Sami S Zoghbi

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. 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
  2. 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
  3. 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
  4. pmc A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 1026, USA
    J Cereb Blood Flow Metab 33:53-8. 2013
  5. pmc Imaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligands
    Garth E Terry
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 51:112-20. 2010
  6. 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
  7. pmc P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
    J Nucl Med 51:559-66. 2010
  8. 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
  9. 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
  10. 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

Detail Information

Publications79

  1. 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...
  2. 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
    ....
  3. 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...
  4. pmc A genetic polymorphism for translocator protein 18 kDa affects both in vitro and in vivo radioligand binding in human brain to this putative biomarker of neuroinflammation
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 1026, USA
    J Cereb Blood Flow Metab 33:53-8. 2013
    ..011). Our results show that TSPO genotype influences PBR28 binding in vitro and in vivo. Correcting for this genotype increased statistical power in our postmortem study and is recommended for in vivo positron emission tomography studies...
  5. pmc Imaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligands
    Garth E Terry
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 51:112-20. 2010
    ..We evaluated several promising analogs in the monkey brain and chose the (18)F-di-deutero fluoromethoxy analog ((18)F-FMPEP-d(2)) to evaluate further in the human brain...
  6. 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...
  7. pmc P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
    J Nucl Med 51:559-66. 2010
    ..We examined the ability of (11)C-dLop to quantify P-gp function in humans after increasing doses of tariquidar, an inhibitor of P-gp...
  8. 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...
  9. 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...
  10. 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...
  11. 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...
  12. 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...
  13. pmc Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET
    Emmanuelle Briard
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 52:688-99. 2009
    ..In rat, a low level radiometabolite of intermediate lipophilicity was identified as [18F]2-fluoro-N-(2-phenoxyphenyl)acetamide ([18F]11). [18F]9 is a promising radioligand for future imaging of PBR in living human brain...
  14. 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...
  15. pmc Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout mice
    Nicholas Seneca
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Nucl Med Biol 37:335-45. 2010
    ..We aimed to test whether inhibition of CYP3A4 with ketoconazole might reduce the metabolism of [(11)C]loperamide and [(11)C]dLop in mice, and thereby improve the quality of these radiotracers...
  16. pmc Metabotropic glutamate subtype 5 receptors are quantified in the human brain with a novel radioligand for PET
    Amira K Brown
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland, USA
    J Nucl Med 49:2042-8. 2008
    ....
  17. doi request reprint Synthesis and characterization in monkey of [11C]SP203 as a radioligand for imaging brain metabotropic glutamate 5 receptors
    Fabrice G Siméon
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Eur J Nucl Med Mol Imaging 39:1949-58. 2012
    ..4 min) and to characterize its behavior as a radioligand with PET in the monkey...
  18. 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...
  19. 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...
  20. 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
    ....
  21. 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...
  22. pmc [¹¹C]Rhodamine-123: synthesis and biodistribution in rodents
    Xiaofeng Bao
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892 1003, USA
    Nucl Med Biol 39:1128-36. 2012
    ..For this purpose, we aimed to label rhodamine-123 with carbon-11 (t(1/2)=20.4min) and to study its biodistribution in rodents...
  23. pmc Brain and whole-body imaging of nociceptin/orphanin FQ peptide receptor in humans using the PET ligand 11C-NOP-1A
    Talakad G Lohith
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1026, USA
    J Nucl Med 53:385-92. 2012
    ..Here, we assessed the ability of (11)C-NOP-1A to quantify NOP receptors in human brain and estimated its radiation safety profile...
  24. 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...
  25. 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%...
  26. pmc Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoprotein
    Nicholas Seneca
    National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
    J Nucl Med 50:807-13. 2009
    ..The purposes of this study were to determine whether (11)C-dLop is a substrate for P-gp at the blood-brain barrier in humans and to measure the distribution of radioactivity in the entire body to estimate radiation exposure...
