Victor W Pike

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. ncbi request reprint Radioiodinated SB 207710 as a radioligand in vivo: imaging of brain 5-HT4 receptors with SPET
    Victor W Pike
    MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, DuCane Road, W12 0NN, London, UK
    Eur J Nucl Med Mol Imaging 30:1520-8. 2003
  2. ncbi request reprint Synthesis and structure-affinity relationships of new 4-(6-iodo-H-imidazo[1,2-a]pyridin-2-yl)-N-dimethylbenzeneamine derivatives as ligands for human beta-amyloid plaques
    Lisheng Cai
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 50:4746-58. 2007
  3. ncbi request reprint Effect of a P-glycoprotein inhibitor, Cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(-)-RWAY
    Jeih San Liow
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 0135, USA
    Synapse 61:96-105. 2007
  4. ncbi request reprint In vivo and in vitro measurement of brain phosphodiesterase 4 in rats after antidepressant administration
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
    Synapse 61:78-86. 2007
  5. ncbi request reprint Identification and regional distribution in rat brain of radiometabolites of the dopamine transporter PET radioligand [11C]PE2I
    H Umesha Shetty
    PET Radiopharmaceutical Sciences, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C351, MSC 1003, 10 Center Drive, Bethesda, MD 20892 1003, USA
    Eur J Nucl Med Mol Imaging 34:667-78. 2007
  6. ncbi request reprint Radioligand development for PET imaging of beta-amyloid (Abeta)--current status
    Lisheng Cai
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Curr Med Chem 14:19-52. 2007
  7. pmc Kinetic brain analysis and whole-body imaging in monkey of [11C]MNPA: a dopamine agonist radioligand
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, Building 31, Bethesda, MD 20892, USA
    Synapse 62:700-9. 2008
  8. ncbi request reprint PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurements
    Sami S Zoghbi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 47:520-7. 2006
  9. pmc Occupancy of dopamine D2/3 receptors in rat brain by endogenous dopamine measured with the agonist positron emission tomography radioligand [11C]MNPA
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    Synapse 62:756-63. 2008
  10. ncbi request reprint Synthesis and structure-activity relationships (SARs) of 1,5-diarylpyrazole cannabinoid type-1 (CB(1)) receptor ligands for potential use in molecular imaging
    Sean R Donohue
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Bioorg Med Chem 14:3712-20. 2006

Detail Information

Publications75

  1. ncbi request reprint Radioiodinated SB 207710 as a radioligand in vivo: imaging of brain 5-HT4 receptors with SPET
    Victor W Pike
    MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, DuCane Road, W12 0NN, London, UK
    Eur J Nucl Med Mol Imaging 30:1520-8. 2003
    ..Radioactivity in all brain regions was reduced almost to the level in cerebellum by 176 min after radioligand injection. These findings show that [(123)I]SB 207710 is an effective radioligand for imaging brain 5-HT(4) receptors in vivo...
  2. ncbi request reprint Synthesis and structure-affinity relationships of new 4-(6-iodo-H-imidazo[1,2-a]pyridin-2-yl)-N-dimethylbenzeneamine derivatives as ligands for human beta-amyloid plaques
    Lisheng Cai
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 50:4746-58. 2007
    ..The structure-activity relationships revealed in this study extends insight into the topography of the binding site for IMPY-like ligands in human Abeta plaques...
  3. ncbi request reprint Effect of a P-glycoprotein inhibitor, Cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(-)-RWAY
    Jeih San Liow
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 0135, USA
    Synapse 61:96-105. 2007
    ..The effects of CsA in rats are mediated by both P-gp blockade and displacement of the radiotracer from plasma proteins. Studies with wild type and knockout mice showed that CsA affected only P-gp in this species...
