Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2 (424 views)
Psychopharmacology (ISSN: 0033-3158), 2006 Sep; 188(1): 119-127.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.625, 5-year impact factor: 4.141
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33747616636&partnerID=40&md5=68edb0abcce87719b5e67f71a2a59683
Keywords: S)-[18f]fmener-D2, Atomoxetine, Nonhuman Primate Brain, Norepinephrine Transporter Occupancy, Drug Metabolite, Fluorodeoxyglucose F 18, N Noratomoxetine, Noradrenalin Transporter, Radiopharmaceutical Agent, Unclassified Drug, Animal Experiment, Article, Caudate Nucleus, Cingulate Gyrus, Controlled Study, Drug Absorption, Drug Blood Level, Drug Uptake, In Vivo Study, Locus Ceruleus, Mesencephalon, Monkey, Positron Emission Tomography, Priority Journal, Radioactivity, Thalamus, Adrenergic Uptake Inhibitors, Binding, Competitive, Dose-Response Relationship, Fluorine Radioisotopes, Macaca Fascicularis, Morpholines, Norepinephrine Plasma Membrane Transport Proteins, Positron-Emission Tomography, Propylamines, Protein Binding, S)-[18f] Fmener-D2,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Karolinska Institutet, Karolinska Hospital, S-17176 Stockholm, Sweden
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, United States
Biostructure and Bioimaging Institute, National Research Council, Napoli, Italy
Lilly Research Laboratories, Eli Lilly and Co., Indianapolis, IN, United States
References:
Andree, B., Seneca, N., Schou, M., Mozley, P.D., Potter, W.Z., Farde, L., Gulyas, B., Halldin, C., Regional central norepinephrine transporter occupancy induced by reboxetine determined in man using [11C]MeNER (2004) Neuroimage, 22 (2 SUPPL.), p. 3
Aston-Jones, G., Shipley, M.T., Chouvet, G., Ennis, M., Van Bockstaele, E., Pieribone, V., Shiekhattar, R., Astier, B., Afferent regulation of locus coeruleus neurons: Anatomy, physiology and pharmacology (1991) Prog Brain Res, 88, pp. 47-75
Bobb, A.J., Addington, A.M., Sidransky, E., Gornick, M.C., Lerch, J.P., Greenstein, D.K., Clasen, L.S., Rapoport, J.L., Support for association between ADHD and two candidate genes: NET1 and DRD1 (2005) Am J Med Genet B Neuropsychiatr Genet, 134, pp. 67-72
Bymaster, F.P., Katner, J.S., Nelson, D.L., Hemrick-Luecke, S.K., Threlkeld, P.G., Heiligenstein, J.H., Morin, S.M., Perry, K.W., Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: A potential mechanism for efficacy in attention deficit/hyperactivity disorder (2002) Neuropsychopharmacology, 27, pp. 699-711
Carson, R.E., Wu, Y., Lang, L., Ma, Y., Der, M.G., Herscovitch, P., Eckelman, W.C., Brain uptake of the acid metabolites of F-18-labeled WAY 100635 analogs (2003) J Cereb Blood Flow Metab, 23, pp. 249-260
Charnay, Y., Leger, L., Vallet, P.G., Hof, P.R., Jouvet, M., Bouras, C., [3H]Nisoxetine binding sites in the cat brain: An autoradiographic study (1995) Neuroscience, 69, pp. 259-270
Ding, Y.S., Lin, K.S., Logan, J., Benveniste, H., Carter, P., Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3-Cl-[11C]methylreboxetine and [18F]fluororeboxetine), (R)-[11C] nisoxetine, [11C]oxaprotiline and [11C]lortalamine (2005) J Neurochem, 94, pp. 337-351
Donnan, G.A., Kaczmarczyk, S.J., Paxinos, G., Chilco, P.J., Kalnins, R.M., Woodhouse, D.G., Mendelsohn, F.A., Distribution of catecholamine uptake sites in human brain as determined by quantitative [3H] mazindol autoradiography (1991) J Comp Neurol, 304, pp. 419-434
Gehlert, D.R., Gackenheimer, S.L., Robertson, D.W., Localization of rat brain binding sites for [3H]tomoxetine, an enantiomerically pure ligand for norepinephrine reuptake sites (1993) Neurosci Lett, 157, pp. 203-206
