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Genomes and Genes | Robert B InnisSummaryAffiliation: National Institutes of Health Country: USA Publications
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Consensus nomenclature for in vivo imaging of reversibly binding radioligandsRobert B Innis
National Institute of Mental Health, Molecular Imaging Branch, Bethesda, Maryland, USA
J Cereb Blood Flow Metab 27:1533-9. 2007..An international group of experts in pharmacokinetic modeling recommends a consensus nomenclature to describe in vivo molecular imaging of reversibly binding radioligands...
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivoEmmanuelle 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...
Imaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligandsGarth 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...
D2 dopamine receptor internalization prolongs the decrease of radioligand binding after amphetamine: a PET study in a receptor internalization-deficient mouse modelMette 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...
Pre- and post-synaptic dopamine imaging and its relation with frontostriatal cognitive function in Parkinson disease: PET studies with [11C]NNC 112 and [18F]FDOPAVanessa 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...
Biodistribution and radiation dosimetry of the serotonin transporter ligand 11C-DASB determined from human whole-body PETJian 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...
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 diseaseLisheng 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...
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 biomarkerWilliam 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...
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 bindingMette 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...
Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoproteinNicholas 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...
Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptorsMasao 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...
P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamideWilliam 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...
Quantification of serotonin 5-HT1A receptors in humans with [11C](R)-(-)-RWAY: radiometabolite(s) likely confound brain measurementsXiang 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...
Synthesis and initial evaluation of [11C](R)-RWAY in monkey-a new, simply labeled antagonist radioligand for imaging brain 5-HT1A receptors with PETJulie 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...
Occupancy of dopamine D2/3 receptors in rat brain by endogenous dopamine measured with the agonist positron emission tomography radioligand [11C]MNPANicholas Seneca
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892 2035, USA
Synapse 62:756-63. 2008....
In vivo and in vitro measurement of brain phosphodiesterase 4 in rats after antidepressant administrationMasahiro 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...
Brain and whole-body imaging in nonhuman primates with [11C]MeS-IMPY, a candidate radioligand for beta-amyloid plaquesNicholas 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...
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 analysesDavid 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...
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp functionNeva 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...
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 brH 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...
Metabotropic glutamate subtype 5 receptors are quantified in the human brain with a novel radioligand for PETAmira K Brown
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland, USA
J Nucl Med 49:2042-8. 2008....
P-glycoprotein function at the blood-brain barrier imaged using 11C-N-desmethyl-loperamide in monkeysJeih 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...
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PETEmmanuelle 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...
Absolute quantification of regional cerebral glucose utilization in mice by 18F-FDG small animal PET scanning and 2-14C-DG autoradiographyHiroshi 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...
Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout miceNicholas 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...
Brain and whole-body imaging of nociceptin/orphanin FQ peptide receptor in humans using the PET ligand 11C-NOP-1ATalakad 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...
Identification and regional distribution in rat brain of radiometabolites of the dopamine transporter PET radioligand [11C]PE2IH 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...
Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammationAmira 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...
PET imaging of brain 5-HT1A receptors in rat in vivo with 18F-FCWAY and improvement by successful inhibition of radioligand defluorination with miconazoleDnyanesh 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...
PET imaging of neurokinin-1 receptors with [(18)F]SPA-RQ in human subjects: assessment of reference tissue models and their test-retest reproducibilityFumihiko 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...
Whole-body biodistribution and estimation of radiation-absorbed doses of the dopamine D1 receptor radioligand 11C-NNC 112 in humansVanessa 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....
Kinetic evaluation in nonhuman primates of two new PET ligands for peripheral benzodiazepine receptors in brainMasao 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...
Whole-body biodistribution and radiation dosimetry estimates for the PET dopamine transporter probe 18F-FECNT in non-human primatesDnyanesh 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...
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 chemotypeXiaofeng 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...
Quantification of metabotropic glutamate subtype 5 receptors in the brain by an equilibrium method using 18F-SP203Yasuyuki 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...
Effect of a P-glycoprotein inhibitor, Cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(-)-RWAYJeih 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...
