Research Topics
Species | S ChalonSummaryCountry: France Publications
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Publications
Hypoxic preconditioning reduces apoptosis in a rat model of immature brain hypoxia-ischaemiaSylvain Cantagrel
INSERM U 316, UFR des Sciences Pharmaceutiques, Tours, France
Neurosci Lett 347:106-10. 2003..We demonstrated here that regulation of apoptotic cell death is one of the mechanisms involved in tolerance to hypoxia-ischaemia induced by hypoxic preconditioning...
Pharmacological characterization of N,N-dimethyl-2-(2-amino-4-methylphenyl thio)benzylamine as a ligand of the serotonin transporter with high affinity and selectivitySylvie Chalon
Institut National de la Sante et de la Recherche Medicale U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, Tours, France
J Pharmacol Exp Ther 304:81-7. 2003....
Pharmacological characterization of (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)n ortropane as a selective and potent inhibitor of the neuronal dopamine transporterS Chalon
Institut National de la Sante et de la Recherche Medicale U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Tours, France
J Pharmacol Exp Ther 291:648-54. 1999..All of these findings, combined with previously published data, support the use of PE2I as a selective and potent tool to study the DAT both in vivo and in vitro...
Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl)nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporterSylvie Chalon
Institut National de la Sante et de la Recherche Medicale U619, Tours, France
J Pharmacol Exp Ther 317:147-52. 2006..Taken together, these findings demonstrate that LBT-999 is a highly promising agent for in vivo exploration of the DAT. This probe is currently labeled with (18)F for further characterizations...
ADAM is an effective tool for in vivo study of serotonergic function: validation in rat modelsSylvie Chalon
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, UFR des Sciences Pharmaceutiques, 37200 Tours, France
Synapse 52:136-42. 2004....
Polyunsaturated fatty acids and cerebral function: focus on monoaminergic neurotransmissionS Chalon
INSERM U316, Laboratoire Biophysique Médicale et Pharmaceutique, Universite Francois Rabelais, 37200 Tours, France
Lipids 36:937-44. 2001..Animal models are tools of choice for the understanding of such links. Improved prevention and complementary treatment of neurological and psychiatric diseases can be expected from these studies...
Time course of changes in striatal dopamine transporters and D2 receptors with specific iodinated markers in a rat model of Parkinson's diseaseS Chalon
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Tours, France
Synapse 31:134-9. 1999..The exploration of both DAT and D2R would improve follow-up of this disease...
A selective radiobrominated cocaine analogue for imaging of dopamine uptake sites: pharmacological evaluation and PET experimentsJ Helfenbein
INSERM U316 Laboratoire de Biophysique Médicale et Pharmaceutique, Tours, France
Life Sci 65:2715-26. 1999..These results showed that [76Br]PE2Br is in vivo a potent and selective radioligand suitable for PET imagingof the dopamine transporter...
Synthesis and in vitro binding properties of halogenated analogues of GBR as new dopamine uptake carrier ligandsC Foulon
INSERM U 316, Tours, France
Int J Rad Appl Instrum B 19:597-600. 1992..We prepared iodo-GBR labeled with iodide-125 from the brominated derivative and concluded that [123I]iodo-GBR could be a potential tool to explore the in vivo dopamine uptake carrier...
Synthesis of tropane and nortropane analogues with phenyl substitutions as serotonin transporter ligandsP Emond
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, 31 Avenue Monge, 37200 Tours, France
Bioorg Med Chem 9:1849-55. 2001....
Neuroprotection of nerve growth factor-loaded microspheres on the D2 dopaminergic receptor positive-striatal neurones in quinolinic acid-lesioned rats: a quantitative autoradiographic assessment with iodobenzamideC Gouhier
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, UFR des Sciences Pharmaceutiques, Tours, France
Neurosci Lett 288:71-5. 2000..Moreover, tolerance of microspheres was demonstrated by in vitro autoradiography with the marker of gliosis, [(3)H]-PK 11195...