Ghose, S., Fujita, M., Morrison, P., Uhl, G., Murphy, D.L., Mozley, P.D., Schou, M., Innis, R., Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters (2005) Synapse, 56, pp. 100-104
Gross-Isseroff, R., Israeli, M., Biegon, A., Autoradiographic analysis of [3H]desmethylimipramine binding in the human brain postmortem (1988) Brain Res, 456, pp. 120-126
Haller, J., Bakos, N., Rodriguiz, R.M., Caron, M.G., Wetsel, W.C., Liposits, Z., Behavioral responses to social stress in noradrenaline transporter knockout mice: Effects on social behavior and depression (2002) Brain Res Bull, 58, pp. 279-284
Haughey, H.M., Kaiser, A.L., Johnson, T.E., Bennett, B., Sikela, J.M., Zahniser, N.R., Norepinephrine transporter: A candidate gene for initial ethanol sensitivity in inbred long-sleep and short-sleep mice (2005) Alcohol Clin Exp Res, 29, pp. 1759-1768
Hargreaves, R., Imaging substance P receptors (NK1) in the living human brain using positron emission tomography (2002) J Clin Psychiatry, 63 (11 SUPPL.), pp. 18-24
Ichise, M., Liow, J.S., Lu, J.Q., Takano, A., Model, K., Toyama, H., Suhara, T., Carson, R.E., Linearized reference tissue parametric imaging methods: Application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain (2003) J Cereb Blood Flow Metab, 23, pp. 1096-1112
Iversen, L., Neurotransmitter transporters and their impact on the development of psychopharmacology (2006) Br J Pharmacol, 147 (1 SUPPL.), pp. S82-S88
Karlsson, P., Farde, L., Halldin, C., Swahn, C.G., Sedvall, G., Foged, C., Hansen, K.T., Skrumsager, B., PET examination of [11C] NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor (1993) Psychopharmacology, 113, pp. 149-156. , Berl
Klimek, V., Stockmeier, C., Overholser, J., Meltzer, H.Y., Kalka, S., Dilley, G., Ordway, G.A., Reduced levels of norepinephrine transporters in the locus coeruleus in major depression (1997) J Neurosci, 17, pp. 8451-8458
Lammertsma, A.A., Hume, S.P., Simplified reference tissue model for PET receptor studies (1996) Neuroimage, 4, pp. 153-158
Li, W., Knowlton, D., Van Winkle, D.M., Habecker, B.A., Infarction alters both the distribution and noradrenergic properties of cardiac sympathetic neurons (2004) Am J Physiol Heart Circ Physiol, 286, pp. H2229-H2236
Logan, J., Fowler, J.S., Volkow, N.D., Wang, G.J., Ding, Y.S., Alexoff, D.L., Distribution volume ratios without blood sampling from graphical analysis of PET data (1996) J Cereb Blood Flow Metab, 16, pp. 834-840
Michelson, D., Faries, D., Wernicke, J., Kelsey, D., Kendrick, K., Sallee, F.R., Spencer, T., Atomoxetine in the treatment of children and adolescents with attention-deficit/hyperactivity disorder: A randomized, placebo-controlled, dose-response study (2001) Pediatrics, 108, pp. E83
Roland, P.E., Zilles, K., Brain atlases-a new research tool (1994) Trends Neurosci, 17, pp. 458-467
Schou, M., Halldin, C., Sovago, J., Pike, V.W., Gulyas, B., Mozley, P.D., Johnson, D.P., Farde, L., Specific in vivo binding to the norepinephrine transporter demonstrated with the PET radioligand, (S,S)-[11C]MeNER (2003) Nucl Med Biol, 30, pp. 707-714
Seneca, N., Andree, B., Sjoholm, N., Schou, M., Pauli, S., Mozley, P.D., Stubbs, J.B., Halldin, C., Whole-body biodistribution, radiation dosimetry estimates for the PET norepinephrine transporter probe (S,S)-[18F]FMeNER-D2 in non-human primates (2005) Nucl Med Commun, 26, pp. 695-700
Spencer, T., Biederman, J., Wilens, T., Prince, J., Hatch, M., Jones, J., Harding, M., Seidman, L., Effectiveness and tolerability of tomoxetine in adults with attention deficit hyperactivity disorder (1998) Am J Psychiatry, 155, pp. 693-695
