Eugenii A Rabiner

Summary

Affiliation: Imperial College
Country: UK

Publications

  1. ncbi request reprint Pindolol augmentation of selective serotonin reuptake inhibitors: PET evidence that the dose used in clinical trials is too low
    E A Rabiner
    MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, London, UK
    Am J Psychiatry 158:2080-2. 2001
  2. ncbi request reprint Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with [11C]WAY-100635 and [11C]raclopride
    Eugenii A Rabiner
    MRC Cyclotron Unit, Hammersmith Hospital, Imperial College School of Medicine, London, UK
    J Psychopharmacol 16:195-9. 2002
  3. pmc Within-subject comparison of [(11)C]-(+)-PHNO and [(11)C]raclopride sensitivity to acute amphetamine challenge in healthy humans
    Paul Shotbolt
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 32:127-36. 2012
  4. pmc Kinetic analysis of drug-target interactions with PET for characterization of pharmacological hysteresis
    Cristian Salinas
    GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 33:700-7. 2013
  5. doi request reprint Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor
    Christine A Parker
    Clinical Imaging Centre, GlaxoSmithKline, London, UK
    J Nucl Med 53:295-303. 2012
  6. pmc Two binding sites for [3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation
    David R Owen
    Department of Experimental Medicine and Toxicology, Imperial College London, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 30:1608-18. 2010
  7. doi request reprint Phosphodiesterase 10A PET radioligand development program: from pig to human
    Christophe Plisson
    Imanova Ltd, Centre for Imaging Sciences, Hammersmith Hospital, London, United Kingdom
    J Nucl Med 55:595-601. 2014
  8. doi request reprint Biodistribution and radiation dosimetry of the serotonin 5-HT₆ ligand [¹¹C]GSK215083 determined from human whole-body PET
    Robert A Comley
    GlaxoSmithKline Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK
    Mol Imaging Biol 14:517-21. 2012
  9. pmc An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28
    David R Owen
    Division of Experimental Medicine, Department of Medicine, Imperial College London, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 32:1-5. 2012
  10. pmc An evaluation of the brain distribution of [(11)C]GSK1034702, a muscarinic-1 (M 1) positive allosteric modulator in the living human brain using positron emission tomography
    Khanum Ridler
    Clinical Imaging Centre, GlaxoSmithKline, Burlington Danes Building, Hammersmith Hospital, Du Cane Road, London, UK
    EJNMMI Res 4:66. 2014

Detail Information

Publications51

  1. ncbi request reprint Pindolol augmentation of selective serotonin reuptake inhibitors: PET evidence that the dose used in clinical trials is too low
    E A Rabiner
    MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, London, UK
    Am J Psychiatry 158:2080-2. 2001
    ....
  2. ncbi request reprint Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with [11C]WAY-100635 and [11C]raclopride
    Eugenii A Rabiner
    MRC Cyclotron Unit, Hammersmith Hospital, Imperial College School of Medicine, London, UK
    J Psychopharmacol 16:195-9. 2002
    ..The differential effects of EMD 128 130 at the D2 and the 5-HT1A receptor (antagonist at D2 receptor, agonist at the 5-HTIA receptor) may explain the differences in occupancy observed...
  3. pmc Within-subject comparison of [(11)C]-(+)-PHNO and [(11)C]raclopride sensitivity to acute amphetamine challenge in healthy humans
    Paul Shotbolt
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 32:127-36. 2012
    ..This study indicates that [(11)C]-(+)-PHNO is superior to [(11)C]raclopride for studying acute fluctuations in synaptic dopamine in the human striatum. [(11)C]-(+)-PHNO also enables measurement of synaptic dopamine in D(3) regions...
  4. pmc Kinetic analysis of drug-target interactions with PET for characterization of pharmacological hysteresis
    Cristian Salinas
    GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 33:700-7. 2013
    ..An indirect pharmacokinetic-receptor occupancy model was identified as a suitable model for the calculation of affinity when a compound exhibits pharmacological hysteresis...
  5. doi request reprint Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor
    Christine A Parker
    Clinical Imaging Centre, GlaxoSmithKline, London, UK
    J Nucl Med 53:295-303. 2012
    ..In addition, such a tool would assist in the development of novel drugs targeting the 5-HT6 receptor...
