Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2 (639 views)
Psychopharmacology (ISSN: 0033-3158), 2006 Sep; 188(1): 119-127.
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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:
Not available.
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:
Not available.
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 (721 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 (464 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 (582 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 (546 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 (721 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 (464 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 (582 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 (546 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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