Stahl, S.M., Neurotransmission of cognition, part 2. Selective NRIs are smart drugs: Exploiting regionally selective actions on both dopamine and norepinephrine to enhance cognition (2003) J Clin Psychiatry, 64, pp. 110-111
Tejani-Butt, S.M., [3H]nisoxetine: A radioligand for quantitation of norepinephrine uptake sites by autoradiography or by homogenate binding (1992) J Pharmacol Exp Ther, 260, pp. 427-436
Tipre, D., Zoghbi, S., Liow, J.S., Green, M., Seidel, J., Ichise, M., Innis, R.B., Pike, V.W., PET imaging of brain 5-HT1A receptors in rat in vivo with [18F]FCWAYand improvement by successful inhibition of radioligand defluorination with miconazole (2006) J Nucl Med, 47, pp. 1-9
Xu, F., Gainetdinov, R.R., Wetsel, W.C., Jones, S.R., Bohn, L.M., Miller, G.W., Wang, Y.M., Caron, M.G., Mice lacking the norepinephrine transporter are supersensitive to psychostimulants (2000) Nat Neurosci, 3, pp. 465-471
Wienhard, K., Dahlbom, M., Eriksson, L., Michel, C., Bruckbauer, T., Pietrzyk, U., Heiss, W.D., The ECAT EXACT HR: Performance of a new high resolution positron scanner (1994) J Comput Assist Tomogr, 18, pp. 110-118
Wilson, A.A., Johnson, D.P., Mozley, D., Hussey, D., Ginovart, N., Nobrega, J., Garcia, A., Houle, S., Synthesis and in vivo evaluation of novel radiotracers for the in vivo imaging of the norepinephrine transporter (2003) Nucl Med Biol, 30, pp. 85-92
Wong, D.T., Threlkeld, P.G., Best, K.L., Bymaster, F.P., A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain (1982) J Pharmacol Exp Ther, 222, pp. 61-65
Wong, D., Kuwabara, H., Mozley, P.D., Dannals, R., Kumar, A., Ye, W., Brasic, J., Gjedde, A., Characterization of dose dependent norepinephrine transporter blockade by atomoxetine in human brain using [11C]MeNER PET (2005) J Cereb Blood Flow Metab, 25, pp. S599
Bobb, A. J., Addington, A. M., Sidransky, E., Gornick, M. C., Lerch, J. P., Greenstein, D. K., Clasen, L. S., Rapoport, J. L., Support for association between ADHD and two candidate genes: NET1 and DRD1 (2005) Am J Med Genet B Neuropsychiatr Genet, 134, pp. 67-72
Bymaster, F. P., Katner, J. S., Nelson, D. L., Hemrick-Luecke, S. K., Threlkeld, P. G., Heiligenstein, J. H., Morin, S. M., Perry, K. W., Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: A potential mechanism for efficacy in attention deficit/hyperactivity disorder (2002) Neuropsychopharmacology, 27, pp. 699-711
Carson, R. E., Wu, Y., Lang, L., Ma, Y., Der, M. G., Herscovitch, P., Eckelman, W. C., Brain uptake of the acid metabolites of F-18-labeled WAY 100635 analogs (2003) J Cereb Blood Flow Metab, 23, pp. 249-260
Ding, Y. S., Lin, K. S., Logan, J., Benveniste, H., Carter, P., Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S, S) and (R, R) enantiomers of reboxetine analogs ([11C] methylreboxetine, 3-Cl- [11C] methylreboxetine and [18F] fluororeboxetine), (R) - [11C] nisoxetine, [11C] oxaprotiline and [11C] lortalamine (2005) J Neurochem, 94, pp. 337-351
Donnan, G. A., Kaczmarczyk, S. J., Paxinos, G., Chilco, P. J., Kalnins, R. M., Woodhouse, D. G., Mendelsohn, F. A., Distribution of catecholamine uptake sites in human brain as determined by quantitative [3H] mazindol autoradiography (1991) J Comp Neurol, 304, pp. 419-434
Gehlert, D. R., Gackenheimer, S. L., Robertson, D. W., Localization of rat brain binding sites for [3H] tomoxetine, an enantiomerically pure ligand for norepinephrine reuptake sites (1993) Neurosci Lett, 157, pp. 203-206