  4. ncbi request reprint In vivo and in vitro measurement of brain phosphodiesterase 4 in rats after antidepressant administration
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
    Synapse 61:78-86. 2007
    ..g., continuous infusion vs. intermittent injection of antidepressant) in large brain areas. However, the results do not deny possibility of changes in discrete areas, which were not studied in the current study applying PET...
  5. ncbi request reprint Identification and regional distribution in rat brain of radiometabolites of the dopamine transporter PET radioligand [11C]PE2I
    H Umesha Shetty
    PET Radiopharmaceutical Sciences, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C351, MSC 1003, 10 Center Drive, Bethesda, MD 20892 1003, USA
    Eur J Nucl Med Mol Imaging 34:667-78. 2007
    ..We aimed to determine the composition of radioactivity in rat brain after intravenous administration of the dopamine transporter radioligand, [(11)C]PE2I...
  6. ncbi request reprint Radioligand development for PET imaging of beta-amyloid (Abeta)--current status
    Lisheng Cai
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Curr Med Chem 14:19-52. 2007
    ..Also a few radioligands applicable to imaging Abeta plaques in living human brain with positron emission tomography (PET) have emerged, including [(11)C]PIB, [(11)C]SB-13 and [(18)F]FDDNP...
  7. pmc Kinetic brain analysis and whole-body imaging in monkey of [11C]MNPA: a dopamine agonist radioligand
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, Building 31, Bethesda, MD 20892, USA
    Synapse 62:700-9. 2008
    ..4 muSv/MBq (23.5 mrem/mCi). In conclusion, brain uptake of [(11)C]MNPA reflected the density of D(2/3) receptors, quantified relative to serial arterial measurements, and caused moderate to low radiation exposure...
  8. ncbi request reprint PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurements
    Sami S Zoghbi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 47:520-7. 2006
    ....
  9. pmc Occupancy of dopamine D2/3 receptors in rat brain by endogenous dopamine measured with the agonist positron emission tomography radioligand [11C]MNPA
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    Synapse 62:756-63. 2008
    ....
  10. ncbi request reprint Synthesis and structure-activity relationships (SARs) of 1,5-diarylpyrazole cannabinoid type-1 (CB(1)) receptor ligands for potential use in molecular imaging
    Sean R Donohue
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Bioorg Med Chem 14:3712-20. 2006
    ..85), for labeling with carbon-11 and development as a radioligand for imaging brain CB(1) receptors in vivo with positron emission tomography (PET)...
  11. pmc Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography
    Victor W Pike
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, United States
    J Med Chem 54:2687-700. 2011
    ..Overall, [(11)C](S)-10c showed the most favorable receptor-specific signal and kinetics and is now selected for evaluation in human subjects...
  12. ncbi request reprint PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat
    Masao Imaizumi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 1, Room B3 10, 1 Center Drive, MSC 0135, Bethesda, MD 20892 0135, USA
    Neurosci Lett 411:200-5. 2007
    ..In this first study to demonstrate neuroinflammation in vivo with small animal PET, [11C]PBR28 had adequate sensitivity to localize and quantify the associated increase in PBRs...
  13. ncbi request reprint Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammation
    Amira K Brown
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 48:2072-9. 2007
    ..The aim of this study was to estimate the human radiation doses of (11)C-PBR28 based on biodistribution data in monkeys and humans. In addition, we scanned 1 human subject who fortuitously behaved as if he lacked the PBR binding protein...
  14. ncbi request reprint Brain and whole-body imaging in nonhuman primates with [11C]MeS-IMPY, a candidate radioligand for beta-amyloid plaques
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 2035, USA
    Nucl Med Biol 34:681-9. 2007
    ..Calculated dosimetry results are comparable with those for other (11)C-labeled brain imaging radioligands...
