethane diglycidylmethacrylic ester, p,​p'-​dihydroxydiphenylpropane diglycidylmethacrylic ester, 2-​hydroxyethyl methacrylate (HEMA)​, 2,​2-​dimethylaminoethyl methacrylate (DMAEMA)​, ethylenedimethacrylate glycidyl methacrylate, N-​vinylcarbazole, acrylonitrile, vinylpyridine, N-​methyl-​N-​vinylacetamide, aminostyrene, -​30-​Me acrylate, Et acrylate, Me methacrylate, N-​vinylcaprolactam, N-​methyl-​N-​vinylacetamide. Said metal salt cation is selected from the alkali group, preferably lithium, sodium, potassium, rubidium and cesium, the alk. earth metal group, preferably magnesium, calcium, strontium and barium, and the ammonium cation (NH4+)​; - said salt is selected from the group of halogenides, preferably fluor, chlor, brome, and iode, hydroxide, carbonates, phosphates, sulfates, carboxylates, acetate, alcoholates and perchlorate; - a complexing agent is selected from the group consisting of cryptands, including kryptofixs, such as 1,​4,​10-​Trioxa-​7,​13-​diazacyclopentadecane, 4,​7,​13,​16,​21,​24-​Hexaoxa-​1,​10-​diazabicyclo[8.8.8]​hexacosane, 4,​7,​13,​16,​21-​Pentaoxa-​1,​10-​diazabicyclo[8.8.5]​tricosane, 4,​7,​13,​18-​Tetraoxa-​1,​10-​diazabicyclo[8.5.5]​eicosane, 5,​6-​Benzo-​4,​7,​13,​16,​21,​24-​hexaoxa-​1,​10-​diazabicyclo[8.8.8]​hexacos-​5-​ene. [less ▲]

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See detailMethof for the elution of 18F fluoride trapped on an anion-exchange phase in a form suitable for efficient radiolabelling without any evaporation step
Aerts, Joël ULg; Lemaire, Christian ULg; Lignon, Steve et al

Patent (2008)

The invention relates to a method to ext. out of an aq. soln., conc. and​/or reformulate [18F] fluorides without any evapn. step, characterized in that the eluting soln. is a low water content, preferably ... [more ▼]

The invention relates to a method to ext. out of an aq. soln., conc. and​/or reformulate [18F] fluorides without any evapn. step, characterized in that the eluting soln. is a low water content, preferably <3​% water, org. soln. contg. at least: a first compd. (A) which is a tertiary alc.-​function bearing mol., a second compd. (B) which is a phase transfer agent suitable for radiolabeling and which is necessary to the anion exchange process. Said org. solvent is selected from acetonitrile (ACN)​, DMSO)​, dimethylacetamide, DMF, THF, di-​Et ether, dioxane, Et acetate, acetone, isobutyronitrile, benzonitrile, pyridine, di-​Et carbonate, sulfolane, hexamethylphosphotriamide (HMPA​/HMPT)​, and any mix of these solvents. Said nonpolar org. solvent is selected from pentane, hexane, heptane, octane, nonane, decane, and cyclohexane. [less ▲]

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See detailCyclosporine, a P-glycoprotein modulator, increases [18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies.
Lacan, Goran; Plenevaux, Alain ULg; Rubins, Daniel J. et al

in European Journal of Nuclear Medicine and Molecular Imaging (2008), 35(12), 2256-66

PURPOSE: Pretreatment with cyclosporine, a P-glycoprotein (P-gp) modulator increases brain uptake of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p-[(18)F]fluorobenzamido]ethylpiperaz ine ([(18)F]MPPF) for ... [more ▼]