Iodobenzamide for in vivo exploration of central dopamine receptors: evaluation in animal models of supersensitivityS Chalon
INSERM U316, Laboratoire de Biophysique Medicale, Tours, France
Life Sci 47:729-34. 1990..Thus IBZM labelled with 123I can be a very useful imaging agent for the exploration of D2 receptors in pathological situations...
mRNA D(2) dopaminergic receptor expression after hypoxia-ischemia in rat immature brainS Cantagrel
INSERM U316, Faculte de Pharmacie, Tours, France
Biol Neonate 80:68-73. 2001..The early decrease in mRNA D(2)R could explain the delayed reduced D(2)R after neonatal hypoxia-ischemia...
MPTP intoxication in mice: a useful model of Leigh syndrome to study mitochondrial diseases in childhoodE Lagrue
Unité Imagerie et Cerveau, INSERM, U930, Tours, France
Metab Brain Dis 24:321-35. 2009..01). Taken together, these results confirm that acute MPTP intoxication in young mice provides a reproducible pharmacological paradigm of LS, thus opening new avenues for neuroprotection research...
PET and SPECT exploration of central monoaminergic transporters for the development of new drugs and treatments in brain disordersD Guilloteau
INSERM U619, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, Tours, France
Curr Pharm Des 11:3237-45. 2005....
Spatio-temporal diffusion of dynamic PET imagesC Tauber
INSERM U930, CNRS ERL3106, Universite Francois Rabelais, Tours, France
Phys Med Biol 56:6583-96. 2011..Our simulations suggest that the proposed method can be used to significantly increase the signal-to-noise ratio in dynamic PET imaging...
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligandsJohnny Vercouillie
, INSERM U619, , 31 Avenue Monge, 37200 Tours, France
Bioorg Med Chem Lett 16:1297-300. 2006..Three of these exhibited good to high in vitro affinity (0.5 nM < K(i) < 11 nM) and selectivity for the SERT over the other monoamine transporters...
Maternal exposure to LPS induces hypomyelination in the internal capsule and programmed cell death in the deep gray matter in newborn ratsCatherine I Rousset
INSERM U619, 37000 Tours, France
Pediatr Res 59:428-33. 2006..This model should be relevant for the study of the pathophysiological mechanisms involved in cerebral white matter damage in preterm human newborns and in the development of therapeutic strategies...
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....
Omega-3 fatty acids and monoamine neurotransmissionSylvie Chalon
INSERM U619, Tours, France
Prostaglandins Leukot Essent Fatty Acids 75:259-69. 2006....
Cerebral asymmetry and behavioral lateralization in rats chronically lacking n-3 polyunsaturated fatty acidsSylvie Vancassel
INRA Laboratoire de Nutrition et Sécurité Alimentaire, Jouy en Josas, France
Biol Psychiatry 58:805-11. 2005....
[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....
Lamotrigine is neuroprotective in the energy deficiency model of MPTP intoxicated miceEmmanuelle Lagrue
INSERM, U619, Tours, F 37000 France
Pediatr Res 62:14-9. 2007..Lamotrigine, a widely used and well-tolerated molecule in young patients, could represent a valuable adjuvant therapy in various energy deficiency conditions during childhood...
Ex vivo and in vivo evaluation of (2R,3R)-5-[(18)F]-fluoroethoxy- and fluoropropoxy-benzovesamicol, as PET radioligands for the vesicular acetylcholine transporterNicolas Giboureau
INSERM, U619, 37000 Tours, France
Synapse 61:962-70. 2007..The in vivo PET study of [(18)F]2 performed in baboon also revealed rapid defluorination as the main problem. Therefore [(18)F]1 and [(18)F]2 appear to be unsuitable for in vivo imaging of the VAChT using PET...