Haughey, H. M., Kaiser, A. L., Johnson, T. E., Bennett, B., Sikela, J. M., Zahniser, N. R., Norepinephrine transporter: A candidate gene for initial ethanol sensitivity in inbred long-sleep and short-sleep mice (2005) Alcohol Clin Exp Res, 29, pp. 1759-1768
Lammertsma, A. A., Hume, S. P., Simplified reference tissue model for PET receptor studies (1996) Neuroimage, 4, pp. 153-158
Roland, P. E., Zilles, K., Brain atlases-a new research tool (1994) Trends Neurosci, 17, pp. 458-467
Stahl, S. M., Neurotransmission of cognition, part 2. Selective NRIs are smart drugs: Exploiting regionally selective actions on both dopamine and norepinephrine to enhance cognition (2003) J Clin Psychiatry, 64, pp. 110-111
Tejani-Butt, S. M., [3H] nisoxetine: A radioligand for quantitation of norepinephrine uptake sites by autoradiography or by homogenate binding (1992) J Pharmacol Exp Ther, 260, pp. 427-436
Wilson, A. A., Johnson, D. P., Mozley, D., Hussey, D., Ginovart, N., Nobrega, J., Garcia, A., Houle, S., Synthesis and in vivo evaluation of novel radiotracers for the in vivo imaging of the norepinephrine transporter (2003) Nucl Med Biol, 30, pp. 85-92
Wong, D. T., Threlkeld, P. G., Best, K. L., Bymaster, F. P., A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain (1982) J Pharmacol Exp Ther, 222, pp. 61-65
Psychopharmacology (ISSN: 0033-3158), 2006 Sep; 188(1): 119-127.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 3.625, 5-year impact factor: 4.141
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33747616636&partnerID=40&md5=68edb0abcce87719b5e67f71a2a59683
Keywords: S)-[18f]fmener-D2, Atomoxetine, Nonhuman Primate Brain, Norepinephrine Transporter Occupancy, Drug Metabolite, Fluorodeoxyglucose F 18, N Noratomoxetine, Noradrenalin Transporter, Radiopharmaceutical Agent, Unclassified Drug, Animal Experiment, Article, Caudate Nucleus, Cingulate Gyrus, Controlled Study, Drug Absorption, Drug Blood Level, Drug Uptake, In Vivo Study, Locus Ceruleus, Mesencephalon, Monkey, Positron Emission Tomography, Priority Journal, Radioactivity, Thalamus, Adrenergic Uptake Inhibitors, Binding, Competitive, Dose-Response Relationship, Fluorine Radioisotopes, Macaca Fascicularis, Morpholines, Norepinephrine Plasma Membrane Transport Proteins, Positron-Emission Tomography, Propylamines, Protein Binding, S)-[18f] Fmener-D2,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Karolinska Institutet, Karolinska Hospital, S-17176 Stockholm, Sweden
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD, United States
Biostructure and Bioimaging Institute, National Research Council, Napoli, Italy
Lilly Research Laboratories, Eli Lilly and Co., Indianapolis, IN, United States
References:
Andree, B., Seneca, N., Schou, M., Mozley, P.D., Potter, W.Z., Farde, L., Gulyas, B., Halldin, C., Regional central norepinephrine transporter occupancy induced by reboxetine determined in man using [11C]MeNER (2004) Neuroimage, 22 (2 SUPPL.), p. 3
Aston-Jones, G., Shipley, M.T., Chouvet, G., Ennis, M., Van Bockstaele, E., Pieribone, V., Shiekhattar, R., Astier, B., Afferent regulation of locus coeruleus neurons: Anatomy, physiology and pharmacology (1991) Prog Brain Res, 88, pp. 47-75
Bobb, A.J., Addington, A.M., Sidransky, E., Gornick, M.C., Lerch, J.P., Greenstein, D.K., Clasen, L.S., Rapoport, J.L., Support for association between ADHD and two candidate genes: NET1 and DRD1 (2005) Am J Med Genet B Neuropsychiatr Genet, 134, pp. 67-72
Bymaster, F.P., Katner, J.S., Nelson, D.L., Hemrick-Luecke, S.K., Threlkeld, P.G., Heiligenstein, J.H., Morin, S.M., Perry, K.W., Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: A potential mechanism for efficacy in attention deficit/hyperactivity disorder (2002) Neuropsychopharmacology, 27, pp. 699-711
