Heric Valette

Summary

Country: France

Publications

  1. ncbi request reprint [18F]FPhEP and [18F]F2PhEP, two new epibatidine-based radioligands: evaluation for imaging nicotinic acetylcholine receptors in baboon brain
    Heric Valette
    CEA, Institut d Imagerie Biomédicale, Service Hospitalier Frederic Joliot, 4 Place du General Leclerc, F 91406 Orsay, France
    Synapse 61:764-70. 2007
  2. ncbi request reprint 18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboons
    Heric Valette
    CEA, I2BM, Service Hospitalier Frederic Joliot, LIME, Orsay, France
    J Nucl Med 50:1349-55. 2009
  3. ncbi request reprint Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[(11)C]one, as a potent NR(1A)/2B subtype selective NMDA PET radiotracer
    Gaelle Roger
    Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 11:5401-8. 2003
  4. ncbi request reprint Acute inhibition of cardiac monoamine oxidase A after tobacco smoke inhalation: validation study of [11C]befloxatone in rats followed by a positron emission tomography application in baboons
    Heric Valette
    Service Hospitalier Frederic Joliot, DSV DRM CEA, French Atomic Agency, F 91406 Orsay, France
    J Pharmacol Exp Ther 314:431-6. 2005
  5. pmc In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [(11)C]befloxatone and the multi-injection approach
    Michel Bottlaender
    CEA, DSV, I2BM, Service Hospitalier Frederic Joliot, 4, place du General Leclerc, F 91401 Orsay, France
    J Cereb Blood Flow Metab 30:792-800. 2010
  6. ncbi request reprint In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET
    Jean Dominique Gallezot
    Service Hospitalier Frederic Joliot, Département de Recherche Médicale Direction des Sciences du Vivant, Commissariat a l Energie Atomique, F 91406 Orsay, France
    J Nucl Med 46:240-7. 2005
  7. ncbi request reprint Synthesis and radiosynthesis of [(18)F]FPhEP, a novel alpha(4)beta(2)-selective, epibatidine-based antagonist for PET imaging of nicotinic acetylcholine receptors
    Gaelle Roger
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 14:3848-58. 2006
  8. ncbi request reprint Synthesis and in vivo imaging properties of [11C]befloxatone: a novel highly potent positron emission tomography ligand for mono-amine oxidase-A
    Frederic Dolle
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91406 Orsay, France
    Bioorg Med Chem Lett 13:1771-5. 2003
  9. ncbi request reprint Synthesis of a [2-pyridinyl-18F]-labelled fluoro derivative of (-)-cytisine as a candidate radioligand for brain nicotinic alpha4beta2 receptor imaging with PET
    Gaelle Roger
    Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 11:5333-43. 2003
  10. ncbi request reprint 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
    Bertrand Kuhnast
    Service Hospitalier Frederic Joliot, SHFJ CEA DSV, 4 Place du General Leclerc, 91401 Orsay, France
    Nucl Med Biol 33:785-95. 2006