  6. pmc Two binding sites for [3H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation
    David R Owen
    Department of Experimental Medicine and Toxicology, Imperial College London, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 30:1608-18. 2010
    ..The functional significance of differences in binding characteristics warrants further investigation...
  7. doi request reprint Phosphodiesterase 10A PET radioligand development program: from pig to human
    Christophe Plisson
    Imanova Ltd, Centre for Imaging Sciences, Hammersmith Hospital, London, United Kingdom
    J Nucl Med 55:595-601. 2014
    ..Four novel phosphodiesterase 10A (PDE10A) PET tracers have been synthesized, characterized in preclinical studies, and compared with the previously reported (11)C-MP-10...
  8. doi request reprint Biodistribution and radiation dosimetry of the serotonin 5-HT₆ ligand [¹¹C]GSK215083 determined from human whole-body PET
    Robert A Comley
    GlaxoSmithKline Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK
    Mol Imaging Biol 14:517-21. 2012
    ..We measured the whole-body distribution of IV-injected [¹¹C]GSK215083, a new 5-HT₆ antagonist PET tracer, as a function of time in adult subjects, in order to determine the radiation exposure...
  9. pmc An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28
    David R Owen
    Division of Experimental Medicine, Department of Medicine, Imperial College London, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 32:1-5. 2012
    ....
  10. pmc An evaluation of the brain distribution of [(11)C]GSK1034702, a muscarinic-1 (M 1) positive allosteric modulator in the living human brain using positron emission tomography
    Khanum Ridler
    Clinical Imaging Centre, GlaxoSmithKline, Burlington Danes Building, Hammersmith Hospital, Du Cane Road, London, UK
    EJNMMI Res 4:66. 2014
    ....
  11. doi request reprint Loss of phosphodiesterase 10A expression is associated with progression and severity in Parkinson's disease
    Flavia Niccolini
    1 Neurodegeneration Imaging Group, Department of Basic and Clinical Neuroscience, Institute of Psychiatry, Psychology and Neuroscience, King s College London, London, UK 2 Division of Brain Sciences, Department of Medicine, Imperial College London, London, UK
    Brain 138:3003-15. 2015
    ..PDE10A is an enzyme that could be targeted with novel pharmacotherapy, and this may help improve dopaminergic signalling and striatal output, and therefore alleviate symptoms and complications of Parkinson's disease. ..
  12. doi request reprint Translational characterization of [11C]GSK931145, a PET ligand for the glycine transporter type 1
    Roger N Gunn
    GlaxoSmithKline, Clinical Imaging Center, Hammersmith Hospital, London, United Kingdom
    Synapse 65:1319-32. 2011
    ..GSK1018921 EC(50) estimates were 22.5 and 45.7 ng/ml in primates and humans, respectively...
  13. ncbi request reprint 5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide: a[11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-py
    Eugenii A Rabiner
    Medical Research Council Cyclotron Unit, Hammersmith Hospital, Imperial College School of Medicine, London, UK
    J Pharmacol Exp Ther 301:1144-50. 2002
    ..At 24 h after the last dose 5-HT(1A) occupancy was approximately 50% of that achieved at 2 h. This study demonstrates that high occupancy of the human brain 5-HT(1A) receptor can be achieved at doses producing minimal acute side effects...
  14. doi request reprint Evaluation of 11C-GSK189254 as a novel radioligand for the H3 receptor in humans using PET
    Sharon Ashworth
    GlaxoSmithKline Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, London, United Kingdom
    J Nucl Med 51:1021-9. 2010
    ..The purpose of the present study was to evaluate (11)C-GSK189254 as a PET radioligand for human studies and to determine the dose-receptor occupancy relationship of GSK189254 in the human brain...
  15. doi request reprint Loss of extra-striatal phosphodiesterase 10A expression in early premanifest Huntington's disease gene carriers
    Heather Wilson
    Neurodegeneration Imaging Group, Department of Basic and Clinical Neuroscience, Institute of Psychiatry, Psychology and Neuroscience, King s College London, London, UK
    J Neurol Sci 368:243-8. 2016
    ..Our findings suggest that dysregulation of PDE10A-mediated intracellular signalling could be an early phenomenon in the course of HD with relevance also for extra-striatal brain areas. ..