  15. ncbi request reprint Synthesis and initial evaluation of [11C](R)-RWAY in monkey-a new, simply labeled antagonist radioligand for imaging brain 5-HT1A receptors with PET
    Julie A McCarron
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, B3 C346A, 10 Center Drive, Bethesda, MD 20892, USA
    Eur J Nucl Med Mol Imaging 34:1670-82. 2007
    ..We aimed to fulfill a need for a radioligand that may be simply labeled with carbon-11 for effective positron emission tomography (PET) imaging of brain 5-HT(1A) receptors...
  16. ncbi request reprint Synthesis and evaluation of N-methyl and S-methyl 11C-labeled 6-methylthio-2-(4'-N,N-dimethylamino)phenylimidazo[1,2-a]pyridines as radioligands for imaging beta-amyloid plaques in Alzheimer's disease
    Lisheng Cai
    Molecular Imaging Branch and Clinical Brain Disorders Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 51:148-58. 2008
    ..The ex vivo brain radiometabolites observed in rats have a peripheral origin. Overall, [ (11)C] 7 merits further evaluation in human subjects...
  17. ncbi request reprint Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography
    Fabrice G Siméon
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, Maryland 20892 1003, USA
    J Med Chem 50:3256-66. 2007
    ..In monkey in vivo, a single polar radiometabolite of [18F]3 appeared rapidly in plasma. [18F]3 merits further evaluation as a PET radioligand for mGluR5 in human subjects...
  18. pmc Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, 31 Center Drive, MSC 2035, Bethesda, MD 20892 2035, USA
    Neuroimage 40:43-52. 2008
    ..In conclusion, with the exception of those subjects who appeared to have no PBR binding, [(11)C]PBR28 is a promising ligand to quantify PBRs and localize inflammation associated with increased densities of PBRs...
  19. doi request reprint Identification of the transition states in the inversion of 1,4-benzodiazepines with the ab initio replica path method
    Yong Sok Lee
    Center for Molecular Modeling, Division of Computational Bioscience, Center for Information Technology, National Institutes of Health, Building 12A, Room 2049, Bethesda, Maryland 20892, USA
    J Phys Chem A 112:1604-11. 2008
    ..These results show the advantages of the replica path method for locating the TSs as well as for constructing the reaction paths for the inversion of 1,4-benzodiazepines...
  20. doi request reprint 11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux
    Sami S Zoghbi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 0135, USA
    J Nucl Med 49:649-56. 2008
    ..We evaluated 11C-loperamide as a PET radiotracer to measure P-gp function in vivo...
  21. ncbi request reprint PET imaging of neurokinin-1 receptors with [(18)F]SPA-RQ in human subjects: assessment of reference tissue models and their test-retest reproducibility
    Fumihiko Yasuno
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
    Synapse 61:242-51. 2007
    ..7 in gray matter regions. In conclusion, a two-parameter reference tissue method (MRTM2) provided reproducible and reliable measurements of [(18)F]SPA-RQ brain uptake using 240 min of both regional and voxel-wise data...
  22. doi request reprint Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors
    Sean R Donohue
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 51:5608-16. 2008
    ..Polar radiometabolites of [11C](-)-12a appeared moderately slowly in plasma. Radioligand [11C](-)-12a is promising for the study of brain CB1 receptors and merits further investigation in human subjects...
  23. ncbi request reprint Whole-body biodistribution and estimation of radiation-absorbed doses of the dopamine D1 receptor radioligand 11C-NNC 112 in humans
    Vanessa L Cropley
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 47:100-4. 2006
    ....
  24. pmc PET radiotracers: crossing the blood-brain barrier and surviving metabolism
    Victor W Pike
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Trends Pharmacol Sci 30:431-40. 2009
    ....
  25. pmc Biodistribution and dosimetry in humans of two inverse agonists to image cannabinoid CB1 receptors using positron emission tomography
    Garth E Terry
    Molecular Imaging Branch, National Institute of Mental Health, 31 Center Drive, Bethesda, MD 20892 2035, USA
    Eur J Nucl Med Mol Imaging 37:1499-506. 2010
    ..We recently reported brain imaging of CB(1) receptors with two PET radioligands: (11)C-MePPEP and (18)F-FMPEP-d (2). Here we describe the biodistribution and dosimetry estimates for these two radioligands...