Image-derived input function for human brain using high resolution PET imaging with [C](R)-rolipram and [C]PBR28Paolo 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...
Quantification of serotonin 5-HT1A receptors in monkey brain with [11C](R)-(-)-RWAYFumihiko Yasuno
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892-0135, USA
Synapse 60:510-20. 2006....
Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humansYasuyuki 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....
Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodentsGarth 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%...
Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammationMasahiro 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...
11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein effluxSami 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...
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 plaquesLisheng 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...
Brain and whole-body imaging in rhesus monkeys of 11C-NOP-1A, a promising PET radioligand for nociceptin/orphanin FQ peptide receptorsYasuyuki 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...
N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrierPavitra 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...
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...
Disulfiram inhibits defluorination of (18)F-FCWAY, reduces bone radioactivity, and enhances visualization of radioligand binding to serotonin 5-HT1A receptors in human brainYong 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...
Quantification of translocator protein (18 kDa) in the human brain with PET and a novel radioligand, (18)F-PBR06Yota 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....
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 ratsTetsuji 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...
Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PETPavitra 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...
PET [11C]DASB imaging of serotonin transporters in patients with alcoholismAmira 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...
Increased in vivo expression of an inflammatory marker in temporal lobe epilepsyJussi 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...
Biodistribution and dosimetry in humans of two inverse agonists to image cannabinoid CB1 receptors using positron emission tomographyGarth 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...
In vivo binding of protoporphyrin IX to rat translocator protein imaged with positron emission tomographyHarushige 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...
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 functionPaolo 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...
Decreased neurokinin-1 (substance P) receptor binding in patients with panic disorder: positron emission tomographic study with [18F]SPA-RQYota 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...
Quantification of brain phosphodiesterase 4 in rat with (R)-[11C]Rolipram-PETMasahiro 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)...
Kinetic brain analysis and whole-body imaging in monkey of [11C]MNPA: a dopamine agonist radioligandNicholas 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...
Small effect of dopamine release and no effect of dopamine depletion on [18F]fallypride binding in healthy humansVanessa 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...
PET imaging of the dopamine transporter with 18F-FECNT: a polar radiometabolite confounds brain radioligand measurementsSami 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....
Human biodistribution and radiation dosimetry of the tachykinin NK1 antagonist radioligand [18F]SPA-RQ: comparison of thin-slice, bisected, and 2-dimensional planar image analysisDavid 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...
Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligandGarth 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...
Effects of cAMP-dependent protein kinase activator and inhibitor on in vivo rolipram binding to phosphodiesterase 4 in conscious ratsTetsuji Itoh
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
Synapse 64:172-6. 2010..These results support the value of measuring in vivo [(11)C](R)-rolipram binding in brain to assess responses to physiological or pharmacological challenges to the cAMP second messenger system...
Widespread decrease of nicotinic acetylcholine receptors in Parkinson's diseaseMasahiro 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...
Comparison of 18F- and 11C-labeled aryloxyanilide analogs to measure translocator protein in human brain using positron emission tomographyLeah 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....
PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in ratMasao 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...
PET imaging of serotonin transporters with [11C]DASB: test-retest reproducibility using a multilinear reference tissue parametric imaging methodJae Seung Kim
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland, USA
J Nucl Med 47:208-14. 2006....
Pharmacological and genetic characterization of two selective serotonin transporter ligands: 2-[2-(dimethylaminomethylphenylthio)]-5-fluoromethylphenylamine (AFM) and 3-amino-4-[2-(dimethylaminomethyl-phenylthio)]benzonitrile (DASB)Qian Li
Laboratory of Clinical Science, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA
J Pharmacol Exp Ther 308:481-6. 2004..In addition, fenfluramine showed a low capability to compete with [(3)H]AFM. The present results suggest that both AFM and DASB are highly selective SERT ligands potentially suitable for use in human PET studies of SERT...
The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brainFumihiko 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...
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...
