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210 results on '"Valette, Héric"'

11. Synthesis, radiosynthesis and in vivo preliminary evaluation of [ 11C]LBT-999, a selective radioligand for the visualisation of the dopamine transporter with PET

Author

Dollé, Frédéric, Emond, Patrick, Mavel, Sylvie, Demphel, Stéphane, Hinnen, Françoise, Mincheva, Zoïa, Saba, Wadad, Valette, Heric, Chalon, Sylvie, Halldin, Christer, Helfenbein, Julie, Legaillard, Joël, Madelmont, Jean-Claude, Deloye, Jean-Bernard, Bottlaender, Michel, and Guilloteau, Denis

Published
2006
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18. Synthesis of a [2- Pyridinyl- 18F]-labelled fluoro derivative of (−)-Cytisine as a candidate radioligand for brain nicotinic α4β2 receptor imaging with PET

Author

Roger, Gaëlle, Lagnel, Béatrice, Rouden, Jacques, Besret, Laurent, Valette, Héric, Demphel, Stéphane, Gopisetti, JaganMohan, Coulon, Christine, Ottaviani, Michele, Wrenn, Lori A, Letchworth, Sharon R, Bohme, Georg A, Benavides, Jesus, Lasne, Marie-Claire, Bottlaender, Michel, and Dollé, Frédéric

Published
2003
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24. Differential influence of propofol and isoflurane anesthesia in non-human primate on the brain kinetics and binding of [$^{18}$F]DPA-714, a PET imaging marker of glial activation

Author

Saba, Wadad, Goutal, Sébastien, Kuhnast, Bertrand, Dollé, Frédéric, Auvity, Sylvain, Fontyn, Yoan, Cayla, Jérôme, Peyronneau, Marie-Anne, Valette, Héric, Tournier, Nicolas, Imagerie Moléculaire in Vivo (IMIV - U1023 - ERL9218), Service Hospitalier Frédéric Joliot (SHFJ), Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS)-Institut National de la Santé et de la Recherche Médicale (INSERM), Université Paris-Saclay, Université Paris-Saclay-Direction de Recherche Fondamentale (CEA) (DRF (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), and Tournier, Nicolas

Subjects
[SDV] Life Sciences [q-bio], in vitro binding, positron emission tomography, baboon, anesthetic, [SDV.SP.PHARMA] Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology, [SDV]Life Sciences [q-bio], [SDV.NEU.NB]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology, [SDV.NEU.NB] Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology, peripheral benzodiazepine receptor, [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology, neuroinflammation
Abstract

International audience; Translocator protein 18 kDa (TSPO) expression at the mitochondrial membrane of glial cells is related to glial activation. TSPO radioligands such as [$^{18}$F]DPA‐714 are useful for the non‐invasive study of neuroimmune processes using positron emission tomography (PET). Anesthetic agents were shown to impact mitochondrial function and may influence [$^{18}$F]DPA‐714 binding parameters and PET kinetics. [$^{18}$F]DPA‐714 PET imaging was performed in $Papio\ anubis$ baboons anesthetized using either intravenous propofol ($n$ = 3) or inhaled isoflurane ($n$ = 3). Brain kinetics and metabolite‐corrected input function were measured to estimate [$^{18}$F]DPA‐714 brain distribution ($V_T$). Displacement experiments were performed using PK11195 (1.5 mg/kg). In vitro [$^{18}$F]DPA‐714 binding experiments were performed using baboon brain tissue in the absence and presence of tested anesthetics. Brain radioactivity peaked higher in isoflurane‐anesthetized animals compared with propofol (SUVmax = 2.7 ± 0.5 vs. 1.3 ± 0.2, respectively) but was not different after 30 min. Brain $V_T$ was not different under propofol and isoflurane. Displacement resulted in a 35.8 ± 8.4% decrease of brain radioactivity under propofol but not under isoflurane (0.1 ± 7.0%). In vitro, the presence of propofol increased TSPO density and dramatically reduced its affinity for [$^{18}$F]DPA‐714 compared with control. This in vitro effect was not significant with isoflurane. Exposure to propofol and isoflurane differentially influences TSPO interaction with its specific radioligand [$^{18}F$]DPA‐714 with subsequent impact on its tissue kinetics and specific binding estimated in vivo using PET. Therefore, the choice of anesthetics and their potential influence on PET data should be considered for the design of imaging studies using TSPO radioligands, especially in a translational research context.