  26. pmc Comparison of [(11)C]-(R)-PK 11195 and [(11)C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarker
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
    Neuroimage 49:2924-32. 2010
    ..Non-binding may be differentially expressed in organs of the body. The relatively low in vivo specific binding of [(11)C]-(R)-PK 11195 may have obscured its detection of non-binding in peripheral organs...
  27. ncbi request reprint The pyridinyl-6 position of WAY-100635 as a site for radiofluorination--effect on 5-HT1A receptor radioligand behavior in vivo
    Julie A McCarron
    PET Radiopharmaceutical Sciences Section, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
    Mol Imaging Biol 6:17-26. 2004
    ....
  28. pmc Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands
    Victor W Pike
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, United States
    J Med Chem 54:366-73. 2011
    ..31 showed high affinity for HABs, MABs, and LABs. In conclusion, [(11)C]31 represents a promising new chemotype for developing novel TSPO radioligands as biomarkers of neuroinflammation...
  29. pmc Decreased neurokinin-1 (substance P) receptor binding in patients with panic disorder: positron emission tomographic study with [18F]SPA-RQ
    Yota Fujimura
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
    Biol Psychiatry 66:94-7. 2009
    ..We also sought to determine if a drug-induced panic attack releases substance P in brain, as measured by decreased binding of [(18)F]SPA-RQ...
  30. ncbi request reprint Whole-body biodistribution and radiation dosimetry estimates for the PET dopamine transporter probe 18F-FECNT in non-human primates
    Dnyanesh N Tipre
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bldg 1 Rm B3 10, 1 Center Drive, Bethesda, MD 20892 0135, USA
    Nucl Med Commun 25:737-42. 2004
    ..The aim of the current study was to quantify the distribution of radioactivity in three rhesus monkeys after the injection of approximately 185 MBq (5 mCi) of 18F-FECNT...
  31. pmc Nucleophile assisting leaving groups: a strategy for aliphatic 18F-fluorination
    Shuiyu Lu
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 1003, USA
    J Org Chem 74:5290-6. 2009
    ..Under microwave irradiation and without the assistance of a cryptand, such as K2.2.2, primary substrates with select NALGs led to a substantial improvement (2-3-fold) in radiofluorination yields over traditional leaving groups...
  32. ncbi request reprint Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor
    Shui Yu Lu
    PET Radiopharmaceutical Sciences, Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1003, USA
    Lab Chip 4:523-5. 2004
    ....
  33. pmc Efficient and regioselective halogenations of 2-amino-1,3-thiazoles with copper salts
    Fabrice G Siméon
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3C346A, 10 Center Drive, Bethesda, Maryland 20892 1003, USA
    J Org Chem 74:2578-80. 2009
    ..Halogenations proceed easily in the presence of copper(I) or copper(II) chlorides, bromides, or iodides directly in solution or with supported copper halides...
  34. pmc Radiodefluorination of 3-fluoro-5-(2-(2-[18F](fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a radioligand for imaging brain metabotropic glutamate subtype-5 receptors with positron emission tomography, occurs by glutathionylation in rat br
    H Umesha Shetty
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1003, USA
    J Pharmacol Exp Ther 327:727-35. 2008
    ..Thus, glutathionylation at the 2-fluoromethyl group is responsible for the radiodefluorination of [(18)F]SP203 in rat. This study provides the first demonstration of glutathione-promoted radiodefluorination of a PET radioligand...
  35. pmc P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeys
    Jeih San Liow
    Molecular Imaging Branch, PET Department, Clinical Center, National Institutes of Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 50:108-15. 2009
    ..Should further demethylation of 11C-dLop occur, radiometabolites with low entry into the brain are generated. Therefore, we evaluated the ability of 11C-dLop to quantify the function of P-gp at the blood-brain barrier in monkeys...
