Research Topics
| Christian HeidbrederSummaryAffiliation: GlaxoSmithKline Research and Development Country: USA Publications
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Detail Information
Publications
Novel pharmacotherapeutic approaches for the treatment of drug addiction and cravingChristian A Heidbreder
Department of Biology, Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy
Curr Opin Pharmacol 5:107-18. 2005..These long-term molecular and neurochemical changes might, in turn, explain the core features of addiction--the compulsive seeking and taking of the drug--as well as the risk of relapse...- Novel pharmacotherapeutic targets for the management of drug addictionChristian Heidbreder
Department of Neuropsychopharmacology, Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A Fleming 4, 37135 Verona, Italy
Eur J Pharmacol 526:101-12. 2005.... - Role of dopamine D3 receptors in the addictive properties of ethanolChristian A Heidbreder
Center of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A Fleming 4, 37135 Verona, Italy
Drugs Today (Barc) 40:355-65. 2004..The present review is intended to highlight a new, promising area in alcohol research that focuses on the role of the dopamine D(3) receptor in the addictive properties of ethanol... - The medial prefrontal cortex in the rat: evidence for a dorso-ventral distinction based upon functional and anatomical characteristicsChristian A Heidbreder
Department of Biology, Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A Fleming 4, 37135 Verona, Italy
Neurosci Biobehav Rev 27:555-79. 2003..The present review covers recent findings with the intent of correlating these distinct functional differences in the dorso-ventral axis of the rat medial prefrontal cortex with anatomical and neurochemical patterns... - Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivoChristian A Heidbreder
Department of Biology, Center of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy
Synapse 50:269-76. 2003..Collectively, the results of the present study provide potential new mechanisms through which MPEP exerts its anxiolytic and antidepressant effects... - New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systemsFabrizio Micheli
GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
Bioorg Med Chem Lett 18:901-7. 2008..The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported... - Selective antagonism at dopamine D3 receptors prevents nicotine-triggered relapse to nicotine-seeking behaviorMichela Andreoli
Center of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A. Fleming 4, 37135 Verona, Italy
Neuropsychopharmacology 28:1272-80. 2003..These findings point toward the potential use of selective DA D(3) receptor antagonists for the pharmacotherapeutic management of relapse to drug-seeking behaviors... - 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonistsFabrizio Micheli
Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
J Med Chem 53:374-91. 2010..Several members of this series also significantly attenuate the expression of conditioned place preference (CPP) to nicotine and cocaine... - Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonistsFabrizio Micheli
Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
J Med Chem 53:7129-39. 2010..In this manuscript, we are reporting a detailed exploration of the region of the receptor interacting with the amine terminus of the scaffold wherein SAR and developability data associated with these novel templates was undertaken... - In vivo autofluorescence spectrofluorometry of central serotoninFrancesco Crespi
Department of Biology, Psychiatry C.E.D.D, GlaxoSmithKline S.p.A, Verona, Italy
J Neurosci Methods 140:67-73. 2004..This is a reliable evidence of the in vivo application of spectroscopy together with optic fiber probe for in vivo, in situ and real time measurement of 5-HT in discrete brain areas... - The orexin-1 receptor antagonist SB-334867 reduces amphetamine-evoked dopamine outflow in the shell of the nucleus accumbens and decreases the expression of amphetamine sensitizationDavide Quarta
Department of Biology, Neurosciences CEDD, GlaxoSmithKline Medicines Research Centre, Verona, Italy
Neurochem Int 56:11-5. 2010.... - New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systemsFabrizio Micheli
GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy
Bioorg Med Chem Lett 18:908-12. 2008..The new scaffolds of the [g]-fused and the hetero-fused tricyclic benzazepine are here reported together with their pharmacokinetic profile... - [3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonistsFabrizio Micheli
Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
Bioorg Med Chem Lett 20:5491-4. 2010..A new class of azabicyclo[3.1.0]benzenesulfonamides is presented as selective dopamine D3 antagonists together with SAR and selectivity data... - Orexin-1 receptor antagonist SB-334867 reduces the acquisition and expression of cocaine-conditioned reinforcement and the expression of amphetamine-conditioned rewardDaniel M Hutcheson
Department of Biology, Neurosciences CEDD, GlaxoSmithKline Medicines Research Centre, Verona, Italy