Collaborators

Detail Information

Publications31

  1. ncbi request reprint [18F]FPhEP and [18F]F2PhEP, two new epibatidine-based radioligands: evaluation for imaging nicotinic acetylcholine receptors in baboon brain
    Heric Valette
    CEA, Institut d Imagerie Biomédicale, Service Hospitalier Frederic Joliot, 4 Place du General Leclerc, F 91406 Orsay, France
    Synapse 61:764-70. 2007
    ..In a displacement experiment with nicotine only a small amount of [(18)F]F(2)PhEP was dislodged. In spite of a moderate to high in vitro affinity, both ligands do not fulfill the widely adopted criteria for a PET radioligand...
  2. ncbi request reprint 18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboons
    Heric Valette
    CEA, I2BM, Service Hospitalier Frederic Joliot, LIME, Orsay, France
    J Nucl Med 50:1349-55. 2009
    ..Two halogeno-derivatives of A-85380 are being used in humans. Nevertheless, these derivatives still display too-slow brain kinetics and low signal-to-noise ratio...
  3. ncbi request reprint Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[(11)C]one, as a potent NR(1A)/2B subtype selective NMDA PET radiotracer
    Gaelle Roger
    Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 11:5401-8. 2003
    ..In view of these results, and especially considering the low brain penetration of the radiotracer, [(11)C]-1 does not have the required properties for imaging NMDA receptors using positron emission tomography...
  4. ncbi request reprint Acute inhibition of cardiac monoamine oxidase A after tobacco smoke inhalation: validation study of [11C]befloxatone in rats followed by a positron emission tomography application in baboons
    Heric Valette
    Service Hospitalier Frederic Joliot, DSV DRM CEA, French Atomic Agency, F 91406 Orsay, France
    J Pharmacol Exp Ther 314:431-6. 2005
    ..Cardiac MAO-A Bmax was quantified and a clear effect of acute inhalation of tobacco smoke was evidenced. Therefore, a single cigarette can interfere with the cardiac turnover of catecholamines...
  5. pmc In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [(11)C]befloxatone and the multi-injection approach
    Michel Bottlaender
    CEA, DSV, I2BM, Service Hospitalier Frederic Joliot, 4, place du General Leclerc, F 91401 Orsay, France
    J Cereb Blood Flow Metab 30:792-800. 2010
    ..The cerebellum presented the lowest binding site density (66+/-13 pmol/mL). Apparent affinity was found to be similar in all structures (K(d)V(R)=6.4+/-1.5 nmol/L). This study is the first PET-based estimation of the B(max) of an enzyme...
  6. ncbi request reprint In vivo imaging of human cerebral nicotinic acetylcholine receptors with 2-18F-fluoro-A-85380 and PET
    Jean Dominique Gallezot
    Service Hospitalier Frederic Joliot, Département de Recherche Médicale Direction des Sciences du Vivant, Commissariat a l Energie Atomique, F 91406 Orsay, France
    J Nucl Med 46:240-7. 2005
    ..The purpose of this study was to evaluate different strategies to quantify 2-(18)F-fluoro-A-85380 binding in healthy nonsmoking human volunteers...
  7. ncbi request reprint Synthesis and radiosynthesis of [(18)F]FPhEP, a novel alpha(4)beta(2)-selective, epibatidine-based antagonist for PET imaging of nicotinic acetylcholine receptors
    Gaelle Roger
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 14:3848-58. 2006
    ..Taken together, the preliminary data obtained confirm that [(18)F]FPhEP ([(18)F]-1) has potential for in vivo imaging nAChRs in the brain with PET...
  8. ncbi request reprint Synthesis and in vivo imaging properties of [11C]befloxatone: a novel highly potent positron emission tomography ligand for mono-amine oxidase-A
    Frederic Dolle
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91406 Orsay, France
    Bioorg Med Chem Lett 13:1771-5. 2003
    ....
  9. ncbi request reprint Synthesis of a [2-pyridinyl-18F]-labelled fluoro derivative of (-)-cytisine as a candidate radioligand for brain nicotinic alpha4beta2 receptor imaging with PET
    Gaelle Roger
    Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 11:5333-43. 2003
    ..These experiments clearly indicate that (-)-9-(2-[18F]fluoropyridinyl)cytisine ([18F]-3) does not have the required properties for imaging nAChRs using PET...
  10. ncbi request reprint 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
    Bertrand Kuhnast
    Service Hospitalier Frederic Joliot, SHFJ CEA DSV, 4 Place du General Leclerc, 91401 Orsay, France