Carson, R.E., Wu, Y., Lang, L., Ma, Y., Der, M.G., Herscovitch, P., Eckelman, W.C., Brain uptake of the acid metabolites of F-18-labeled WAY 100635 analogs (2003) J Cereb Blood Flow Metab, 23, pp. 249-260
Charnay, Y., Leger, L., Vallet, P.G., Hof, P.R., Jouvet, M., Bouras, C., [3H]Nisoxetine binding sites in the cat brain: An autoradiographic study (1995) Neuroscience, 69, pp. 259-270
Ding, Y.S., Lin, K.S., Logan, J., Benveniste, H., Carter, P., Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3-Cl-[11C]methylreboxetine and [18F]fluororeboxetine), (R)-[11C] nisoxetine, [11C]oxaprotiline and [11C]lortalamine (2005) J Neurochem, 94, pp. 337-351
Donnan, G.A., Kaczmarczyk, S.J., Paxinos, G., Chilco, P.J., Kalnins, R.M., Woodhouse, D.G., Mendelsohn, F.A., Distribution of catecholamine uptake sites in human brain as determined by quantitative [3H] mazindol autoradiography (1991) J Comp Neurol, 304, pp. 419-434
Gehlert, D.R., Gackenheimer, S.L., Robertson, D.W., Localization of rat brain binding sites for [3H]tomoxetine, an enantiomerically pure ligand for norepinephrine reuptake sites (1993) Neurosci Lett, 157, pp. 203-206
Ghose, S., Fujita, M., Morrison, P., Uhl, G., Murphy, D.L., Mozley, P.D., Schou, M., Innis, R., Specific in vitro binding of (S,S)-[3H]MeNER to norepinephrine transporters (2005) Synapse, 56, pp. 100-104
Gross-Isseroff, R., Israeli, M., Biegon, A., Autoradiographic analysis of [3H]desmethylimipramine binding in the human brain postmortem (1988) Brain Res, 456, pp. 120-126
Haller, J., Bakos, N., Rodriguiz, R.M., Caron, M.G., Wetsel, W.C., Liposits, Z., Behavioral responses to social stress in noradrenaline transporter knockout mice: Effects on social behavior and depression (2002) Brain Res Bull, 58, pp. 279-284
Haughey, H.M., Kaiser, A.L., Johnson, T.E., Bennett, B., Sikela, J.M., Zahniser, N.R., Norepinephrine transporter: A candidate gene for initial ethanol sensitivity in inbred long-sleep and short-sleep mice (2005) Alcohol Clin Exp Res, 29, pp. 1759-1768
Hargreaves, R., Imaging substance P receptors (NK1) in the living human brain using positron emission tomography (2002) J Clin Psychiatry, 63 (11 SUPPL.), pp. 18-24
Ichise, M., Liow, J.S., Lu, J.Q., Takano, A., Model, K., Toyama, H., Suhara, T., Carson, R.E., Linearized reference tissue parametric imaging methods: Application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain (2003) J Cereb Blood Flow Metab, 23, pp. 1096-1112
Iversen, L., Neurotransmitter transporters and their impact on the development of psychopharmacology (2006) Br J Pharmacol, 147 (1 SUPPL.), pp. S82-S88
Karlsson, P., Farde, L., Halldin, C., Swahn, C.G., Sedvall, G., Foged, C., Hansen, K.T., Skrumsager, B., PET examination of [11C] NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor (1993) Psychopharmacology, 113, pp. 149-156. , Berl
Klimek, V., Stockmeier, C., Overholser, J., Meltzer, H.Y., Kalka, S., Dilley, G., Ordway, G.A., Reduced levels of norepinephrine transporters in the locus coeruleus in major depression (1997) J Neurosci, 17, pp. 8451-8458
Lammertsma, A.A., Hume, S.P., Simplified reference tissue model for PET receptor studies (1996) Neuroimage, 4, pp. 153-158
Li, W., Knowlton, D., Van Winkle, D.M., Habecker, B.A., Infarction alters both the distribution and noradrenergic properties of cardiac sympathetic neurons (2004) Am J Physiol Heart Circ Physiol, 286, pp. H2229-H2236