  16. doi request reprint Human Kinetic Modeling of the 5HT6 PET Radioligand 11C-GSK215083 and Its Utility for Determining Occupancy at Both 5HT6 and 5HT2A Receptors by SB742457 as a Potential Therapeutic Mechanism of Action in Alzheimer Disease
    Christine A Parker
    GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, United Kingdom Division of Brain Sciences, Department of Medicine, Imperial College London, London, United Kingdom
    J Nucl Med 56:1901-9. 2015
    ....
  17. doi request reprint Mathematical modelling of [¹¹C]-(+)-PHNO human competition studies
    Graham E Searle
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK
    Neuroimage 68:119-32. 2013
    ..The comparisons and conclusions drawn from these can inform the design and analysis of future PET studies with [(11)C]-(+)-PHNO...
  18. doi request reprint Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [11C] P943: a positron emission tomography study in Papio anubis
    Khanum Ridler
    GlaxoSmithKline, Clinical Imaging Centre, London, UK
    Synapse 65:1119-27. 2011
    ..11 C] P943 shows promise as a tracer to image serotonin function in healthy subjects as well as subjects with psychiatric or neurologic conditions...
  19. pmc Measuring drug occupancy in the absence of a reference region: the Lassen plot re-visited
    Vincent J Cunningham
    GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 30:46-50. 2010
    ..We present a transformation of a graphical method, originally introduced by Lassen, using regional estimates of V(T) alone to determine occupancy, together with an extension that does not require baseline data...
  20. ncbi request reprint Occupancy of agonist drugs at the 5-HT1A receptor
    R Alexander Bantick
    Cyclotron Building, CSc, The Hammersmith Hospital, Imperial College London, London, UK
    Neuropsychopharmacology 29:847-59. 2004
    ....
  21. doi request reprint Imaging dopamine receptors in humans with [11C]-(+)-PHNO: dissection of D3 signal and anatomy
    Andri C Tziortzi
    GlaxoSmithKline, Clinical Imaging Centre, Imperial College, London, UK
    Neuroimage 54:264-77. 2011
    ..An automated approach for the delineation of these anatomical regions of interest was also developed and investigated in terms of its reproducibility and accuracy...
  22. pmc Hippocampal Neuroinflammation, Functional Connectivity, and Depressive Symptoms in Multiple Sclerosis
    Alessandro Colasanti
    Division of Brain Sciences, Department of Medicine, Imperial College London, London, United Kingdom Centre for Affective Disorders, Institute of Psychiatry, Psychology and Neuroscience, King s College London, London, United Kingdom Imanova Centre for Imaging Sciences, London, United Kingdom Electronic address
    Biol Psychiatry 80:62-72. 2016
    ..To evaluate pathophysiologic mechanisms, we explored the relationships between hippocampal neuroinflammation, depressive symptoms, and hippocampal functional connectivities defined by resting-state functional magnetic resonance imaging...
  23. doi request reprint Phosphodiesterase 10A in Schizophrenia: A PET Study Using [(11)C]IMA107
    Tiago Reis Marques
    From the Department of Psychosis Studies, the Neurodegeneration Imaging Group, the Department of Basic and Clinical Neuroscience, and the Department of Neuroimaging, Institute of Psychiatry, Psychology, and Neuroscience, King s College London, London the Division of Brain Sciences, Department of Medicine, and the Psychiatric Imaging Group, Medical Research Council Clinical Sciences Centre, Institute of Clinical Science, Imperial College London, London and Imanova Ltd, Centre for Imaging Sciences, Hammersmith Hospital, London
    Am J Psychiatry 173:714-21. 2016
    ..However, the status of PDE10A in schizophrenia is unknown. Using a newly developed and validated radioligand, [(11)C]IMA107, the authors report the first in vivo assessment of PDE10A brain expression in patients with schizophrenia...
  24. pmc Determination of [(11)C]PBR28 binding potential in vivo: a first human TSPO blocking study
    David R Owen
    Division of Brain Sciences, Department of Medicine, Imperial College, London, UK
    J Cereb Blood Flow Metab 34:989-94. 2014
    ..Our estimates of [(11)C]PBR28 VND and hence BPND in the healthy human brain are consistent with in vitro predictions. XBD173 blockade provides a practical means of estimating VND for TSPO targeting radioligands. ..