    Nucl Med Biol 33:785-95. 2006
    ....
  11. doi request reprint Difficulties in dopamine transporter radioligand PET analysis: the example of LBT-999 using [18F] and [11C] labelling: part II: Metabolism studies
    Marie Anne Peyronneau
    CEA, I2BM, Service Hospitalier Frederic Joliot, F 91406 Orsay, France
    Nucl Med Biol 39:347-59. 2012
    ..Therefore, in vitro and in vivo metabolism of these radiotracers was investigated...
  12. ncbi request reprint Biodistribution and radiation dosimetry of 18F-fluoro-A-85380 in healthy volunteers
    Michel Bottlaender
    Department of Medical Research, Division of Life Sciences, Service Hospitalier Frederic Joliot, French Atomic Agency, 4 Place du General Leclerc, F 91406 Orsay, France
    J Nucl Med 44:596-601. 2003
    ..This study reports on the biodistribution and radiation dosimetry of 2-(18)F-Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine ((18)F-fluoro-A-85380), a promising radioligand for the imaging of central nicotinic acetylcholine receptors (nAChRs)...
  13. ncbi request reprint Synthesis of a fluorine-18-labelled derivative of 6-nitroquipazine, as a radioligand for the in vivo serotonin transporter imaging with PET
    Mylène Karramkam
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA, 4 Place du General Leclerc, F 91401 Orsay, France
    Bioorg Med Chem 10:2611-23. 2002
    ....
  14. ncbi request reprint [11C]LBT-999: a suitable radioligand for investigation of extra-striatal dopamine transporter with PET
    Wadad Saba
    CEA, Service Hospitalier Frederic Joliot, DRM DSV, Orsay, France
    Synapse 61:17-23. 2007
    ....
  15. doi request reprint Difficulties in dopamine transporter radioligand PET analysis: the example of LBT-999 using [18F] and [11C] labelling Part I: PET studies
    Wadad Saba
    CEA, I2BM, Service Hospitalier Frederic Joliot, 4 Place du General Leclerc, F 91401 Orsay, France
    Nucl Med Biol 39:227-33. 2012
    ..18)F]LBT-999 was first labelled with carbon-11; we will now describe its in vivo behaviour in comparison to that of [(11)C]LBT-999...
  16. doi request reprint [(11)C]SL25.1188, a new reversible radioligand to study the monoamine oxidase type B with PET: preclinical characterisation in nonhuman primate
    Wadad Saba
    CEA, DSV, I2BM, Service Hospitalier Frederic Joliot, Orsay F 91401, France
    Synapse 64:61-9. 2010
    ..Therefore, [(11)C]SL25.1188 is characterized in vivo by reversible binding, high brain uptake and very slow plasma metabolism, strongly suggesting that this radioligand is a potent tool for the in vivo study of brain MAO-B...
  17. ncbi request reprint Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeys
    Heric Valette
    Service Hospitalier Frederic Joliot, Department of Medical Research French Atomic Agency, Orsay, France
    Synapse 44:58-9. 2002
  18. pmc Effects of selected OATP and/or ABC transporter inhibitors on the brain and whole-body distribution of glyburide
    Nicolas Tournier
    CEA, DSV, I2BM, Service Hospitalier Frederic Joliot, Orsay, 91401, France
    AAPS J 15:1082-90. 2013
    ..Conversely, P-gp, BCRP, and probably multidrug resistance protein 4 work in synergy to limit GLB brain uptake. ..
  19. ncbi request reprint Quantification of cerebral nicotinic acetylcholine receptors by PET using 2-[18F]fluoro-A-85380 and the multiinjection approach
    Jean Dominique Gallezot
    Service Hospitalier Frederic Joliot, I2BM, DSV, CEA, Orsay, France
    J Cereb Blood Flow Metab 28:172-89. 2008
    ..The ratio of radioligand concentration in these two compartments then overestimates the true equilibrium value, an unfavorable situation to estimate distribution volumes from late images after a bolus injection...
  20. ncbi request reprint Radiosynthesis of (E)-N-(2-[11C]methoxybenzyl)-3-phenyl-acrylamidine, a novel subnanomolar NR2B subtype-selective NMDA receptor antagonist
    Cyrille Thominiaux
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, 4 Place du General Leclerc, F 91401 Orsay, France
    Appl Radiat Isot 64:348-54. 2006
    ..8 to 1.2 Ci/micromol (29.6-44.4 GBq/micromol) at the end of radiosynthesis. No attempts were made to further optimise these reactions, as sufficient material was obtained to allow for preliminary pharmacological characterisation...
  21. doi request reprint Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand
    Marie Anne Peyronneau
    CEA, DSV, I2BM, Service Hospitalier Frederic Joliot, 4 Place du General Leclerc, 91406 Orsay, France