(E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporterPatrick Emond
INSERM U619, 37000 Tours, France
Nucl Med Biol 34:967-71. 2007..These results made [125I]-( R,R)-5-AOIBV inferior to [125I]-IBVM for the VAChT exploration in vivo...
Improved synthesis and metabolic stability analysis of the dopamine transporter ligand [(18)F]FECTSatish K Chitneni
Laboratory for Radiopharmacy, Faculty of Pharmaceutical Sciences, Katholieke Universiteit Leuven, BE 3000, Leuven, Belgium
Nucl Med Biol 35:75-82. 2008..We report an improved radiosynthesis procedure and affinity data and have analyzed both brain tissue and plasma samples for the presence of radiometabolites as a function of time post intravenous injection of [(18)F]FECT to rats...
IMPY, a potential beta-amyloid imaging probe for detection of prion deposits in scrapie-infected micePu Jiao Song
INSERM, U619, F 37000 Tours, France
Nucl Med Biol 35:197-201. 2008....
Partial recovery of dopaminergic pathway after graft of adult mesenchymal stem cells in a rat model of Parkinson's diseaseGaëlle Bouchez
INSERM U930, Laboratory Biophysique médicale and pharmaceutique, UFR Pharmacie, 31 Avenue Monge, Tours, France
Neurochem Int 52:1332-42. 2008..This cellular approach might be a restorative therapy in Parkinson's disease...
DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterizationMichelle L James
Department of Pharmacology, University of Sydney, Sydney, New South Wales, Australia
J Nucl Med 49:814-22. 2008..Radioligands for the TSPO can therefore measure active disease in the brain. This article details the synthesis, radiofluorination, and pharmacologic evaluation of a new TSPO-specific pyrazolopyrimidine, DPA-714...
Multiinjection approach for D2 receptor binding quantification in living rats using [11C]raclopride and the beta-microprobe: crossvalidation with in vitro binding dataGweltas Mauger
Unité de Recherche Associée Commissariat á l Energie Atomique Centre National de La Recherche Scientifique, Orsay, France
J Cereb Blood Flow Metab 25:1517-27. 2005..These results validate the multi-injection modelling approach coupled to beta-microprobe acquisitions as a mean to provide accurate and separate estimates of dopamine D2-receptor density and affinity, in the living rodent striatum...
Prenatal 3,4-methylenedioxymethamphetamine (ecstasy) exposure induces long-term alterations in the dopaminergic and serotonergic functions in the ratLaurent Galineau
INSERM U619, IFR135, , , 31 Avenue Monge, 37200 Tours, France
Brain Res Dev Brain Res 154:165-76. 2005..This study suggests that a prenatal exposure to MDMA induces transient and long-term neurochemical and behavioural modifications in dopaminergic and serotonergic functions...
Synthesis, radiolabeling and preliminary biological evaluation of radiolabeled 5-methyl-6-nitroquipazine, a potential radioligand for the serotonin transporterJohan Sandell
Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 171 76 Stockholm, Sweden
Bioorg Med Chem Lett 12:3611-3. 2002..The high affinity and the facile labeling of [11C]5-methyl-6-nitroquipazine makes it a promising radioligand for visualization of the serotonin transporter with positron emission tomography...
Substituted diphenyl sulfides as selective serotonin transporter ligands: synthesis and in vitro evaluationPatrick Emond
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, 31 Avenue Monge, 37200 Tours, France
J Med Chem 45:1253-8. 2002..From this series, the most SERT selective derivatives (such as 8b, 8c, and 8g) are now evaluated for their potential as positron emission tomography imaging agents when labeled with carbon-11...
Relevance of different striatal markers in assessment of the MPP+-induced dopaminergic nigrostriatal injury in ratStéphanie Barc
Groupe d Etudes des Mécanismes Cellulaires de l Ischémie GEMCI, EA 1223, Poitiers, France
J Neurochem 80:365-74. 2002....
