Robert B Innis

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. 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
  2. pmc Is metabotropic glutamate receptor 5 upregulated in prefrontal cortex in fragile X syndrome?
    Talakad G Lohith
    Molecular Imaging Branch, National Institute of Mental Health, 10 Center Drive, Bethesda, MD 20892 1026, USA
    Mol Autism 4:15. 2013
  3. 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
  4. 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
  5. ncbi request reprint Biodistribution and radiation dosimetry of the serotonin transporter ligand 11C-DASB determined from human whole-body PET
    Jian Qiang Lu
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 45:1555-9. 2004
  6. 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
  7. 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
  8. pmc D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model
    Mette Skinbjerg
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
    Neuroimage 50:1402-7. 2010
  9. 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
  10. 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

Collaborators

Detail Information

Publications70

  1. 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...
  2. pmc Is metabotropic glutamate receptor 5 upregulated in prefrontal cortex in fragile X syndrome?
    Talakad G Lohith
    Molecular Imaging Branch, National Institute of Mental Health, 10 Center Drive, Bethesda, MD 20892 1026, USA
    Mol Autism 4:15. 2013
    ..However, mGluR5 density in human FXS remains unknown...
  3. 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...
  4. 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...
  5. ncbi request reprint Biodistribution and radiation dosimetry of the serotonin transporter ligand 11C-DASB determined from human whole-body PET
    Jian Qiang Lu
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
    J Nucl Med 45:1555-9. 2004
    ..The goal of this study was to provide dosimetry estimates for 11C-DASB based on human whole-body PET...
  6. 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...
  7. 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...
  8. pmc D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse model
    Mette Skinbjerg
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
    Neuroimage 50:1402-7. 2010
    ..In addition, this study demonstrates the utility of small animal PET to study receptor trafficking in vivo in genetically modified mice...
  9. 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...
  10. 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...
  11. pmc Dopamine beta-hydroxylase-deficient mice have normal densities of D(2) dopamine receptors in the high-affinity state based on in vivo PET imaging and in vitro radioligand binding
    Mette Skinbjerg
    Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
    Synapse 64:699-703. 2010
    ..In summary, our results suggest that DBH knockout mice have normal levels of D(2) receptors in the high-affinity state and that additional mechanisms contribute to their behavioral sensitivity to psychostimulants...
  12. 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...
  13. 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...
  14. 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...
  15. 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...
  16. ncbi request reprint Absolute quantification of regional cerebral glucose utilization in mice by 18F-FDG small animal PET scanning and 2-14C-DG autoradiography
    Hiroshi Toyama
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, USA
    J Nucl Med 45:1398-405. 2004
    ..In addition, we compared the rCMR(glc) values under isoflurane, ketamine and xylazine anesthesia, and awake states...
  17. 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
    ....
  18. 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...
  19. 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...
  20. 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. ..
  21. 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...
  22. 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
    ....
  23. 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...
  24. 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...
  25. 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...
  26. 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
    ....
  27. 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...
  28. 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
    ....
  29. 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...
  30. 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...
  31. 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...
  32. 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...
  33. 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...
  34. 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...
  35. pmc Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans
    Yasuyuki Kimura
    Molecular Imaging Branch, National Institute of Mental Health, 10 Center Drive, Bethesda, MD 20892 1026, USA
    Eur J Nucl Med Mol Imaging 37:1943-9. 2010
    ....
  36. 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...
  37. 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...
  38. 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...
  39. 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...
  40. 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...
  41. 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...
  42. 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
    ....
  43. 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...
  44. 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...
  45. 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...
  46. 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%...
  47. 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...
  48. 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...
  49. 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)...
  50. 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...
  51. 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...
  52. 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
    ....
  53. 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...
  54. 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...
  55. 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
    ....
  56. 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)...
  57. 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...
  58. 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...
  59. 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...
  60. ncbi request reprint PET [11C]DASB imaging of serotonin transporters in patients with alcoholism
    Amira K Brown
    Molecular Imaging Branch, National Institute of Mental Health, One Center Drive, Bethesda, MD 20892, USA
    Alcohol Clin Exp Res 31:28-32. 2007
    ..We measured densities of the serotonin transporter (SERT) in a moderate-sized sample of alcoholic patients who were assessed for aggressive characteristics...
  61. 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...
  62. 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
    ....
  63. pmc Biodistribution and radiation dosimetry in humans of a new PET ligand, (18)F-PBR06, to image translocator protein (18 kDa)
    Yota Fujimura
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 2035, USA
    J Nucl Med 51:145-9. 2010
    ..The objective of this study was to estimate the radiation absorbed doses of (18)F-PBR06 based on biodistribution data in humans...
  64. 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...
  65. pmc Increased in vivo expression of an inflammatory marker in temporal lobe epilepsy
    Jussi Hirvonen
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892 1026, USA
    J Nucl Med 53:234-40. 2012
    ..In this study, we sought to determine whether in vivo expression of TSPO is increased ipsilateral to the seizure focus in patients with temporal lobe epilepsy...
  66. 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...
  67. 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...
  68. 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...
  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. 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...