Effects of early life stress on [11C]DASB positron emission tomography imaging of serotonin transporters in adolescent peer- and mother-reared rhesus monkeysMasanori Ichise
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, Maryland 20892, USA
J Neurosci 26:4638-43. 2006....
Increased peripheral benzodiazepine receptors in arterial plaque of patients with atherosclerosis: an autoradiographic study with [(3)H]PK 11195Yota Fujimura
Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA
Atherosclerosis 201:108-11. 2008..In conclusion, this study demonstrated that macrophage and inflammatory activity in atherosclerotic plaque can be imaged specifically by the binding of PBR indicating future application of PET imaging for PBR...
Evaluation of 2 scatter correction methods using a striatal phantom for quantitative brain SPECTDouglass C Vines
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892 0135, USA
J Nucl Med Technol 31:157-60. 2003..The first is based on thresholding the energy spectrum (ES), and the second is based on a modification of the transmission-dependent convolution subtraction (TDCS) method...
Molecular imaging of the dopaminergic system and its association with human cognitive functionVanessa L Cropley
Department of Physiology, Behavioural Neuroscience Laboratory, Monash Centre for Brain and Behaviour, Monash University, Victoria, Australia
Biol Psychiatry 59:898-907. 2006....
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 diseaseLisheng 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....
Quantification of nicotinic acetylcholine receptors in human brain using [123I]5-I-A-85380 SPETMasahiro 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...
Pharmacological characterization of 2-methoxy-N-propylnorapomorphine's interactions with D2 and D3 dopamine receptorsMette Skinbjerg
Molecular Neuropharmacology Section, National Institute of Neurological Disorders and Stroke, Bethesda, Maryland 20892 9405, USA
Synapse 63:462-75. 2009..Taken together, our data indicate that the PET tracer, MNPA, is a full and potent agonist at both D(2) and D(3) receptors...
Strategies to improve neuroreceptor parameter estimation by linear regression analysisMasanori Ichise
Molecular Imaging Branch, National Institutes of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
J Cereb Blood Flow Metab 22:1271-81. 2002..For tracers with slow kinetics and low to moderate noise, however, MA2 may provide the lowest bias while maintaining computational ease for pixelwise parameter estimation...
Radioligand development for PET imaging of beta-amyloid (Abeta)--current statusLisheng 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...
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomographyVictor 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...
Effect of scatter correction on the compartmental measurement of striatal and extrastriatal dopamine D2 receptors using [123I]epidepride SPETMasahiro 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...
Changes in human in vivo serotonin and dopamine transporter availabilities during chronic antidepressant administrationAkira Kugaya
Department of Psychiatry, Yale University School of Medicine, New Haven, CT, USA
Neuropsychopharmacology 28:413-20. 2003..This apparent SSRI-induced modulation of the dopamine system may be associated with the side effects of these agents, including sexual dysfunction...
Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjectsMasahiro 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...
Unaltered dopamine transporter availability in adult attention deficit hyperactivity disorderChristopher H van Dyck
Department of Psychiatry, Yale University School of Medicine, Cognitive Disorders Clinic, New Haven, CT 06510, USA
Am J Psychiatry 159:309-12. 2002..The authors examined whether patients with attention deficit hyperactivity disorder (ADHD) have altered striatal dopamine transporter levels, which may explain psychostimulant effects in this disorder...
Age-related decline in dopamine transporters: analysis of striatal subregions, nonlinear effects, and hemispheric asymmetriesChristopher 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...
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imagingXing Fu
Department of Psychiatry, Yale University School of Medicine and VA Connecticut Health Care Service, West Haven, Connecticut 06516, USA
J Med Chem 45:2319-24. 2002..The novel compound (4-fluorophenyl)-(1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl])methanol was particularly promising with high 5-HT2A potency (K(i) = 1.63 nM) and >300-fold selectivity over other 5-HT receptor types...
Synthesis of cyclopentadienyltricarbonyl rhenium phenyltropanes by double ligand transfer: organometallic ligands for the dopamine transporterRichard 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...