  27. 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...
  28. 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...
  29. pmc Population-based input function and image-derived input function for [¹¹C](R)-rolipram PET imaging: methodology, validation and application to the study of major depressive disorder
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
    Neuroimage 63:1532-41. 2012
    ....
  30. pmc In vivo radioligand binding to translocator protein correlates with severity of Alzheimer's disease
    William C Kreisl
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
    Brain 136:2228-38. 2013
    ..11)C-PBR28 may be useful in longitudinal studies to mark the conversion from mild cognitive impairment or to assess response to experimental treatments of Alzheimer's disease. ..
  31. pmc Quantification of metabotropic glutamate subtype 5 receptors in the brain by an equilibrium method using 18F-SP203
    Yasuyuki Kimura
    Molecular Imaging Branch, 10 Center Drive, MSC 1026, Bldg 10, National Institute of Mental Health, Bethesda, MD 20892, USA
    Neuroimage 59:2124-30. 2012
    ..In addition, when using 18F-SP203, the equilibrium method is more efficient because it requires much less data...
  32. pmc Image-derived input function for human brain using high resolution PET imaging with [C](R)-rolipram and [C]PBR28
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health NIMH, National Institutes of Health NIH, Bethesda, Maryland, United States of America
    PLoS ONE 6:e17056. 2011
    ..Three of the methods required arterial blood samples to scale the image-input, and four were blood-free methods...
  33. pmc Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET
    Pavitra Kannan
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 108:2593-8. 2011
    ..In summary, tariquidar and [(11)C]dLop can be used in combination to selectively measure the function of P-gp at the blood-brain barrier...
  34. pmc PET measurement of the in vivo affinity of 11C-(R)-rolipram and the density of its target, phosphodiesterase-4, in the brains of conscious and anesthetized rats
    Tetsuji Itoh
    National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
    J Nucl Med 50:749-56. 2009
    ..We also studied 2 critical factors in small-animal PET scans: the influence of anesthesia and the difference in binding under in vivo and in vitro conditions...
  35. 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...
  36. 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...
  37. 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...
  38. pmc Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype
    Xiaofeng Bao
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Room B3 C346A, 10 Center Drive, Bethesda, Maryland 20892, USA
    J Med Chem 55:2406-15. 2012
    ..The nitro compound 12 was found to have even higher H(3) receptor affinity, indicating the potential of this chemotype for the development of further promising PET radioligands...
  39. pmc N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier
    Pavitra Kannan
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    Drug Metab Dispos 38:917-22. 2010
    ..e., a competitive substrate). Because low concentrations of radiotracer are used for PET imaging, [(11)C]dLop acts selectively and only as a substrate for P-gp...
  40. 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...
  41. pmc Quantification of translocator protein (18 kDa) in the human brain with PET and a novel radioligand, (18)F-PBR06
    Yota Fujimura
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 50:1047-53. 2009
    ....
  42. pmc Brain and whole-body imaging in rhesus monkeys of 11C-NOP-1A, a promising PET radioligand for nociceptin/orphanin FQ peptide receptors
    Yasuyuki Kimura
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 1026, USA
    J Nucl Med 52:1638-45. 2011
    ..4) for PET brain imaging. Here, we assessed the utility of (11)C-NOP-1A for quantifying NOP receptors in the monkey brain and estimated the radiation safety profile of this radioligand based on its biodistribution in monkeys...
  43. pmc PET reveals inflammation around calcified Taenia solium granulomas with perilesional edema
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health Bethesda, Maryland, United States of America
    PLoS ONE 8:e74052. 2013
    ..To investigate whether perilesional edema is due to inflammation, we imaged a marker of neuroinflammation, translocater protein (TSPO), using positron emission tomography (PET) and the selective ligand (11)C-PBR28...