  36. ncbi request reprint Quantification of brain phosphodiesterase 4 in rat with (R)-[11C]Rolipram-PET
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, Building 1, Room B3 10, 1 Center Drive, MSC 0135, Bethesda, MD 20892 0135, USA
    Neuroimage 26:1201-10. 2005
    ..Phosphodiesterase 4 (PDE4) catabolizes the second messenger 3', 5'-cyclic adenosine monophosphate and may play a critical role in brain diseases. Our aim was to quantify PDE4 in rats with positron emission tomography (PET)...
  37. ncbi request reprint Synthesis and evaluation of two 18F-labeled 6-iodo-2-(4'-N,N-dimethylamino)phenylimidazo[1,2-a]pyridine derivatives as prospective radioligands for beta-amyloid in Alzheimer's disease
    Lisheng Cai
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Bethesda, Maryland 20892, USA
    J Med Chem 47:2208-18. 2004
    ....
  38. pmc Conformational structure and energetics of 2-methylphenyl(2'-methoxyphenyl)iodonium chloride: evidence for solution clusters
    Yong Sok Lee
    Center for Molecular Modeling, Division of Computational Bioscience, Center for Information Technology, National Institutes of Health, Department of Health and Human Services, Building 12A, Room 2049, Bethesda, MD 20892, USA
    Chemistry 16:10418-23. 2010
    ....
  39. 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
    ....
  40. ncbi request reprint Two C-methyl derivatives of [11C]WAY-100635--effects of an amido alpha-methyl group on metabolism and brain 5-HT1A receptor radioligand behavior in monkey
    Julie A McCarron
    MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, DuCane Road, London, W12 0NN, UK
    Mol Imaging Biol 7:209-19. 2005
    ..Here, in a search for a radioligand that overcomes these limitations, we investigated the effects of introducing a single methyl group at either of the carbon atoms alpha to the amide bond in [11C]WAY-100635...
  41. pmc Whole-body biodistribution and radiation dosimetry in monkeys and humans of the phosphodiesterase 4 radioligand [(11)C](R)-rolipram: comparison of two-dimensional planar, bisected and quadrisected image analyses
    David R Sprague
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
    Nucl Med Biol 35:493-500. 2008
    ..The aim of this study was to estimate the human radiation absorbed dose of the radioligand based on its biodistribution in both monkeys and humans...
  42. ncbi request reprint Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo
    Emmanuelle Briard
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 51:17-30. 2008
    ..11)C] 3 and [ (11)C] 10 are effective for imaging PBR in monkey brain. [ (11)C] 10 especially warrants further evaluation in human subjects...
  43. doi request reprint Small effect of dopamine release and no effect of dopamine depletion on [18F]fallypride binding in healthy humans
    Vanessa L Cropley
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    Synapse 62:399-408. 2008
    ..These findings indicate that [18F]fallypride is useful for measuring amphetamine-induced dopamine release, but may be unreliable for estimating tonic dopamine levels, in striatum and extrastriatal regions of healthy humans...
  44. pmc Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function
    Neva Lazarova
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 1103, USA
    J Med Chem 51:6034-43. 2008
    ..11)C]3 is an effective new radiotracer for imaging brain P-gp function and, in favor of future successful quantification, appears free of extensive brain-penetrant radiometabolites...
  45. ncbi request reprint The PET radioligand [carbonyl-(11)C]desmethyl-WAY-100635 binds to 5-HT(1A) receptors and provides a higher radioactive signal than [carbonyl-(11)C]WAY-100635 in the human brain
    Bengt Andree
    Psychiatry Section, Department of Clinical Neuroscience, Karolinska Hospital, Karolinska Institutet, Stockholm, Sweden
    J Nucl Med 43:292-303. 2002
    ..The aim of this PET study was to compare (11)C-WAY with the putative metabolite and selective radioligand [carbonyl-(11)C]desmethyl-WAY-100635 ((11)C-DWAY)...