Published
2015

32. Transport of Selected PET Radiotracers by Human P-Glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2): An In Vitro Screening

Author

Tournier, Nicolas, primary, Valette, Héric, additional, Peyronneau, Marie-Anne, additional, Saba, Wadad, additional, Goutal, Sébastien, additional, Kuhnast, Bertrand, additional, Dollé, Frédéric, additional, Scherrmann, Jean-Michel, additional, Cisternino, Salvatore, additional, and Bottlaender, Michel, additional

Published
2011
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36. 18F-ZW-104: A New Radioligand for Imaging Neuronal Nicotinic Acetylcholine Receptors—In Vitro Binding Properties and PET Studies in Baboons

Author

Valette, Héric, primary, Xiao, Yingxiang, additional, Peyronneau, Marie-Anne, additional, Damont, Annelaure, additional, Kozikowski, Alan P., additional, Wei, Zhi-Liang, additional, Kassiou, Michael, additional, Kellar, Kenneth J., additional, Dollé, Frédéric, additional, and Bottlaender, Michel, additional

Published
2009
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38. Quantification of Cerebral Nicotinic Acetylcholine Receptors by PET Using 2-[18F]Fluoro-A-85380 and the Multiinjection Approach

Author

Gallezot, Jean-Dominique, primary, Bottlaender, Michel A, additional, Delforge, Jacques, additional, Valette, Héric, additional, Saba, Wadad, additional, Dollé, Frédéric, additional, Coulon, Christine M, additional, Ottaviani, Michèle P, additional, Hinnen, Françoise, additional, Syrota, André, additional, and Grégoire, Marie-Claude, additional

Published
2007
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39. Differential influence of propofol and isoflurane anesthesia in a non-human primate on the brain kinetics and binding of [18F] DPA-714, a positron emission tomography imaging marker of glial activation.

Author

Saba, Wadad, Goutal, Sébastien, Kuhnast, Bertrand, Dollé, Frédéric, Auvity, Sylvain, Fontyn, Yoan, Cayla, Jérôme, Peyronneau, Marie‐Anne, Valette, Héric, and Tournier, Nicolas

Subjects
PROPOFOL, DRUG efficacy, ISOFLURANE, ANESTHESIA, POSITRON emission tomography, PRIMATES, BIOMARKERS, NEUROGLIA, THERAPEUTICS
Abstract

Translocator protein 18 kDa ( TSPO) expression at the mitochondrial membrane of glial cells is related to glial activation. TSPO radioligands such as [18F] DPA-714 are useful for the non-invasive study of neuroimmune processes using positron emission tomography ( PET). Anesthetic agents were shown to impact mitochondrial function and may influence [18F] DPA-714 binding parameters and PET kinetics. [18F] DPA-714 PET imaging was performed in Papio anubis baboons anesthetized using either intravenous propofol ( n = 3) or inhaled isoflurane ( n = 3). Brain kinetics and metabolite-corrected input function were measured to estimate [18F] DPA-714 brain distribution ( VT). Displacement experiments were performed using PK11195 (1.5 mg/kg). In vitro [18F] DPA-714 binding experiments were performed using baboon brain tissue in the absence and presence of tested anesthetics. Brain radioactivity peaked higher in isoflurane-anesthetized animals compared with propofol ( SUVmax = 2.7 ± 0.5 vs. 1.3 ± 0.2, respectively) but was not different after 30 min. Brain VT was not different under propofol and isoflurane. Displacement resulted in a 35.8 ± 8.4% decrease of brain radioactivity under propofol but not under isoflurane (0.1 ± 7.0%). In vitro, the presence of propofol increased TSPO density and dramatically reduced its affinity for [18F] DPA-714 compared with control. This in vitro effect was not significant with isoflurane. Exposure to propofol and isoflurane differentially influences TSPO interaction with its specific radioligand [18F] DPA-714 with subsequent impact on its tissue kinetics and specific binding estimated in vivo using PET. Therefore, the choice of anesthetics and their potential influence on PET data should be considered for the design of imaging studies using TSPO radioligands, especially in a translational research context. [ABSTRACT FROM AUTHOR]

Published
2015
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40. Influence of P-Glycoprotein Inhibition or Deficiency at the Blood-Brain Barrier on F-2-Fluoro-2-Deoxy- d-glucose (F-FDG) Brain Kinetics.