  25. doi request reprint Radiation dose estimates for carbon-11-labelled PET tracers
    Jasper van der Aart
    GlaxoSmithKline, Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, W120NN London, UK
    Nucl Med Biol 39:305-14. 2012
    ..This review describes radiation dosimetry of carbon-11-labelled molecules in the context of current PET research and the most widely used regulatory guidelines...
  26. ncbi request reprint A database of [(11)C]WAY-100635 binding to 5-HT(1A) receptors in normal male volunteers: normative data and relationship to methodological, demographic, physiological, and behavioral variables
    Eugenii A Rabiner
    MRC Cyclotron Unit, Division of Neuroscience and Psychological Medicine, Imperial College School of Medicine, Hammersmith Hospital, London W12 0NN, United Kingdom
    Neuroimage 15:620-32. 2002
    ..The large between-subject variability observed could not be explained by common methodological, physiological, or behavioral factors and hence the biological basis of this variability remains to be clarified...
  27. doi request reprint Characterising the plasma-target occupancy relationship of the neurokinin antagonist GSK1144814 with PET
    Khanum Ridler
    1Imanova Ltd, London, UK
    J Psychopharmacol 28:244-53. 2014
    ..Our data provided support for the further progression of this compound and have optimised the likely therapeutic dose range...
  28. pmc In vivo imaging of cerebral dopamine D3 receptors in alcoholism
    David Erritzoe
    Centre for Neuropsychopharmacology, Division of Brain Sciences, Faculty of Medicine, Imperial College London, London, UK
    Neuropsychopharmacology 39:1703-12. 2014
    ..This may be relevant to the development of future therapeutic strategies to treat alcohol abuse...
  29. pmc Blunted Endogenous Opioid Release Following an Oral Amphetamine Challenge in Pathological Gamblers
    Inge Mick
    Centre for Neuropsychopharmacology, Division of Brain Sciences, Faculty of Medicine, Imperial College London, London, UK
    Neuropsychopharmacology 41:1742-50. 2016
    ..Our findings are consistent with growing evidence that dysregulation of endogenous opioids may have an important role in the pathophysiology of addictions. ..
  30. doi request reprint Altered PDE10A expression detectable early before symptomatic onset in Huntington's disease
    Flavia Niccolini
    1 Neurodegeneration Imaging Group, Department of Clinical Neuroscience, Institute of Psychiatry, Psychology and Neuroscience, King s College London, London, UK 2 Division of Brain Sciences, Department of Medicine, Imperial College London, London, UK
    Brain 138:3016-29. 2015
    ....
  31. pmc Bipolar Disorder is associated with the rs6971 polymorphism in the gene encoding 18 kDa Translocator Protein (TSPO)
    Alessandro Colasanti
    Division of Brain Sciences, Imperial College, London, United Kingdom Imanova Centre for Imaging Sciences, Hammersmith Hospital Campus, London, United Kingdom Electronic address
    Psychoneuroendocrinology 38:2826-9. 2013
    ..This supports the hypothesis that HPA dysregulation has a causal role in Bipolar Disorder, and is not just a consequence of the disease. ..
  32. pmc A graphical method to compare the in vivo binding potential of PET radioligands in the absence of a reference region: application to [¹¹C]PBR28 and [¹⁸F]PBR111 for TSPO imaging
    Qi Guo
    1 Centre for Neuroimaging Sciences, Institute of Psychiatry, King s College London, London, UK 2 Imanova, Centre for Imaging Sciences, London, UK 3 Division of Brain Sciences, Department of Medicine, Imperial College London, London, UK
    J Cereb Blood Flow Metab 34:1162-8. 2014
    ..The analysis determined that [(11)C]PBR28 had a higher BPND than [(18)F]PBR111...
  33. pmc Identifying improved TSPO PET imaging probes through biomathematics: the impact of multiple TSPO binding sites in vivo
    Qi Guo
    Division of Experimental Medicine, Imperial College London, Hammersmith Hospital, UK
    Neuroimage 60:902-10. 2012
    ....
  34. pmc Mixed-affinity binding in humans with 18-kDa translocator protein ligands
    David R J Owen
    Division of Experimental Medicine, Imperial College, Hammersmith Hospital, London, United Kingdom
    J Nucl Med 52:24-32. 2011
    ....