Logan, J., Fowler, J.S., Volkow, N.D., Wang, G.J., Ding, Y.S., Alexoff, D.L., Distribution volume ratios without blood sampling from graphical analysis of PET data (1996) J Cereb Blood Flow Metab, 16, pp. 834-840
Michelson, D., Faries, D., Wernicke, J., Kelsey, D., Kendrick, K., Sallee, F.R., Spencer, T., Atomoxetine in the treatment of children and adolescents with attention-deficit/hyperactivity disorder: A randomized, placebo-controlled, dose-response study (2001) Pediatrics, 108, pp. E83
Roland, P.E., Zilles, K., Brain atlases-a new research tool (1994) Trends Neurosci, 17, pp. 458-467
Schou, M., Halldin, C., Sovago, J., Pike, V.W., Gulyas, B., Mozley, P.D., Johnson, D.P., Farde, L., Specific in vivo binding to the norepinephrine transporter demonstrated with the PET radioligand, (S,S)-[11C]MeNER (2003) Nucl Med Biol, 30, pp. 707-714
Seneca, N., Andree, B., Sjoholm, N., Schou, M., Pauli, S., Mozley, P.D., Stubbs, J.B., Halldin, C., Whole-body biodistribution, radiation dosimetry estimates for the PET norepinephrine transporter probe (S,S)-[18F]FMeNER-D2 in non-human primates (2005) Nucl Med Commun, 26, pp. 695-700
Spencer, T., Biederman, J., Wilens, T., Prince, J., Hatch, M., Jones, J., Harding, M., Seidman, L., Effectiveness and tolerability of tomoxetine in adults with attention deficit hyperactivity disorder (1998) Am J Psychiatry, 155, pp. 693-695
Stahl, S.M., Neurotransmission of cognition, part 2. Selective NRIs are smart drugs: Exploiting regionally selective actions on both dopamine and norepinephrine to enhance cognition (2003) J Clin Psychiatry, 64, pp. 110-111
Tejani-Butt, S.M., [3H]nisoxetine: A radioligand for quantitation of norepinephrine uptake sites by autoradiography or by homogenate binding (1992) J Pharmacol Exp Ther, 260, pp. 427-436
Tipre, D., Zoghbi, S., Liow, J.S., Green, M., Seidel, J., Ichise, M., Innis, R.B., Pike, V.W., PET imaging of brain 5-HT1A receptors in rat in vivo with [18F]FCWAYand improvement by successful inhibition of radioligand defluorination with miconazole (2006) J Nucl Med, 47, pp. 1-9
Xu, F., Gainetdinov, R.R., Wetsel, W.C., Jones, S.R., Bohn, L.M., Miller, G.W., Wang, Y.M., Caron, M.G., Mice lacking the norepinephrine transporter are supersensitive to psychostimulants (2000) Nat Neurosci, 3, pp. 465-471
Wienhard, K., Dahlbom, M., Eriksson, L., Michel, C., Bruckbauer, T., Pietrzyk, U., Heiss, W.D., The ECAT EXACT HR: Performance of a new high resolution positron scanner (1994) J Comput Assist Tomogr, 18, pp. 110-118
Wilson, A.A., Johnson, D.P., Mozley, D., Hussey, D., Ginovart, N., Nobrega, J., Garcia, A., Houle, S., Synthesis and in vivo evaluation of novel radiotracers for the in vivo imaging of the norepinephrine transporter (2003) Nucl Med Biol, 30, pp. 85-92
Wong, D.T., Threlkeld, P.G., Best, K.L., Bymaster, F.P., A new inhibitor of norepinephrine uptake devoid of affinity for receptors in rat brain (1982) J Pharmacol Exp Ther, 222, pp. 61-65
Wong, D., Kuwabara, H., Mozley, P.D., Dannals, R., Kumar, A., Ye, W., Brasic, J., Gjedde, A., Characterization of dose dependent norepinephrine transporter blockade by atomoxetine in human brain using [11C]MeNER PET (2005) J Cereb Blood Flow Metab, 25, pp. S599
Bobb, A. J., Addington, A. M., Sidransky, E., Gornick, M. C., Lerch, J. P., Greenstein, D. K., Clasen, L. S., Rapoport, J. L., Support for association between ADHD and two candidate genes: NET1 and DRD1 (2005) Am J Med Genet B Neuropsychiatr Genet, 134, pp. 67-72
Bymaster, F. P., Katner, J. S., Nelson, D. L., Hemrick-Luecke, S. K., Threlkeld, P. G., Heiligenstein, J. H., Morin, S. M., Perry, K. W., Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: A potential mechanism for efficacy in attention deficit/hyperactivity disorder (2002) Neuropsychopharmacology, 27, pp. 699-711