Linearized reference tissue parametric imaging methods: application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brainMasanori Ichise
National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892, USA
J Cereb Blood Flow Metab 23:1096-112. 2003..MRTM2 allowed rapid generation of parametric images with the noise reductions consistent with the simulations. Rapid parametric imaging by MRTM2 should be a useful method for human [11C]DASB positron emission tomography studies...
Synthesis, radiolabeling and baboon SPECT imaging of 2beta-carbomethoxy-3beta-(3'-[(123)I]iodophenyl)tropane ([(123)I]YP256) as a serotonin transporter radiotracerFrederic Bois
Yale University, School of Medicine, VA Connecticut HCS 116A2, West Haven, CT 06516, USA
Nucl Med Biol 35:53-9. 2008..Although the ligand displayed high selectivity for 5-HTT over dopamine transporter in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo...
Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: a comparison of the agonist radioligand [11C]MNPA and antagonist [11C]racloprideNicholas Seneca
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Karolinska Hospital, S 17176 Stockholm, Sweden
Synapse 59:260-9. 2006....
Post-mortem human brain autoradiography of the norepinephrine transporter using (S,S)-[18F]FMeNER-D2Magnus 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...
A preliminary PET evaluation of the new dopamine D2 receptor agonist [11C]MNPA in cynomolgus monkeySjoerd J Finnema
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institute, Karolinska University Hospital, S-17176 Stockholm, Sweden
Nucl Med Biol 32:353-60. 2005....
Increased dopamine transporter availability associated with the 9-repeat allele of the SLC6A3 geneChristopher H van Dyck
Department of Psychiatry, Yale University School of Medicine, One Church Street, New Haven, CT 06510, USA
J Nucl Med 46:745-51. 2005..Previous investigations of the effects of the SLC6A3 polymorphism on DAT availability in smaller samples of humans have yielded divergent results...
PET imaging of brain with the beta-amyloid probe, [11C]6-OH-BTA-1, in a transgenic mouse model of Alzheimer's diseaseHiroshi 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)...
Brain serotonin transporter availability predicts treatment response to selective serotonin reuptake inhibitorsAkira Kugaya
Department of Psychiatry, Yale University, New Haven, Connecticut, USA
Biol Psychiatry 56:497-502. 2004..This study used brain imaging to examine the relationship between pretreatment brain SERT availability and transporter occupancy by SSRIs with treatment response in two independent depressed populations...
PET evaluation of novel radiofluorinated reboxetine analogs as norepinephrine transporter probes in the monkey brainMagnus Schou
Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-17176 Stockholm, Sweden
Synapse 53:57-67. 2004....
Central serotonin transporter availability measured with [123I]beta-CIT SPECT in relation to serotonin transporter genotypeChristopher H van Dyck
Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06510, USA
Am J Psychiatry 161:525-31. 2004..In vitro studies of nonneural cells have suggested that the long allele may have higher transcriptional activity than the short allele. However, the relevance of these findings for SERT levels in the brain remains unclear...
Dopamine mediation of positive reinforcing effects of amphetamine in stimulant naïve healthy volunteers: results from a large cohortAnissa Abi-Dargham
Department of Psychiatry, Columbia University, New York, NY, USA
Eur Neuropsychopharmacol 13:459-68. 2003..This study indicates that both a large dopaminergic response and young age during a first encounter with a drug of abuse potential contribute to higher positive reinforcing effects...
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZMRonald M Baldwin
Department of Psychiatry, Yale University and VA CT/HCS, West Haven, CT 06516, USA
Bioorg Med Chem Lett 13:4015-7. 2003..The isomer 5-IBZM had 100-fold lower affinity than IBZM and migrated with similar retention time as the byproduct formed during electrophilic iodination of BZM...
Specific in vivo binding to the norepinephrine transporter demonstrated with the PET radioligand, (S,S)-[11C]MeNERMagnus 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...
Chemical fate of the nicotinic acetylcholinergic radiotracer [123I]5-IA-85380 in baboon brain and plasmaRonald M Baldwin
Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06510, USA
Nucl Med Biol 33:549-54. 2006....