  35. ncbi request reprint Translocator positron-emission tomography and magnetic resonance spectroscopic imaging of brain glial cell activation in multiple sclerosis
    Gourab Datta
    Division of Brain Sciences, Department of Medicine, Imperial College London, London, UK
    Mult Scler . 2016
    ..Brain translocator protein (TSPO) positron-emission tomography (PET) and [myo-inositol] magnetic resonance spectroscopy (MRS) were used together to assess this...
  36. pmc Neuroinflammation in treated HIV-positive individuals: A TSPO PET study
    Jaime H Vera
    From the Division of Medicine, Section of Infectious Diseases J H V, A W, Division of Brain Sciences J H C, R N G, P M M, and Centre for Immunology and Vaccinology A B, L G, P K, Imperial College London Division of Medicine J H V, Brighton and Sussex Medical School Imanova Centre for Imaging Sciences Q G, E A R, N K, C B, R N G, London and Chelsea and Westminster Hospital A B, L G, P K, London, UK
    Neurology 86:1425-32. 2016
    ....
  37. pmc Presynaptic 5-HT1A is related to 5-HTT receptor density in the human brain
    Subrata K Bose
    PET Methodology, MRC Clinical Sciences Centre, Imperial College London, Hammersmith Hospital Campus, London, UK
    Neuropsychopharmacology 36:2258-65. 2011
    ..This latter finding may reflect differences in 5-HT tone between individuals, and highlights probable substrates sensitive to variations in DRN 5-HT function...
  38. pmc Positron emission tomography molecular imaging for drug development
    Paul M Matthews
    GSK Clinical Imaging Centre, GlaxoSmithKline Research and Development Ltd, Hammersmith Hospital, London, UK
    Br J Clin Pharmacol 73:175-86. 2012
    ..We urge that the potential value of a translational molecular imaging strategy be considered routinely and at the earliest stages of new drug development...
  39. doi request reprint Radiosynthesis and in vivo evaluation of [(11)C]MP-10 as a positron emission tomography radioligand for phosphodiesterase 10A
    Christophe Plisson
    GlaxoSmithKline, Clinical Imaging Centre Hammersmith Hospital, London, W12 0NN, UK
    Nucl Med Biol 38:875-84. 2011
    ..The aim of this study was to evaluate a newly reported positron emission tomography (PET) radioligand [(11)C]MP-10, a potent and selective inhibitor of the central phosphodiesterase 10A enzyme (PDE10A) in vivo, using PET...
  40. ncbi request reprint Role of 18F-fluorodeoxyglucose Positron Emission Tomography in the Monitoring of Inflammatory Activity in Crohn's Disease
    Evangelos A Russo
    Division of Experimental Medicine, Department of Medicine, Imperial College London, London, United Kingdom Departments of Gastroenterology and Imaging, Imperial College Healthcare NHS Trust, London, United Kingdom Imanova Centre for Imaging Sciences, London, United Kingdom Centre for Neuroimaging Sciences, King s College, London, United Kingdom Centre for Medical Imaging, University College London, London, United Kingdom Division of Brain Sciences, Department of Medicine, Imperial College London, London, United Kingdom and Division of Hepatology and Gastroenterology, Department of Surgery and Cancer, Imperial College Healthcare NHS Trust, London, United Kingdom
    Inflamm Bowel Dis 22:2619-2629. 2016
    ..The aim of this study was to assess the utility of FDG-PET as a marker of progression of inflammatory activity and its response to treatment in patients with CD...
  41. doi request reprint In Vivo Assessment of Brain White Matter Inflammation in Multiple Sclerosis with (18)F-PBR111 PET
    Alessandro Colasanti
    Division of Brain Sciences, Department of Medicine, Imperial College London, London, United Kingdom Imanova Centre for Imaging Sciences, London, United Kingdom
    J Nucl Med 55:1112-8. 2014
    ..In this study, we used (18)F-PBR111 PET and MR imaging to measure relative binding in the lesional, perilesional, and surrounding normal-appearing white matter of MS patients, as an index of the innate immune response...
  42. pmc The gut hormones PYY 3-36 and GLP-1 7-36 amide reduce food intake and modulate brain activity in appetite centers in humans
    Akila De Silva
    Section of Investigative Medicine, Division of Diabetes, Endocrinology and Metabolism, Imperial College London, London, UK
    Cell Metab 14:700-6. 2011
    ....