  44. pmc Downregulation of brain phosphodiesterase type IV measured with 11C-(R)-rolipram positron emission tomography in major depressive disorder
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 1026, USA
    Biol Psychiatry 72:548-54. 2012
    ..This study sought to quantify the binding of 11C-(R)-rolipram, a PDE4 inhibitor, as an indirect measure of this enzyme's activity in the brain of individuals with major depressive disorder (MDD) compared with healthy control subjects...
  45. pmc Image-derived input function in PET brain studies: blood-based methods are resistant to motion artifacts
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, NIH, Bethesda, Maryland 20892 2035, USA
    Nucl Med Commun 33:982-9. 2012
    ..The present study used both simulated and clinical [11C](R)-rolipram data to assess the robustness of a blood-based IDIF method (a method that is ultimately normalized with blood samples) with regard to motion artifacts...
  46. pmc Kinetic analysis in human brain of [11C](R)-rolipram, a positron emission tomographic radioligand to image phosphodiesterase 4: a retest study and use of an image-derived input function
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    Neuroimage 54:1903-9. 2011
    ..The aims of this study were to perform kinetic modeling of [(11)C](R)-rolipram in healthy humans using an arterial input function and to replace this arterial input in humans with an image-derived input function...
  47. pmc In vivo binding of protoporphyrin IX to rat translocator protein imaged with positron emission tomography
    Harushige Ozaki
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
    Synapse 64:649-53. 2010
    ..Although PPIX at physiological concentrations would likely occupy an insignificant percentage of TSPOs, it does reach high-enough concentrations in porphyria to occupy and have pharmacological effects via this target...
  48. pmc Population-based input function modeling for [(18)F]FMPEP-d 2, an inverse agonist radioligand for cannabinoid CB1 receptors: validation in clinical studies
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
    PLoS ONE 8:e60231. 2013
    ....
  49. pmc 11C-LY2428703, a positron emission tomographic radioligand for the metabotropic glutamate receptor 1, is unsuitable for imaging in monkey and human brains
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, 10 Center Drive, Bethesda, MD 20892, USA
    EJNMMI Res 3:47. 2013
    ..The present study evaluated 11C-LY2428703 for imaging mGluR1 in monkey and human brains...
  50. pmc Binding of a tritiated inverse agonist to cannabinoid CB1 receptors is increased in patients with schizophrenia
    Kimberly J Jenko
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1003, USA
    Schizophr Res 141:185-8. 2012
    ..05)...
  51. 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
    ....
  52. pmc Retest imaging of [11C]NOP-1A binding to nociceptin/orphanin FQ peptide (NOP) receptors in the brain of healthy humans
    Talakad G Lohith
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA Electronic address
    Neuroimage 87:89-95. 2014
    ..Moderately good reproducibility and reliability measures of VT for [(11)C]NOP-1A make it a useful PET ligand for comparing NOP receptor binding between different subject groups or under different conditions in the same subject. ..
  53. 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)...
  54. pmc On quantitative relationships between drug-like compound lipophilicity and plasma free fraction in monkey and human
    Sami S Zoghbi
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Pharm Sci 101:1028-39. 2012
    ..4) distribution strongly models that between plasma proteins and remaining plasma and moreover that (m) logD accounts for over 74% of compound (m) logD(pr/pl) and is a strong determinant of f(P)...
  55. 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...
  56. pmc Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligand
    Garth E Terry
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
    Neuroimage 48:362-70. 2009
    ..These results suggest that brain uptake can be used for within subject studies (e.g., to measure receptor occupancy by medications) but that distribution volume remains the gold standard for accurate measurements between groups...
  57. pmc Translocator protein PET imaging for glial activation in multiple sclerosis
    Unsong Oh
    Neuroimmunology Branch, National Institute of Neurological Disorders and Stroke, National Institutes of Health, 10 Center Drive, Bldg 10 Rm 5C103, Bethesda, MD 20892, USA
    J Neuroimmune Pharmacol 6:354-61. 2011
    ..Global [(11)C]PBR28 binding showed correlation with disease duration (p = 0.041), but not with measures of clinical disability. These results further define TSPO as an informative marker of glial activation in MS...