The dopamine mesocorticolimbic pathway is affected by deficiency in n-3 polyunsaturated fatty acidsLuc Zimmer
INSERM U316, , , Tours, France
Am J Clin Nutr 75:662-7. 2002..This provides new neurochemical evidence supporting the effects of n-3 PUFA deficiency on behavior...
Protection of dopaminergic nigrostriatal afferents by GDNF delivered by microspheres in a rodent model of Parkinson's diseaseChristelle Gouhier
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, UFR des Sciences Pharmaceutiques, 37200 Tours, France
Synapse 44:124-31. 2002..In conclusion, this study demonstrates the neuroprotective action of GDNF delivered by microspheres and suggests that PE2I may be an appropriate radiotracer for use in SPET scintigraphy to follow up treatment of PD in humans...
Reversibility of n-3 fatty acid deficiency-induced changes in dopaminergic neurotransmission in rats: critical role of developmental stageErcem Kodas
INSERM U316, UFR des Sciences Pharmaceutiques, 37200 Tours, France
J Lipid Res 43:1209-19. 2002..The occurrence of profound n-3 PUFA deficiency during the lactating period could therefore be an environmental insult leading to irreversible damage to specific brain functions...
Quantification of dopamine transporter by 123I-PE2I SPECT and the noninvasive Logan graphical method in Parkinson's diseaseCaroline Prunier
Nuclear Medicine Department, Institut National de la Santé et de la Recherche Médicale Unit 316, Bretonneau Hospital, Tours, France
J Nucl Med 44:663-70. 2003....
Effect of a diet-induced n-3 PUFA depletion on cholinergic parameters in the rat hippocampusSabah Aïd
INRA, Laboratoire de Nutrition et Securite Alimentaire, Jouy en Josas, France
J Lipid Res 44:1545-51. 2003..Thus, we evidenced that an (n-3) PUFA-deficient diet can affect cholinergic neurotransmission, probably via changes in the phospholipid PUFA composition...
[(11)C]MADAM, a new serotonin transporter radioligand characterized in the monkey brain by PETChrister Halldin
Karolinska Institutet, Department of Clinical Neuroscience, Section of Psychiatry, Stockholm, Sweden
Synapse 58:173-83. 2005..The present characterization of binding in the monkey brain suggests that [(11)C]MADAM is a potential PET radioligand for quantitative studies of 5-HTT binding in the human brain...
Neither the density nor function of striatal dopamine transporters were influenced by chronic n-3 polyunsaturated fatty acid deficiency in rodentsErcem Kodas
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, Universite Francois Rabelais, UFR des Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France
Neurosci Lett 321:95-9. 2002..This suggests lower sensitivity to n-3 PUFA deficiency in the striatum than that previously observed in the frontal cortex...
Involvement of alpha6/alpha3 neuronal nicotinic acetylcholine receptors in neuropsychiatric features of Dementia with Lewy bodies: [(125)I]-alpha-conotoxin MII binding in the thalamus and striatumMelissa Ray
Institute for Ageing and Health, University of Newcastle upon Tyne, MRC Building, Newcastle General Hospital, Westgate Road, Newcastle upon Tyne NE4 6BE, UK
Neurosci Lett 372:220-5. 2004....
Pharmacological characterisation of (E)-N-(3-iodoprop-2-enyl)-2beta-carbomethoxy-3beta-(4'-methylphenyl)nortropane (PE2I) binding to the rat neuronal dopamine transporter expressed in COS cellsGuylène Page
Laboratoire de Pharmacologie Expérimentale FARL, Université catholique de Louvain 54 10, B 1200 Brussels, Belgium
Neurochem Int 40:105-13. 2002..Taken together, these data demonstrate that PE2I was a highly potent inhibitor of cloned DAT compared with GBR 12935 and provided a useful tool for further investigations in cells transfected with cDNA encoding the DAT...
Ontogeny of the dopamine and serotonin transporters in the rat brain: an autoradiographic studyLaurent Galineau
INSERM U619, , , Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France
Neurosci Lett 363:266-71. 2004....