  43. doi request reprint A multi-center randomized proof-of-concept clinical trial applying [¹⁸F]FDG-PET for evaluation of metabolic therapy with rosiglitazone XR in mild to moderate Alzheimer's disease
    Sofia Tzimopoulou
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Alzheimers Dis 22:1241-56. 2010
    ..It suggests that Rosiglitazone is associated with an early increase in whole brain glucose metabolism, but not with any biological or clinical evidence for slowing progression over a 1 year follow up in the symptomatic stages of AD...
  44. doi request reprint In vivo quantification of regional dopamine-D3 receptor binding potential of (+)-PHNO: Studies in non-human primates and transgenic mice
    Eugenii A Rabiner
    GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, UK
    Synapse 63:782-93. 2009
    ..The midbrain is thus an excellent target region to examine D3 receptor occupancy with [(11)C]-(+)-PHNO PET in vivo...
  45. doi request reprint Imaging in Central Nervous System Drug Discovery
    Roger N Gunn
    Imanova Ltd, London, United Kingdom Division of Brain Sciences, Imperial College London, London, United Kingdom Department of Engineering Science, Institute of Biomedical Engineering, University of Oxford, Oxford, United Kingdom Electronic address
    Semin Nucl Med 47:89-98. 2017
    ..Finally, we review the advances in PET science of biomarker development and analysis that enable sophisticated drug-development studies in man...
  46. pmc Investigation of the Brain Biodistribution of the Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitor [18F]GSK2647544 in Healthy Male Subjects
    Mickael Huiban
    Imanova Limited, Burlington Danes Building, Imperial College London, Hammersmith Hospital, Du Cane Road, London, W12 0NN, UK
    Mol Imaging Biol . 2016
    ..In order to refine therapeutic dose predictions and confirm brain penetration, a radiolabelled form of the inhibitor, [18F]GSK2647544, was manufactured for use in a positron emission tomography (PET) biodistribution study...
  47. pmc Prediction of repeat-dose occupancy from single-dose data: characterisation of the relationship between plasma pharmacokinetics and brain target occupancy
    Sergio Abanades
    GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, UK
    J Cereb Blood Flow Metab 31:944-52. 2011
    ..29±1.11 ng/mL). This approach increases the value of SD occupancy studies that are performed as part of first time in human drug development programmes by providing an estimate of the dose required to achieve the desired TO at RD...
  48. ncbi request reprint Preferential 5-HT1A autoreceptor occupancy by pindolol is attenuated in depressed patients: effect of treatment or an endophenotype of depression?
    Eugenii A Rabiner
    PET Psychiatry, Translational Medicine and Technologies, GlaxoSmithKline, Cambridge, UK
    Neuropsychopharmacology 29:1688-98. 2004
    ..Speculatively, the degree of preferential occupancy may serve as a surrogate marker for depression, or the pharmacological effects of antidepressants...
  49. ncbi request reprint Brain 5-HT1A receptor binding in chronic fatigue syndrome measured using positron emission tomography and [11C]WAY-100635
    Anthony J Cleare
    Section of Neurobiology of Mood Disorders, Division of Psychological Medicine, Institute of Psychiatry and Guy s, King s and St Thomas School of Medicine, London, United Kingdom
    Biol Psychiatry 57:239-46. 2005
    ..We assessed brain 5-HT1A receptor binding potential directly using the specific radioligand [11C]WAY-100635 and positron emission tomography (PET)...
  50. ncbi request reprint Fibromyalgia patients show an abnormal dopamine response to pain
    Patrick B Wood
    McGill University Centre for Research on Pain, Faculty of Dentistry, 3640 University Street, Strathcona Building, Montreal, QC, Canada, H3A 2B2
    Eur J Neurosci 25:3576-82. 2007
    ....
  51. pmc A functional genetic variation of the serotonin (5-HT) transporter affects 5-HT1A receptor binding in humans
    Sean P David
    Department of Clinical Pharmacology, Cancer Research United Kingdom General Practice Research Group, University of Oxford, Oxford OX2 6HE, United Kingdom
    J Neurosci 25:2586-90. 2005
    ..The results may offer a plausible physiological mechanism underlying the association between 5-HTTLPR genotype, behavioral traits, and mood states...