  58. pmc Comparison of 18F- and 11C-labeled aryloxyanilide analogs to measure translocator protein in human brain using positron emission tomography
    Leah P Dickstein
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1026, USA
    Eur J Nucl Med Mol Imaging 38:352-7. 2011
    ....
  59. pmc In vitro and in vivo evaluation of (11)C-SD5024, a novel PET radioligand for human brain imaging of cannabinoid CB1 receptors
    Tetsuya Tsujikawa
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
    Neuroimage 84:733-41. 2014
    ..The results suggest that (11)C-SD5024 is slightly better than or equivalent to (11)C-OMAR and that both are suitable for clinical studies, especially those that involve two scans in one day. ..
  60. pmc Widespread decrease of nicotinic acetylcholine receptors in Parkinson's disease
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 1, Room B3 10, I Center Drive, MSC 0135, Bethesda, MD, USA
    Ann Neurol 59:174-7. 2006
    ..Nicotinic acetylcholine receptors have close interactions with the dopaminergic system and play critical roles in cognitive function. The purpose of this study was to compare these receptors between living PD patients and healthy subjects...
  61. pmc Propofol decreases in vivo binding of 11C-PBR28 to translocator protein (18 kDa) in the human brain
    Christina S Hines
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 1026, USA
    J Nucl Med 54:64-9. 2013
    ..The purpose of this study was to determine whether the anesthetic propofol alters brain uptake of (11)C-PBR28 in healthy subjects...
  62. 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...
  63. 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...
  64. 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...
  65. ncbi request reprint Persistent dopamine functions of neurons derived from embryonic stem cells in a rodent model of Parkinson disease
    José A Rodríguez-Gómez
    Laboratory of Molecular Biology, National Institute of Neurological Disorders and Stroke, Porter Neuroscience Research Center, National Institute of Health, Bethesda, Maryland 20892, USA
    Stem Cells 25:918-28. 2007
    ..This work supports continued interest in ES cells as a source of functional DA neurons...
  66. 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
    ....
  67. pmc Evaluation in vitro and in animals of a new 11C-labeled PET radioligand for metabotropic glutamate receptors 1 in brain
    Paolo Zanotti-Fregonara
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892, USA
    Eur J Nucl Med Mol Imaging 40:245-53. 2013
    ..Two allosteric modulators of the group I metabotropic glutamate receptors (mGluR1 and mGluR5) were evaluated as positron emission tomography (PET) radioligands for mGluR1...
  68. ncbi request reprint Quantification of nicotinic acetylcholine receptors in human brain using [123I]5-I-A-85380 SPET
    Masahiro Fujita
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD 20892 0135, USA
    Eur J Nucl Med Mol Imaging 30:1620-9. 2003
    ..These results demonstrate the feasibility of quantifying high-affinity type nAChRs using [123I]5-I-A-85380 in humans and support the use of VT' measured by bolus studies...
  69. ncbi request reprint Influence of acetylcholine levels on the binding of a SPECT nicotinic acetylcholine receptor ligand [123I]5-I-A-85380
    Masahiro Fujita
    Department of Psychiatry, Yale University and VA Connecticut HCS, West Haven, Connecticut, USA
    Synapse 48:116-22. 2003
    ..However, decreased thalamic activities could have been caused by other mechanisms, including internalization of the receptor with an associated decreased affinity for radioligand...
  70. ncbi request reprint Effect of scatter correction on the compartmental measurement of striatal and extrastriatal dopamine D2 receptors using [123I]epidepride SPET
    Masahiro Fujita
    Department of Psychiatry, Yale University School of Medicine and VA Connecticut Healthcare System, West Haven, CT, USA
    Eur J Nucl Med Mol Imaging 31:644-54. 2004
    ..It is concluded that SC is required for accurate quantification of distribution volumes of receptor ligands in SPET studies...
