Research Topics
Species | Heric ValetteSummaryCountry: France Publications
| Collaborators
|
Detail Information
Publications
18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboonsHeric 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...
[18F]FPhEP and [18F]F2PhEP, two new epibatidine-based radioligands: evaluation for imaging nicotinic acetylcholine receptors in baboon brainHeric 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...- 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 radiotracerGaelle 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... 
In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [(11)C]befloxatone and the multi-injection approachMichel 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...- 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 baboonsHeric 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... - Synthesis and radiosynthesis of [(18)F]FPhEP, a novel alpha(4)beta(2)-selective, epibatidine-based antagonist for PET imaging of nicotinic acetylcholine receptorsGaelle 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... - Synthesis and in vivo imaging properties of [11C]befloxatone: a novel highly potent positron emission tomography ligand for mono-amine oxidase-AFrederic 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.... - Difficulties in dopamine transporter radioligand PET analysis: the example of LBT-999 using [18F] and [11C] labelling: part II: Metabolism studiesMarie 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... - Anesthesia affects the disposition of [18F]fluoro-A-85380: a PET study in monkeysHeric Valette
Service Hospitalier Frederic Joliot, Department of Medical Research French Atomic Agency, Orsay, France
Synapse 44:58-9. 2002 - Synthesis of a [2-pyridinyl-18F]-labelled fluoro derivative of (-)-cytisine as a candidate radioligand for brain nicotinic alpha4beta2 receptor imaging with PETGaelle 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... - Difficulties in dopamine transporter radioligand PET analysis: the example of LBT-999 using [18F] and [11C] labelling Part I: PET studiesWadad 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... - [(11)C]SL25.1188, a new reversible radioligand to study the monoamine oxidase type B with PET: preclinical characterisation in nonhuman primateWadad 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... - [11C]LBT-999: a suitable radioligand for investigation of extra-striatal dopamine transporter with PETWadad Saba
CEA, Service Hospitalier Frederic Joliot, DRM DSV, Orsay, France
Synapse 61:17-23. 2007.... - Discrepancies in the P-glycoprotein-mediated transport of (18)F-MPPF: a pharmacokinetic study in mice and non-human primatesNicolas 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... - Long-lasting occupancy of central nicotinic acetylcholine receptors after smoking: a PET study in monkeysHeric 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... - Decrease of nicotinic receptors in the nigrostriatal system in Parkinson's diseaseAurélie 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... - Acute effects of physostigmine and galantamine on the binding of [18F]fluoro-A-85380: a PET study in monkeysHeric Valette
Service Hospitalier Frederic Joliot, Direction of Life Sciences, Department of Medical Research, French Atomic Agency, Orsay, France
Synapse 56:217-21. 2005.... - Quantification of cerebral nicotinic acetylcholine receptors by PET using 2-[18F]fluoro-A-85380 and the multiinjection approachJean 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... - Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligandMarie 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... - Synthesis of a fluorine-18-labelled derivative of 6-nitroquipazine, as a radioligand for the in vivo serotonin transporter imaging with PETMylène 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.... - Mapping the cerebral monoamine oxidase type A: positron emission tomography characterization of the reversible selective inhibitor [11C]befloxatoneMichel 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... - Synthesis, radiosynthesis and in vivo preliminary evaluation of [11C]LBT-999, a selective radioligand for the visualisation of the dopamine transporter with PETFrederic Dolle
Service Hospitalier Frederic Joliot, Departement de Recherche Medicale, CEA DSV, Orsay, France
Bioorg Med Chem 14:1115-25. 2006.... - Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screeningNicolas 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... - Fluoro-A-85380 demonstrated no mutagenic properties in in vivo rat micronucleus and Ames testsHeric 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... - In vivo quantification of myocardial dihydropyridine binding sites: a PET study in dogsHeric 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...