Behav Pharmacol 22:173-81. 2011..These results suggest that orexin-1 receptor antagonism could offer therapeutic potential in reducing the impact of psychostimulant-predictive stimuli that contribute to compulsive drug seeking in human drug users... - Selective dopamine D3 receptor antagonists: a review 2001-2005Fabrizio Micheli
Department of Medicinal Chemistry, Glaxo SmithKline S.p.A, Via A. Fleming 4, 37135 Verona, Italy
Recent Patents CNS Drug Discov 1:271-88. 2006.... - Selective dopamine D3 receptor antagonists enhance cortical acetylcholine levels measured with high-performance liquid chromatography/tandem mass spectrometry without anti-cholinesterasesLaurent P Lacroix
Department of Neuropsychopharmacology, Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline S.p.A, Via A. Fleming 4, 37135 Verona, Italy
J Neurosci Methods 157:25-31. 2006.... - In vivo voltammetry: from wire to wireless measurementsFrancesco Crespi
Department of Biology, Psychiatry CEDD, GlaxoSmithKline, Verona, Italy
J Neurosci Methods 140:153-61. 2004..The PC performs the sampling and elaboration of polarographic traces in a flexible and programmable way... - Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimizationFabrizio Micheli
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicine Research Centre, Verona, Italy
Bioorg Med Chem Lett 19:4011-3. 2009..The lead optimization process to identify new selective dopamine D(3) receptor antagonists is reported. DMPK parameters and binding data suggest that selective D(3) receptor antagonists as potential PET ligands might have been identified... - High-performance liquid chromatography/tandem mass spectrometry assay for the rapid high sensitivity measurement of basal acetylcholine from microdialysatesMark E P Hows
Computational Analytical and Structural Sciences, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK
J Neurosci Methods 121:33-9. 2002..Furthermore, separation conditions were modified to allow simultaneous measurement of ACh and the acetylcholine esterase inhibitor, neostigmine... - High-performance liquid chromatography/tandem mass spectrometric assay for the simultaneous measurement of dopamine, norepinephrine, 5-hydroxytryptamine and cocaine in biological samplesMark E P Hows
Computational Analytical and Structural Sciences, Psychiatry CEDD, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy
J Neurosci Methods 138:123-32. 2004..The analytes were detected using tandem mass spectrometry in the positive ion electrospray mode. The limits of detection for DA, NE, 5HT and cocaine were 200, 1000, 900 pM and 1 pg ml(-1), respectively... - Amino acid neurotransmitters: separation approaches and diagnostic valueAjit J Shah
Computational, Analytical and Structural Sciences, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
J Chromatogr B Analyt Technol Biomed Life Sci 781:151-63. 2002..An overview of the function of amino acid transmitters in the brain is given. In addition, the type of sampling techniques that are used for the determination of amino acid levels in the brain is described... - Localisation of NMU1R and NMU2R in human and rat central nervous system and effects of neuromedin-U following central administration in ratsJane Gartlon
Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline plc, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, United Kingdom
Psychopharmacology (Berl) 177:1-14. 2004..In agreement, centrally administered NmU affects feeding behaviour, energy expenditure and pituitary output. Further central nervous system (CNS) roles for NmU warrant investigation... - Aripiprazole increases dopamine but not noradrenaline and serotonin levels in the mouse prefrontal cortexAlessandro Zocchi
Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Neuropsychopharmacology, Via A Fleming 4, 37135 Verona, Italy
Neurosci Lett 387:157-61. 2005..These data further support the hypothesis that selective activation of dopaminergic neurotransmission in the prefrontal cortex may contribute to the therapeutic efficacy of aripiprazole... - Correlation between serum ghrelin levels and cocaine-seeking behaviour triggered by cocaine-associated conditioned stimuli in ratsMichela Tessari
Department of Biology, Centre of Excellence for Drug Discovery in Psychiatry, Verona, Italy
Addict Biol 12:22-9. 2007..37; NS), and the increased active lever presses only in animals exposed to CS. These findings suggest a potential role of ghrelin in the modulation of cue-triggered reinstatement of cocaine-seeking behaviour... - Pharmacological modulation of functional connectivity: the correlation structure underlying the phMRI response to d-amphetamine modified by selective dopamine D3 receptor antagonist SB277011AAdam J Schwarz
Department of Neuroimaging, Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithKline, Via Fleming 4, 37135 Verona, Italy
Magn Reson Imaging 25:811-20. 2007..The strongest modifications in the correlation patterns occurred in connection with the ventral tegmental area, the source of mesolimbic dopamine projections and a key substrate in the reward system... - Evidence for the role of dopamine D3 receptors in oral operant alcohol self-administration and reinstatement of alcohol-seeking behavior in miceChristian A Heidbreder
Department of Neuropsychopharmacology, Centre of Excellence for Drug Discovery in Psychiatry, Verona, Italy