  71. ncbi request reprint Chemical fate of the nicotinic acetylcholinergic radiotracer [123I]5-IA-85380 in baboon brain and plasma
    Ronald M Baldwin
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06510, USA
    Nucl Med Biol 33:549-54. 2006
    ....
  72. ncbi request reprint Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-beta-Carbomethoxy-3-beta-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET
    Thomas Chaly
    Department of Medicine, North Shore University Hospital, NYU Medical College, PET Research, Manhasset, NY 11030, USA
    Nucl Med Biol 31:125-31. 2004
    ..18F]FPCBT displayed good brain uptake and its high target to non target ratio indicate that it is a potential candidate for DAT imaging...
  73. ncbi request reprint Benzodiazepine receptor distribution in severe intractable tinnitus
    Aditya Daftary
    Department of Diagnostic Radiology, Yale University, New Haven, CT 06510, USA
    Int Tinnitus J 10:17-23. 2004
    ..045). Current understanding suggests GABA receptors and the temporal lobe system as the final common pathway. This pilot study suggests possible alterations on 123I-iomazenil SPECT imaging and the need for larger studies...
  74. ncbi request reprint Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjects
    Masahiro Fujita
    Department of Psychiatry, Yale University School of Medicine and VA Connecticut Healthcare System, VA Connecticut 116A2, West Haven 06516, USA
    Eur J Nucl Med Mol Imaging 29:183-90. 2002
    ..These results suggest that [123I]5-I-A-85380 is a promising SPET agent to image alpha4beta2 nAChRs in humans, with acceptable dosimetry and high brain uptake...
  75. ncbi request reprint Central type benzodiazepine receptors in Gulf War veterans with posttraumatic stress disorder
    Masahiro Fujita
    Department of Psychiatry, Yale University and Veterans Affairs Connecticut Healthcare System, West Haven, Connecticut, USA
    Biol Psychiatry 56:95-100. 2004
    ..To assess the generalizability of this finding to patients with more recent history, we studied central type benzodiazepine receptors in Gulf War veterans with posttraumatic stress disorder...
  76. ncbi request reprint Synthesis of cyclopentadienyltricarbonyl rhenium phenyltropanes by double ligand transfer: organometallic ligands for the dopamine transporter
    Richard R Cesati
    Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, Illinois 61801, USA
    Bioconjug Chem 13:29-39. 2002
    ..By contrast, the 3 beta-conjugates were poor DAT binders. The modular nature of these systems offers considerable flexibility that could be used to improve the binding characteristics of these compounds further...
  77. ncbi request reprint Striatal dopamine transporter availability with [123I]beta-CIT SPECT is unrelated to gender or menstrual cycle
    Susan E Best
    Department of Psychiatry, Yale University School of Medicine, Suite 600, One Church Street, New Haven, CT 06510, USA
    Psychopharmacology (Berl) 183:181-9. 2005
    ..The effect of gender and female menstrual cycle on human striatal dopamine transporters (DATs) was investigated with single-photon emission computed tomography (SPECT) using the ligand 2beta-carbomethoxy-3beta-(4-[(123)I]iodophenyl)tropane...
  78. ncbi request reprint Cerebral benzodiazepine receptors in depressed patients measured with [123I]iomazenil SPECT
    Akira Kugaya
    Department of Psychiatry, Yale University, New Haven, CT, USA
    Biol Psychiatry 54:792-9. 2003
    ..No in vivo study has been reported to measure postsynaptic GABA receptors in the patients...
  79. ncbi request reprint Age-related decline in dopamine transporters: analysis of striatal subregions, nonlinear effects, and hemispheric asymmetries
    Christopher H van Dyck
    Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06510, USA
    Am J Geriatr Psychiatry 10:36-43. 2002
    ..These findings have implications not only for healthy aging but also for neurodegenerative disorders such as PD...