    Drug Metab Dispos 41:122-31. 2013
    ..The main route of excretion of the unchanged radioligand in baboons was hepatobiliary while that of radiometabolites was the urinary system...
  22. doi request reprint Discrepancies in the P-glycoprotein-mediated transport of (18)F-MPPF: a pharmacokinetic study in mice and non-human primates
    Nicolas Tournier
    CEA, I2BM, Service Hospitalier Frederic Joliot, Orsay 91401, France
    Pharm Res 29:2468-76. 2012
    ..However, in vitro assays suggest that MPPF is not a substrate of human P-gp. We have now tested the influence of inhibiting P-gp on the brain kinetics of (18)F-MPPF in mice and non-human primates...
  23. ncbi request reprint Long-lasting occupancy of central nicotinic acetylcholine receptors after smoking: a PET study in monkeys
    Heric Valette
    Service Hospitalier Frederic Joliot, DRM DSV CEA, Orsay, France
    J Neurochem 84:105-11. 2003
    ..No significant effect was observed following 0.15 mg nornicotine. Therefore, nornicotine could contribute to the long-lasting occupancy of central nAChRs after smoking...
  24. doi request reprint Decrease of nicotinic receptors in the nigrostriatal system in Parkinson's disease
    Aurélie Kas
    URA CNRS CEA 2210, MIRCen, I2BM DSV, Orsay, France
    J Cereb Blood Flow Metab 29:1601-8. 2009
    ..05) decrease of 2-[(18)F]fluoro-A-85380 DV in the striatum (-10%) and substantia nigra (-14.9%) in PD patients. Despite the wide range of PD stages, no correlation was found between DV and the clinical and PET markers of PD severity...
  25. ncbi request reprint Acute effects of physostigmine and galantamine on the binding of [18F]fluoro-A-85380: a PET study in monkeys
    Heric Valette
    Service Hospitalier Frederic Joliot, Direction of Life Sciences, Department of Medical Research, French Atomic Agency, Orsay, France
    Synapse 56:217-21. 2005
    ....
  26. doi request reprint [(18)F]Fallypride: metabolism studies and quantification of the radiotracer and its radiometabolites in plasma using a simple and rapid solid-phase extraction method
    Marie Anne Peyronneau
    CEA, I2BM, Service Hospitalier Frederic Joliot, F 91406 Orsay, France Electronic address
    Nucl Med Biol 40:887-95. 2013
    ....
  27. ncbi request reprint Mapping the cerebral monoamine oxidase type A: positron emission tomography characterization of the reversible selective inhibitor [11C]befloxatone
    Michel Bottlaender
    Commissariat a l Energie Atomique, Service Hospitalier Frederic Joliot, Département de Recherche Médicale Direction des Sciences du Vivant, Orsay, France
    J Pharmacol Exp Ther 305:467-73. 2003
    ..02 mg/kg for all studied structures. These results indicate that [(11)C]befloxatone will be an excellent probe for the study of MAO-A in humans using PET...
  28. ncbi request reprint Synthesis, radiosynthesis and in vivo preliminary evaluation of [11C]LBT-999, a selective radioligand for the visualisation of the dopamine transporter with PET
    Frederic Dolle
    Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, Orsay, France
    Bioorg Med Chem 14:1115-25. 2006
    ....
  29. ncbi request reprint Fluoro-A-85380 demonstrated no mutagenic properties in in vivo rat micronucleus and Ames tests
    Heric Valette
    Service Hospitalier Frederic Joliot, CEA, DSV DRM, 4 Place du General Leclerc, F 91406, Orsay, France
    Nucl Med Biol 29:849-53. 2002
    ..No biologically significant increase in the mean number of revertants was noted in all the Salmonella typhimurium strains tested with fluoro-A-85380. Therefore, fluoro-A-85380 demonstrated no mutagenic properties using these two tests...
  30. doi request reprint Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening
    Nicolas Tournier
    CEA, I2BM, Service Hospitalier Frederic Joliot, Orsay, France
    J Nucl Med 52:415-23. 2011
    ..Efflux transporters at the BBB-P-glycoprotein (P-gp) and the breast cancer resistance protein (BCRP)-could limit their uptake by the brain...
  31. ncbi request reprint In vivo quantification of myocardial dihydropyridine binding sites: a PET study in dogs
    Heric Valette
    Department of Medical Research, Direction of Life Sciences, Service Hospitalier Frederic Joliot, French Atomic Agency, Orsay, France
    J Nucl Med 43:1227-33. 2002
    ..In vivo quantification of the density of these channels using PET and an adequate ligand would provide new insights into cardiac disease...