PURPOSE: Pretreatment with cyclosporine, a P-glycoprotein (P-gp) modulator increases brain uptake of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p-[(18)F]fluorobenzamido]ethylpiperaz ine ([(18)F]MPPF) for binding to hydroxytryptamine(1A) (5-HT(1A)) receptors. Those increases were quantified in rat brain with in vivo microPET and ex vivo tissue studies. MATERIALS AND METHODS: Each Sprague-Dawley rat (n = 4) received a baseline [(18)F]MPPF microPET scan followed by second scan 2-3 weeks later that included cyclosporine pretreatment (50 mg/kg, i.p.). Maximum a posteriori reconstructed images and volumetric ROIs were used to generate dynamic radioactivity concentration measurements for hippocampus, striatum, and cerebellum, with simplified reference tissue method (SRTM) analysis. Western blots were used to semiquantify P-gp regional distribution in brain. RESULTS: MicroPET studies showed that hippocampus uptake of [(18)F]MPPF was increased after cyclosporine; ex vivo studies showed similar increases in hippocampus and frontal cortex at 30 min, and for heart and kidney at 2.5 and 5 min, without concomitant increases in [(18)F]MPPF plasma concentration. P-gp content in cerebellum was twofold higher than in hippocampus or frontal cortex. CONCLUSIONS: These studies confirm and extend prior ex vivo results (J. Passchier, et al., Eur J Pharmacol, 2000) that showed [(18)F]MPPF as a substrate for P-gp. Our microPET results showed that P-gp modulation of [(18)F]MPPF binding to 5-HT(1A) receptors can be imaged in rat hippocampus. The heterogeneous brain distribution of P-gp appeared to invalidate the use of cerebellum as a nonspecific reference region for SRTM modeling. Regional quantitation of P-gp may be necessary for accurate PET assessment of 5-HT(1A) receptor density when based on tracer uptake sensitive to P-gp modulation. [less ▲]

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See detailLes corrélats métaboliques des processus contrôlés en mémoire dans la maladie d'Alzheimer très débutante
Bastin, Christine ULg; Kerrouche, Nacer; Lekeu, Françoise ULg et al

in Ergis, Anne-Marie; Fiori, N.; Chaby, L. (Eds.) et al Xème colloque international sur le vieillissement cognitif (2008)

Les processus contrôlés et automatiques de récupération mnésique ont été évalués au moyen de la Procédure de Dissociation des Processus appliquée à une tâche de complètement de trigrammes chez 59 patients ... [more ▼]

Les processus contrôlés et automatiques de récupération mnésique ont été évalués au moyen de la Procédure de Dissociation des Processus appliquée à une tâche de complètement de trigrammes chez 59 patients diagnostiqués comme « questionable Alzheimer’s disease » (QAD ou Mild Cognitive Impairment). Par ailleurs, le métabolisme cérébral du glucose des patients a été mesuré par FDG-PET. Comparativement à des volontaires âgés sains appariés, le profil mnésique des patients QAD était caractérisé par un déficit des processus contrôlés, mais une préservation des processus automatiques. Après un suivi de 30 mois, 27 des patients ont développé une maladie d’Alzheimer, tandis que 23 patients restèrent des QAD stables (9 sujets n’ont pas complété le suivi ou ont reçu un autre diagnostic au terme de celui-ci). Les deux sous-groupes présentaient le même degré de déclin des processus de mémoire contrôlés. Des corrélations cognitivo-métaboliques, ainsi qu’une analyse en composantes principales, ont permis de montrer que les corrélats métaboliques des processus contrôlés (à l’entrée dans l’étude) n’étaient les mêmes chez les patients qui allaient développer la maladie d’Alzheimer et chez les patients qui allaient rester stables. Chez les patients qui développaient ultérieurement une maladie d’Alzheimer, l’utilisation correcte des processus contrôlés était positivement corrélée à l’activité du cortex préfrontal dorsomédian, qui pourrait jouer un rôle dans les processus réflexifs de monitoring agissant sur les produits de la récupération. L’activité du cortex préfrontal dorsomédian était corrélée à l’activité métabolique des régions frontales bilatérales et du cortex cingulaire postérieur. Par contraste, chez les patients QAD stables, nous avons trouvé une corrélation avec la formation hippocampique antérieure, une région qui intervient dans la réactivation de l’épisode d’encodage des événements. [less ▲]

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