Carson, R. E., Wu, Y., Lang, L., Ma, Y., Der, M. G., Herscovitch, P., Eckelman, W. C., Brain uptake of the acid metabolites of F-18-labeled WAY 100635 analogs (2003) J Cereb Blood Flow Metab, 23, pp. 249-260
Ding, Y. S., Lin, K. S., Logan, J., Benveniste, H., Carter, P., Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S, S) and (R, R) enantiomers of reboxetine analogs ([11C] methylreboxetine, 3-Cl- [11C] methylreboxetine and [18F] fluororeboxetine), (R) - [11C] nisoxetine, [11C] oxaprotiline and [11C] lortalamine (2005) J Neurochem, 94, pp. 337-351
Donnan, G. A., Kaczmarczyk, S. J., Paxinos, G., Chilco, P. J., Kalnins, R. M., Woodhouse, D. G., Mendelsohn, F. A., Distribution of catecholamine uptake sites in human brain as determined by quantitative [3H] mazindol autoradiography (1991) J Comp Neurol, 304, pp. 419-434
Gehlert, D. R., Gackenheimer, S. L., Robertson, D. W., Localization of rat brain binding sites for [3H] tomoxetine, an enantiomerically pure ligand for norepinephrine reuptake sites (1993) Neurosci Lett, 157, pp. 203-206
Haughey, H. M., Kaiser, A. L., Johnson, T. E., Bennett, B., Sikela, J. M., Zahniser, N. R., Norepinephrine transporter: A candidate gene for initial ethanol sensitivity in inbred long-sleep and short-sleep mice (2005) Alcohol Clin Exp Res, 29, pp. 1759-1768
Lammertsma, A. A., Hume, S. P., Simplified reference tissue model for PET receptor studies (1996) Neuroimage, 4, pp. 153-158
Roland, P. E., Zilles, K., Brain atlases-a new research tool (1994) Trends Neurosci, 17, pp. 458-467
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Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2
Rationale: Atomoxetine is a potent and selective norepinephrine transporter (NET) reuptake inhibitor acting as a nonstimulant for the treatment of attention-deficit/hyperactivity disorder (ADHD). Previous positron emission tomography (PET) studies had failed to demonstrate the feasibility of measuring a dose-dependent and saturable NET occupancy in human brain using [ 11C]MeNER. Objectives: To determine if atomoxetine occupies NET in a dose-dependent fashion using (S,S)-[18F]FMeNER-D2 in nonhuman primate brain. Methods: A total of eight PET measurements were performed in two cynomolgus monkeys. Each monkey was examined four times with PET: under baseline conditions and after steady-state infusion with 0.03, 0.06, or 0.12 mg/kg/h of atomoxetine. A prolonged intravenous (i.v.) infusion design was developed rather than an i.v. bolus to better mimic an oral absorption profile and to reach plasma steady state. Results: During baseline conditions, (S,S)-[18F]FMeNER-D2 uptake was highest in the locus coeruleus, thalamus, mesencephalon, and the cingulate gyrus, whereas the radioactivity in the caudate was low. Peak equilibrium measurements were achieved using (S,S)-[18F]FMeNER-D2 in contrast to the previously reported data for [11C]MeNER. After administration of atomoxetine, a dose-dependent occupancy from 38 to 82% was observed for various brain regions known to contain high densities of NET. Conclusions: This is the first in vivo PET study to successfully demonstrate the ability to measure a dose-dependent change in NET occupancy in brain using (S,S)-[ 18F]FMeNER-D2. Furthermore, an asymptotic relationship between N-desmethylatomoxetine plasma concentration and NET occupancy was established. In total, these data encourage further PET studies using (S,S)-[18F]FMeNER-D2 in humans. © Springer-Verlag 2006.