  46. doi request reprint Pre- and post-synaptic dopamine imaging and its relation with frontostriatal cognitive function in Parkinson disease: PET studies with [11C]NNC 112 and [18F]FDOPA
    Vanessa L Cropley
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 0135, USA
    Psychiatry Res 163:171-82. 2008
    ..These results suggest that striatal dopamine denervation may contribute to some frontostriatal cognitive impairment in moderate stage PD...
  47. pmc Synthesis, ex vivo evaluation, and radiolabeling of potent 1,5-diphenylpyrrolidin-2-one cannabinoid subtype-1 receptor ligands as candidates for in vivo imaging
    Sean R Donohue
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 51:5833-42. 2008
    ....
  48. pmc Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodents
    Garth Terry
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
    Neuroimage 41:690-8. 2008
    ..Radiometabolites of [11C]MePPEP in brain caused distribution volume to be overestimated by approximately 13%...
  49. pmc Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors
    Masao Imaizumi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bldg 31, Rm B2B37, 31 Center Drive, MSC 2035, Bethesda, MD 20892 2035, USA
    Neuroimage 39:1289-98. 2008
    ..The objectives of the current study were to evaluate kinetics of brain uptake, and the influence of the peripheral binding on the arterial input function in rhesus monkey...
  50. ncbi request reprint Development of radioligands for imaging of brain norepinephrine transporters in vivo with positron emission tomography
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Curr Top Med Chem 7:1806-16. 2007
    ..8 min). This review specifically summarizes the present status of the development of (11)C- or (18)F-labeled ligands as tools for imaging NET in brain with PET in support of neuropsychiatric clinical research and drug development...
  51. ncbi request reprint Post-mortem human brain autoradiography of the norepinephrine transporter using (S,S)-[18F]FMeNER-D2
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Eur Neuropsychopharmacol 15:517-20. 2005
    ..The NET-selectivity of binding was confirmed by co-incubation with desipramine. The dual NET/SERT inhibitor duloxetine also inhibited specific binding, whereas PE2I or citalopram had no evident effect...
  52. ncbi request reprint PET imaging of brain with the beta-amyloid probe, [11C]6-OH-BTA-1, in a transgenic mouse model of Alzheimer's disease
    Hiroshi Toyama
    Department of Radiology, Fujita Health University, 1 98, Dengakugakubo, Kutsukake, Toyoake, 470 1192, Aichi, Japan
    Eur J Nucl Med Mol Imaging 32:593-600. 2005
    ..The purpose of this study was to evaluate the capacity of [11C]6-OH-BTA-1 and positron emission tomography (PET) to quantify beta-amyloid (Abeta) plaques in the Tg2576 mouse model of Alzheimer's disease (AD)...
  53. ncbi request reprint N-oxide analogs of WAY-100635: new high affinity 5-HT(1A) receptor antagonists
    Sandrine Marchais-Oberwinkler
    Department of Medicinal Chemistry, University Center for Pharmacy, University of Groningen, Antonius Deusinglaan 1, NL 9713 AV Groningen, The Netherlands
    Bioorg Med Chem 13:883-93. 2005
    ..Ligand 3 may have value as a new pharmacological tool, but not as a radioligand for brain imaging...
  54. ncbi request reprint Synthesis and first in vivo evaluation of new selective high affinity beta1-adrenoceptor radioligands for SPECT based on ICI 89,406
    Stefan Wagner
    Department of Nuclear Medicine, University Hospital Munster, Albert Schweitzer Strasse 33, 48149 Munster, Germany
    Bioorg Med Chem 12:4117-32. 2004
    ..Therefore further studies in a different animal model will be carried out...
  55. ncbi request reprint PET evaluation of novel radiofluorinated reboxetine analogs as norepinephrine transporter probes in the monkey brain
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Synapse 53:57-67. 2004
    ....