Addict Biol 12:35-50. 2007..Provided these results can be extrapolated to humans, they suggest that selective DA D(3) receptor antagonists may be useful in the pharmacotherapeutic management of alcohol intake and prevention of relapse to alcohol-seeking behavior... - Dopamine responsiveness to drugs of abuse: A shell-core investigation in the nucleus accumbens of the mouseAlessandro Zocchi
Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy
Synapse 50:293-302. 2003..These findings suggest that a careful evaluation of the data is required when subtle changes in extracellular levels of DA are measured... - Postsynaptic 5-HT1B receptors modulate electroshock-induced generalised seizures in ratsTania O Stean
Neurology and GI CEDD, GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW
Br J Pharmacol 144:628-35. 2005..7. Overall, these data demonstrate that stimulation of postsynaptic 5-HT1B receptors inhibits electroshock-induced seizure spread in rats... - Antagonism at metabotropic glutamate 5 receptors inhibits nicotine- and cocaine-taking behaviours and prevents nicotine-triggered relapse to nicotine-seekingMichela Tessari
Center of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A Fleming 4, 37135 Verona, Italy
Eur J Pharmacol 499:121-33. 2004..Altogether, the present findings strengthen the hypothesis that selective antagonism at mGlu5 receptors may be a new potential pharmacotherapeutic approach for the treatment of drug dependence and addiction... - Selective antagonism at dopamine D3 receptors enhances monoaminergic and cholinergic neurotransmission in the rat anterior cingulate cortexLaurent P Lacroix
Center of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, Via A. Fleming 4, 37135 Verona, Italy
Neuropsychopharmacology 28:839-49. 2003.... - 5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortexLaurent P Lacroix
Centre of Excellence for Drug Discovery in Psychiatry, Department of Biology, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy, and Harlow, CM19 5AW, UK
Synapse 51:158-64. 2004..These results further support the rationale for the use of 5-HT(6) receptor antagonists in the treatment of cognitive dysfunction associated with psychiatric diseases... - Gradient of dopamine responsiveness to dopamine receptor agonists in subregions of the rat nucleus accumbensClaire S Shilliam
Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline, New Frontiers Science Park, Essex CM19 5AW, Harlow, United Kingdom
Eur J Pharmacol 477:113-22. 2003..The present findings suggest that quinelorane is one of the most selective dopamine D3 receptor agonists based on its ability to target the shell subregion of the nucleus accumbens... - Systemic administration of ghrelin increases extracellular dopamine in the shell but not the core subdivision of the nucleus accumbensDavide Quarta
Department of Biology, Neurosciences CEDD, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
Neurochem Int 54:89-94. 2009..The present findings therefore suggest that systemic ghrelin may modulate the valence of reinforcers such as food and drugs of abuse by interfering with mesolimbic DA activity... - Autofluorescence spectrofluorometry of central nervous system (CNS) neuromediatorsFrancesco Crespi
Department of Biology, Psychiatry C.E.D.D, GlaxoSmithKline S.p.A, Verona, Italy
Lasers Surg Med 34:39-47. 2004..CONCLUSIONS: Autofluorescence spectroscopy potential is confirmed as a suitable technique for the direct measurement of neurotransmitters... - Selective dopamine D(3) receptor antagonist SB-277011-A potentiates phMRI response to acute amphetamine challenge in the rat brainAdam Schwarz
Department of Neuroimaging, Centre of Excellence for Drug Discovery, Psychiatry, GlaxoSmithKline Medicines Research Centre, 37135 Verona, Italy
Synapse 54:1-10. 2004..The increased response following D(3) receptor antagonism is consistent with this receptor mediating an inhibitory action on brain activity following a dopaminergic stimulus... - 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonistsFabrizio Micheli
Psychiatry Centre of Excellence, Molecular Discovery Research, and Safety Assessment, GlaxoSmithKline Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy
J Med Chem 50:5076-89. 2007.... - Non-invasive in vivo infrared laser spectroscopy to analyse endogenous oxy-haemoglobin, deoxy-haemoglobin, and blood volume in the rat CNSFrancesco Crespi
Biology Department, Psychiatry CEDD, GlaxoSmithKline, Via Fleming 4, 37135 Verona, Italy
J Neurosci Methods 145:11-22. 2005..Afterwards, the effects of pharmacological treatments, such as systemic amphetamine and nicotine treatments on the CNS have been detected... - The role of central dopamine D3 receptors in drug addiction: a review of pharmacological evidenceChristian A Heidbreder
Centre of Excellence for Drug Discovery in Psychiatry, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy
Brain Res Brain Res Rev 49:77-105. 2005..Provided these results can be extrapolated to human drug addicts, they suggest that selective DA D3 receptor antagonists may prove effective as potential pharmacotherapeutic agents to manage drug dependence and addiction... - Cytoskeletal changes in the hippocampus following restraint stress: role of serotonin and microtubulesMassimiliano Bianchi