Serotoninergic neurotransmission is affected by n-3 polyunsaturated fatty acids in the ratErcem Kodas
INSERM U316, , , Tours, France
J Neurochem 89:695-702. 2004..This suggests that provision of essential fatty acids is durably able to affect brain function and that this is related to the developmental stage during which the deficiency occurs...
Time-course of nigrostriatal degeneration in a progressive MPTP-lesioned macaque model of Parkinson's diseaseWassilios Meissner
Basal Gang, Laboratoire de Neurophysiologie, CNRS UMR 5543, , , 33076 Bordeaux Cedex, France
Mol Neurobiol 28:209-18. 2003..In this article, we examine how this and other chronic MPTP models fit with human pathology...
Ropinirole versus L-DOPA effects on striatal opioid peptide precursors in a rodent model of Parkinson's disease: implications for dyskinesiaPaula Ravenscroft
School of Biological Sciences, University of Manchester, Manchester M13 9PT, UK
Exp Neurol 185:36-46. 2004....
Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporterMitchell Quinlivan
Department of Pharmacology, University of Sydney, NSW 2006, Australia
Nucl Med Biol 30:741-6. 2003..In view of these results [(123)I]1 and [(123)I]2 do not appear to be suitable radioligands for in vivo studies of the SERT...
PE2I: a radiopharmaceutical for in vivo exploration of the dopamine transporterPatrick Emond
INSERM, U619, Tours, F 37000 France
CNS Neurosci Ther 14:47-64. 2008..The excellent properties of PE2I are basis for the development of new DAT tracers for use in future PET explorations using fluor-18...
Antenatal bacterial endotoxin sensitizes the immature rat brain to postnatal excitotoxic injuryCatherine I Rousset
INSERM U930, Universite Francois Rabelais, and Neonatology Hôpital Clocheville, CHRU Tours, Tours, France
J Neuropathol Exp Neurol 67:994-1000. 2008....
Drug-dependent requirement of hippocampal neurogenesis in a model of depression and of antidepressant reversalAlexandre Surget
U930, INSERM, Universite Francois Rabelais de Tours, Tours, France
Biol Psychiatry 64:293-301. 2008..We investigated causality between changes in hippocampal neurogenesis and the effects of both chronic stress and chronic ADs...
Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporterYolanda Zea-Ponce
, INSERM U619, , 31 Av. Monge, 37200 Tours, France
Bioorg Med Chem 13:745-53. 2005..4 nM) and (E)-(S,S)-5-AOIBV (Kd=4.3 nM). (R,R)-3, and (R,R)-4 showed the same high affinity for VAChT as (-)-5-IBVM and may be suitable as imaging agents of cholinergic nerve terminals...
Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligandsThaer Assaad
, 37200 Tours, France
Bioorg Med Chem Lett 16:2654-7. 2006..These compounds will be soon radiolabeled with [(125)I] for further biological evaluation using single photon emission computed tomography (SPECT)...
Presymptomatic diagnosis of experimental Parkinsonism with 123I-PE2I SPECTCaroline Prunier
INSERM U316, Laboratoire de Biophysique Medicale et Pharmaceutique, 31 Avenue Monge, 37200 Tours, France
Neuroimage 19:810-6. 2003..It could now be used clinically for early diagnosis and follow-up of neuroprotective treatment...
Decreased vesicular acetylcholine transporter and alpha(4)beta(2) nicotinic receptor density in the rat brain following 192 IgG-saporin immunolesioningMitchell Quinlivan
Universite Francois Rabelais de Tours, INSERM U619, Laboratoire de Biophysique Medicale et Pharmaceutique, 31 Avenue Monge, 37200 Tours, France
Neurosci Lett 415:97-101. 2007..The results with (125)I-A-85380 are unique and are in contrast with work performed in this animal model with other nAChR radioligands, indicating the favourable properties of this radioligand for molecular imaging...