  56. ncbi request reprint Specific in vivo binding to the norepinephrine transporter demonstrated with the PET radioligand, (S,S)-[11C]MeNER
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Nucl Med Biol 30:707-14. 2003
    ..Labeled metabolites of [(11)C]MeNER were all more polar. (S,S)-[(11)C]MeNER is a good lead compound in the search for a selective radioligand for quantitation of NET in the human brain in vivo...
  57. ncbi request reprint Distribution of 5-HT4 receptors in the postmortem human brain--an autoradiographic study using [125I]SB 207710
    Katarina Varnas
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Eur Neuropsychopharmacol 13:228-34. 2003
    ....
  58. ncbi request reprint Design of new beta1-selective adrenoceptor ligands as potential radioligands for in vivo imaging
    Klaus Kopka
    Department of Nuclear Medicine, Albert Schweitzer Str 33, University Hospital Munster, 48149, Munster, Germany
    Bioorg Med Chem 11:3513-27. 2003
    ....
  59. ncbi request reprint Synthesis of a [6-pyridinyl-18F]-labelled fluoro derivative of WAY-100635 as a candidate radioligand for brain 5-HT1A receptor 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 11:2769-82. 2003
    ..7 GBq) aliquot of a batch of cyclotron-produced [(18)F]fluoride. This (18)F-labelled radioligand is now being evaluated in PET studies...
  60. ncbi request reprint Imaging the GABA-benzodiazepine receptor subtype containing the alpha5-subunit in vivo with [11C]Ro15 4513 positron emission tomography
    Anne Lingford-Hughes
    Psychopharmacology Unit, School of Medical Science, University of Bristol, UK
    J Cereb Blood Flow Metab 22:878-89. 2002
    ..The authors conclude that [11C]Ro15 4513 PET labels in vivo the GABA-benzodiazepine receptor containing the alpha5 subtype in limbic structures and can be used to further explore the functional role of this subtype in humans...
  61. ncbi request reprint Synthesis and positron emission tomography evaluation of three norepinephrine transporter radioligands: [C-11]desipramine, [C-11]talopram and [C-11]talsupram
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176, Stockholm, Sweden
    Mol Imaging Biol 8:1-8. 2006
    ..These metabolites were all more polar than their parent radioligand. The data show that these radioligands are inferior to existing radioligands for the study of brain NET with PET in vivo...
  62. ncbi request reprint Amyloid imaging: from benchtop to bedside
    Chunying Wu
    Department of Medicinal Chemistry, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA
    Curr Top Dev Biol 70:171-213. 2005
    ..Furthermore, the success in the development of amyloid-imaging agents helps with the development of imaging agents for in vivo studies of other AD pathologies in particular and of neurodegenerative disorders in general...
  63. ncbi request reprint PET imaging of brain 5-HT1A receptors in rat in vivo with 18F-FCWAY and improvement by successful inhibition of radioligand defluorination with miconazole
    Dnyanesh N Tipre
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 47:345-53. 2006
    ..Our aim was to demonstrate with a rat model that defluorination of 18F-FCWAY may be inhibited in vivo to improve its applicability to measuring brain regional 5-HT1A receptor densities...
  64. ncbi request reprint Disulfiram inhibits defluorination of (18)F-FCWAY, reduces bone radioactivity, and enhances visualization of radioligand binding to serotonin 5-HT1A receptors in human brain
    Yong Hoon Ryu
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Nucl Med 48:1154-61. 2007
    ..We previously showed that miconazole, an inhibitor of CYP2E1, blocks defluorination of FCWAY in rats. Here, we used (18)F-FCWAY to test the ability of the less toxic agent disulfiram to inhibit defluorination in humans...