Author

Tournier, Nicolas, Saba, Wadad, Goutal, Sébastien, Gervais, Philippe, Valette, Héric, Scherrmann, Jean-Michel, Bottlaender, Michel, and Cisternino, Salvatore

Abstract

The fluorinated d-glucose analog F-2-fluoro-2-deoxy- d-glucose (F-FDG) is the most prevalent radiopharmaceutical for positron emission tomography (PET) imaging. P-Glycoprotein's (P-gp, MDR1, and ABCB1) function in various cancer cell lines and tumors was shown to impact F-FDG incorporation, suggesting that P-gp function at the blood-brain barrier may also modulate F-FDG brain kinetics. We tested the influence of P-gp inhibition using the cyclosporine analog valspodar (PSC833; 5 μM) on the uptake of F-FDG in standardized human P-gp-overexpressing cells (MDCKII-MDR1). Consequences for F-FDG brain kinetics were then assessed using (i) F-FDG PET imaging and suitable kinetic modelling in baboons without or with P-gp inhibition by intravenous cyclosporine infusion (15 mg kg h) and (ii) in situ brain perfusion in wild-type and P-gp/Bcrp (breast cancer resistance protein) knockout mice and controlled d-glucose exposure to the brain. In vitro, the time course of F-FDG uptake in MDR1 cells was influenced by the presence of valspodar in the absence of d-glucose but not in the presence of high d-glucose concentration. PET analysis revealed that P-gp inhibition had no significant impact on estimated brain kinetics parameters K, k, k, V, and CMR. The lack of P-gp effect on in vivoF-FDG brain distribution was confirmed in P-gp/Bcrp-deficient mice. P-gp inhibition indirectly modulates F-FDG uptake into P-gp-overexpressing cells, possibly through differences in the energetic cell level state. F-FDG is not a P-gp substrate at the BBB and F-FDG brain kinetics as well as estimated brain glucose metabolism are influenced by neither P-gp inhibition nor P-gp/Bcrp deficiencies in baboon and mice, respectively. [ABSTRACT FROM AUTHOR]

Published
2015
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41. Synthesis and radiolabeling of N-[4-[4-(2-[11C]methoxyphenyl)piperazin-1-yl]butyl]benzo[b]thiophene-2-carboxamide — a potential radiotracer for D3 receptor imaging with PET

Author

Kuhnast, Bertrand, primary, Valette, Héric, additional, Besret, Laurent, additional, Demphel, Stéphane, additional, Coulon, Christine, additional, Ottaviani, Michèle, additional, Guillermier, Martine, additional, Bottlaender, Michel, additional, and Dollé, Frédéric, additional

Published
2006
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44. [11C]LBT-999: A suitable radioligand for investigation of extra-striatal dopamine transporter with PET

Author

Saba, Wadad, primary, Valette, Héric, additional, Schöllhorn-Peyronneau, Marie-Anne, additional, Coulon, Christine, additional, Ottaviani, Michele, additional, Chalon, Sylvie, additional, Dolle, Frédéric, additional, Emond, Patrick, additional, Halldin, Christer, additional, Helfenbein, Julie, additional, Madelmont, Jean-Claude, additional, Deloye, Jean-Bernard, additional, Guilloteau, Denis, additional, and Bottlaender, Michel, additional

Published
2006
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45. Quantification in vivo of nicotinic acetylcholine receptors density and affinity in the baboon brain using 2-[18F]fluoro-A-85380 and a multi-injection approach

Author

Gallezot, Jean-Dominique, primary, Grégoire, Marie-Claude, additional, Bottlaender, Michel, additional, Frédéric, Dollé, additional, Wadad, Saba, additional, Coulon, Christine, additional, Ottaviani, Michèle, additional, Delforge, Jacques, additional, Syrota, André, additional, and Valette, Héric, additional

Published
2005
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49. Synthesis, radiosynthesis and In vivo evaluation of 5-[3-(4-Benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[11C]one, as a potent NR1A/2B subtype selective NMDA PET radiotracer

Author

Roger, Gaëlle, primary, Lagnel, Béatrice, additional, Besret, Laurent, additional, Bramoullé, Yann, additional, Coulon, Christine, additional, Ottaviani, Michelle, additional, Kassiou, Michael, additional, Bottlaender, Michel, additional, Valette, Héric, additional, and Dollé, Frédéric, additional

Published
2003
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50. Synthesis and in vivo imaging properties of [11C]befloxatone: A novel highly potent positron emission tomography ligand for mono-amine oxidase-A

Author

Dolle, Frédéric, primary, Valette, Héric, additional, Bramoulle, Yann, additional, Guenther, Ilonka, additional, Fuseau, Chantal, additional, Coulon, Christine, additional, Lartizien, Carole, additional, Jegham, Samir, additional, George, Pascal, additional, Curet, Olivier, additional, Pinquier, Jean-Louis, additional, and Bottlaender, Michel, additional

Published
2003
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