Center of Excellence for Drug Discovery in Psychiatry, Department of Biology, GlaxoSmithKline Pharmaceuticals, 37135 Verona, Italy
Synapse 49:188-94. 2003..The stress-induced cytoskeletal changes observed in the present study suggest that the microtubular network is a potential new pathway that may increase our understanding of stress-related events... - Effects of the selective dopamine D3 receptor antagonist SB-277011A on the reinforcing effects of nicotine as measured by a progressive-ratio schedule in ratsJason T Ross
Minneapolis Medical Research Foundation, 914 South 8th Street, Minneapolis, MN 55404, USA
Eur J Pharmacol 559:173-9. 2007.... - Acute administration of the selective D3 receptor antagonist SB-277011A blocks the acquisition and expression of the conditioned place preference response to heroin in male ratsCharles R Ashby
Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, Saint John's University, Jamaica, New York 11439, USA
Synapse 48:154-6. 2003 - Blockade of mesolimbic dopamine D3 receptors inhibits stress-induced reinstatement of cocaine-seeking in ratsZheng Xiong Xi
Neuropsychopharmacology Section, Intramural Research Program, Department of Health and Human Services, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
Psychopharmacology (Berl) 176:57-65. 2004..We have previously shown that selective D3 receptor blockade by the novel D3 antagonist SB-277011A inhibits cocaine's reinforcing action and cocaine-induced reinstatement of cocaine-seeking behavior... - Acute administration of SB-277011A, NGB 2904, or BP 897 inhibits cocaine cue-induced reinstatement of drug-seeking behavior in rats: role of dopamine D3 receptorsJeremy G Gilbert
Neuropsychopharmacology Section, Behavioral Neuroscience Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, Maryland 21224, USA
Synapse 57:17-28. 2005.... - The selective dopamine D3 receptor antagonist SB-277011-A attenuates ethanol consumption in ethanol preferring (P) and non-preferring (NP) ratsPanayotis K Thanos
Behavioral Neuropharmacology Lab, Medical Department, Building 490, Brookhaven National Laboratory, Upton, NY 11973 5000, USA
Pharmacol Biochem Behav 81:190-7. 2005.... - The effects of two highly selective dopamine D3 receptor antagonists (SB-277011A and NGB-2904) on food self-administration in a rodent model of obesityPanayotis K Thanos
Behavioral Neuropharmacology and Neuroimaging Lab, Department of Medicine, Brookhaven National Laboratory, Upton, NY 11973 5000, USA
Pharmacol Biochem Behav 89:499-507. 2008..These results suggest that along with its involvement in seeking behavior for drugs of abuse, the D(3) dopamine receptor may also be involved in seeking behavior for natural reinforcers such as food... - Selective dopamine D3 receptor antagonism by SB-277011A attenuates cocaine reinforcement as assessed by progressive-ratio and variable-cost-variable-payoff fixed-ratio cocaine self-administration in ratsZheng-Xiong Xi
Neuropsychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
Eur J Neurosci 21:3427-38. 2005..If these results extrapolate to humans, SB-277011A or similar selective DA D(3) receptor antagonists may be useful in the treatment of cocaine addiction... - Selective antagonism at dopamine D3 receptors attenuates cocaine-seeking behaviour in the ratLuigi Cervo
Istituto di Ricerche Farmacologiche Mario Negri, Via Eritrea, Milan, Italy
Int J Neuropsychopharmacol 10:167-81. 2007..These results, provided they can be extrapolated to abstinent human addicts, suggest the potential therapeutic use of selective DA D3 receptor antagonists for the prevention of cue-controlled cocaine-seeking and relapse... - Role of dopamine D3 receptors in the expression of conditioned fear in ratsShelley N Swain
Department of Psychology, 62 Arch St, Queen s University, Kingston ON, Canada K7L 3N6
Eur J Pharmacol 579:167-76. 2008..Thus, BP 897 and SB-277011A dose-dependently attenuated the expression but not the acquisition of conditioned fear. These findings suggest that BP 897 and SB-277011A reduce the control of responding by aversively conditioned stimuli... - The selective dopamine D3 receptor antagonist SB-277011A reduces nicotine-enhanced brain reward and nicotine-paired environmental cue functionsArlene C Pak
Neuropsychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Baltimore, MD 21224, USA
Int J Neuropsychopharmacol 9:585-602. 2006..The results suggest that selective D3 receptor antagonism constitutes a new and promising pharmacotherapeutic approach to the treatment of nicotine dependence... - SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition modelsWarren D Hirst
Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, Harlow, Essex, CM19 5AW, UK
Eur J Pharmacol 553:109-19. 2006..These studies provide further support for the potential therapeutic utility of 5-HT(6) receptor antagonists in disorders characterised by cognitive deficits such as Alzheimer's disease and schizophrenia... - The effects of lamotrigine on alcohol seeking and relapseValentina Vengeliene
Department of Psychopharmacology, Central Institute of Mental Health, University of Heidelberg, 68159 Mannheim, Germany
Neuropharmacology 53:951-7. 2007....