  65. ncbi request reprint Kinetic evaluation in nonhuman primates of two new PET ligands for peripheral benzodiazepine receptors in brain
    Masao Imaizumi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 2035, USA
    Synapse 61:595-605. 2007
    ..A critical factor for human use will be whether the tracer has adequately fast wash out from brain relative to the half-life of the radionuclide to obtain stable values of distribution volume...
  66. ncbi request reprint Quantification of serotonin 5-HT1A receptors in humans with [11C](R)-(-)-RWAY: radiometabolite(s) likely confound brain measurements
    Xiang Yang Zhang
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    Synapse 61:469-77. 2007
    ..Although prior studies in rodents and nonhuman primates showed [(11)C](R)-(-)-RWAY to be a promising radiotracer, we suspect that a species difference in metabolism caused this serious deficiency in humans...
  67. ncbi request reprint The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain
    Fumihiko Yasuno
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 2035, USA
    Neuropsychopharmacology 33:259-69. 2008
    ..These promising results in monkey justify studying this radioligand in human subjects...
  68. ncbi request reprint Lipophilic analogs of thioflavin S as novel amyloid-imaging agents
    Chunying Wu
    College of Pharmacy, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612, USA
    Curr Alzheimer Res 3:259-66. 2006
    ..Potential applications of these amyloid binding agents include facilitating drug screening in animal models and use as in vivo markers of early and definitive diagnosis of AD...
  69. ncbi request reprint Human biodistribution and radiation dosimetry of the tachykinin NK1 antagonist radioligand [18F]SPA-RQ: comparison of thin-slice, bisected, and 2-dimensional planar image analysis
    David R Sprague
    Molecular Imaging Branch, NIMH, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 48:100-7. 2007
    ..The aims of this study were to estimate the radiation safety profile and relative risks of [(18)F]SPA-RQ with 3 different methods of image analysis...
  70. ncbi request reprint Synthesis of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET
    Magnus Schou
    Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S 17176 Stockholm, Sweden
    Bioorg Med Chem 15:616-25. 2007
    ....
  71. ncbi request reprint Quantification of serotonin 5-HT1A receptors in monkey brain with [11C](R)-(-)-RWAY
    Fumihiko Yasuno
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 0135, USA
    Synapse 60:510-20. 2006
    ....
  72. ncbi request reprint Development of new brain imaging agents based upon nocaine-modafinil hybrid monoamine transporter inhibitors
    John L Musachio
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346, 10 Center Drive, Bethesda, MD 20892 1003, USA
    Bioorg Med Chem Lett 16:3101-4. 2006
    ..Contrary to our expectations, both of these ligands provided brain images that were more typical of those shown by agents binding to the DAT...
  73. ncbi request reprint Imaging and in vivo quantitation of beta-amyloid: an exemplary biomarker for Alzheimer's disease?
    Lisa Nichols
    Molecular Imaging Branch, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    Biol Psychiatry 59:940-7. 2006
    ..This review explores the utility of amyloid as a biomarker and the use of positron emission tomography and magnetic resonance imaging in the diagnosis and treatment of AD...
  74. ncbi request reprint Synthesis of (+)- and (-)-cis-2-[(1-adamantylamino)-methyl]-1-phenylcyclopropane derivatives as high affinity probes for sigma1 and sigma2 binding sites
    Agostino Marrazzo
    Department of Pharmaceutical Sciences, University of Catania, Catana, Italy
    Farmaco 57:45-53. 2002
    ..The N-desmethyl analogues, which are also high affinity ligands, were prepared and shown to undergo satisfactory methylation with iodomethane...
  75. ncbi request reprint Development of novel amyloid imaging agents based upon thioflavin S
    Jingjun Wei
    School of Pharmacy, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612, USA
    Curr Alzheimer Res 2:109-14. 2005
    ..We hypothesized that neutral analogs, based upon the major component, could be developed as novel amyloid imaging agents, that exhibit complementary binding properties and pharmacokinetic profiles compatible with potential human studies...