Rationale: Atomoxetine is a potent and selective norepinephrine transporter (NET) reuptake inhibitor acting as a nonstimulant for the treatment of attention-deficit/hyperactivity disorder (ADHD). Previous positron emission tomography (PET) studies had failed to demonstrate the feasibility of measuring a dose-dependent and saturable NET occupancy in human brain using [ 11C]MeNER. Objectives: To determine if atomoxetine occupies NET in a dose-dependent fashion using (S,S)-[18F]FMeNER-D2 in nonhuman primate brain. Methods: A total of eight PET measurements were performed in two cynomolgus monkeys. Each monkey was examined four times with PET: under baseline conditions and after steady-state infusion with 0.03, 0.06, or 0.12 mg/kg/h of atomoxetine. A prolonged intravenous (i.v.) infusion design was developed rather than an i.v. bolus to better mimic an oral absorption profile and to reach plasma steady state. Results: During baseline conditions, (S,S)-[18F]FMeNER-D2 uptake was highest in the locus coeruleus, thalamus, mesencephalon, and the cingulate gyrus, whereas the radioactivity in the caudate was low. Peak equilibrium measurements were achieved using (S,S)-[18F]FMeNER-D2 in contrast to the previously reported data for [11C]MeNER. After administration of atomoxetine, a dose-dependent occupancy from 38 to 82% was observed for various brain regions known to contain high densities of NET. Conclusions: This is the first in vivo PET study to successfully demonstrate the ability to measure a dose-dependent change in NET occupancy in brain using (S,S)-[ 18F]FMeNER-D2. Furthermore, an asymptotic relationship between N-desmethylatomoxetine plasma concentration and NET occupancy was established. In total, these data encourage further PET studies using (S,S)-[18F]FMeNER-D2 in humans. © Springer-Verlag 2006.
Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2
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Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2
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Sasaki T, Ito H, Kimura Y, Arakawa R, Takano H, Seki C, Kodaka F, Fujie S, Takahata K, Nogami T, Suzuki M, Fujiwara H, Takahashi H, Nakao R, Fukumura T, Varrone A, Halldin C, Nishikawa T, Suhara T
* Quantification of dopamine transporter in human brain using PET with 18F-FE-PE2I (492 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2012 Jul; 53(7): 1065-1073.
Impact Factor: 5.774
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Takano A, Gulyas B, Varrone A, Maguire RP, Halldin C
* Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D (372 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Sep; 36(8): 1308-1314.
Impact Factor: 4.531
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Takano A, Halldin C, Varrone A, Karlsson P, Sjoholm N, Stubbs JB, Schou M, Airaksinen AJ, Tauscher J, Gulyas B
* Biodistribution and radiation dosimetry of the norepinephrine transporter radioligand (S, S)-[18F]FMeNER-D2: A human whole-body PET study (310 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Mar; 35(3): 630-636.
Impact Factor: 4.532
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Takano A, Gulyas B, Varrone A, Karlsson P, Schou M, Airaksinen AJ, Vandenhende F, Tauscher J, Halldin C
* Imaging the norepinephrine transporter with positron emission tomography: Initial human studies with (S, S)-[18F]FMeNER-D2 (306 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Jan; 35(1): 153-157.
Impact Factor: 4.532
View Export to BibTeX Export to EndNote
* Quantification of dopamine transporter in human brain using PET with 18F-FE-PE2I (492 views)
J Nucl Med (ISSN: 0161-5505, 1535-5667, 1535-5667electronic), 2012 Jul; 53(7): 1065-1073.
Impact Factor: 5.774
View Export to BibTeX Export to EndNote
Takano A, Gulyas B, Varrone A, Maguire RP, Halldin C
* Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D (372 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Sep; 36(8): 1308-1314.
Impact Factor: 4.531
View Export to BibTeX Export to EndNote
Takano A, Halldin C, Varrone A, Karlsson P, Sjoholm N, Stubbs JB, Schou M, Airaksinen AJ, Tauscher J, Gulyas B
* Biodistribution and radiation dosimetry of the norepinephrine transporter radioligand (S, S)-[18F]FMeNER-D2: A human whole-body PET study (310 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Mar; 35(3): 630-636.
Impact Factor: 4.532
View Export to BibTeX Export to EndNote
Takano A, Gulyas B, Varrone A, Karlsson P, Schou M, Airaksinen AJ, Vandenhende F, Tauscher J, Halldin C
* Imaging the norepinephrine transporter with positron emission tomography: Initial human studies with (S, S)-[18F]FMeNER-D2 (306 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Jan; 35(1): 153-157.
Impact Factor: 4.532
View Export to BibTeX Export to EndNote
4 Records (4 excluding Abstracts).
Total impact factor: 19.369 (19.369 excluding Abstracts).
Total 5 year impact factor: 19.916 (19.916 excluding Abstracts).
Total impact factor: 19.369 (19.369 excluding Abstracts).
Total 5 year impact factor: 19.916 (19.916 excluding Abstracts).
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