Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D (431 views)
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Sep; 36(8): 1308-1314.
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Paper type: Journal Article,
Impact factor: 4.531, 5-year impact factor: 4.264
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-70349257536&partnerID=40&md5=331ad96015192a19acc4d99fb9c73842
Keywords: Atomoxetine, Norepinephrine Transporter Occupancy, 2 [a (2 Fluoro [2h2] Methoxyphenoxy)benzyl]morpholine F 18, Drug Metabolite, Glucuronidated Atomoxetine, Hydroxylated Atomoxetine, N Noratomoxetine, Noradrenalin Transporter, Radioligand, Radiopharmaceutical Agent, Unclassified Drug, 2 (alpha (2 Fluoromethoxyphenoxy)benzyl)morpholine, 2-(alpha-(2-Fluoromethoxyphenoxy)benzyl)morpholine, Diagnostic Agent, Inhalation Anesthetic Agent, Morpholine Derivative, Propylamine, Animal Experiment, Animal Tissue, Article, Brain Stem, Cingulate Gyrus, Drug Blood Level, Drug Brain Level, Drug Infusion, Drug Protein Binding, Female, Molecular Imaging, Nonhuman, Nuclear Magnetic Resonance Imaging, Positron Emission Tomography, Rhesus Monkey, Steady State, Thalamus, Dose Response, Macaca, Radioactivity, Scintiscanning, Tissue Distribution, Dose-Response Relationship, Macaca Mulatta, Norepinephrine Plasma Membrane Transport Proteins, Positron-Emission Tomography, 2 [a (2 Fluoro [2h2] Methoxyphenoxy) Benzyl] Morpholine F 18, 2 (alpha (2 Fluoromethoxyphenoxy) Benzyl) Morpholine, 2-(alpha-(2-Fluoromethoxyphenoxy) Benzyl) Morpholine,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm S-171 76, Sweden
Pfizer Global Research and Development, New London, CT, United States
Novartis Institutes for BioMedical Research, Basel, Switzerland
References:
Not available.
Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2009 Sep; 36(8): 1308-1314.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 4.531, 5-year impact factor: 4.264
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-70349257536&partnerID=40&md5=331ad96015192a19acc4d99fb9c73842
Keywords: Atomoxetine, Norepinephrine Transporter Occupancy, 2 [a (2 Fluoro [2h2] Methoxyphenoxy)benzyl]morpholine F 18, Drug Metabolite, Glucuronidated Atomoxetine, Hydroxylated Atomoxetine, N Noratomoxetine, Noradrenalin Transporter, Radioligand, Radiopharmaceutical Agent, Unclassified Drug, 2 (alpha (2 Fluoromethoxyphenoxy)benzyl)morpholine, 2-(alpha-(2-Fluoromethoxyphenoxy)benzyl)morpholine, Diagnostic Agent, Inhalation Anesthetic Agent, Morpholine Derivative, Propylamine, Animal Experiment, Animal Tissue, Article, Brain Stem, Cingulate Gyrus, Drug Blood Level, Drug Brain Level, Drug Infusion, Drug Protein Binding, Female, Molecular Imaging, Nonhuman, Nuclear Magnetic Resonance Imaging, Positron Emission Tomography, Rhesus Monkey, Steady State, Thalamus, Dose Response, Macaca, Radioactivity, Scintiscanning, Tissue Distribution, Dose-Response Relationship, Macaca Mulatta, Norepinephrine Plasma Membrane Transport Proteins, Positron-Emission Tomography, 2 [a (2 Fluoro [2h2] Methoxyphenoxy) Benzyl] Morpholine F 18, 2 (alpha (2 Fluoromethoxyphenoxy) Benzyl) Morpholine, 2-(alpha-(2-Fluoromethoxyphenoxy) Benzyl) Morpholine,
Affiliations:
*** IBB - CNR ***
Department of Clinical Neuroscience, Psychiatry Section, Karolinska Institutet, Stockholm S-171 76, Sweden
Pfizer Global Research and Development, New London, CT, United States
Novartis Institutes for BioMedical Research, Basel, Switzerland
References:
Not available.
Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D
Purpose: In a previous PET study on norepinephrine transporter (NET) occupancy in the nonhuman primate brain, the relationship between NET occupancy and atomoxetine plasma concentration, and occupancies among different brain regions, were not demonstrated adequately. It may therefore be difficult to translate the results to the clinical situations. In the present study, the detailed change of NET occupancy was investigated among a wider range of doses in a more advanced manner. Methods: Two rhesus monkeys were examined using a high-resolution PET system with (S,S)-[18F]FMeNER-D2 under baseline conditions and after steady-state infusion of different doses of atomoxetine (0.003 to 0.12 mg/kg per hour). NET occupancy of the thalamus, brainstem and anterior cingulate cortex was calculated using BPND obtained with the simplified reference tissue model. Results: NET occupancy increased regionally and uniformly as the plasma concentration of atomoxetine increased. The estimated Kd value (the amount to occupy 50% of NET) in the thalamus was 16 ng/ml. Conclusion: The results indicate that clinical doses of atomoxetine would occupy NET almost completely. © 2009 Springer-Verlag.
Purpose: In a previous PET study on norepinephrine transporter (NET) occupancy in the nonhuman primate brain, the relationship between NET occupancy and atomoxetine plasma concentration, and occupancies among different brain regions, were not demonstrated adequately. It may therefore be difficult to translate the results to the clinical situations. In the present study, the detailed change of NET occupancy was investigated among a wider range of doses in a more advanced manner. Methods: Two rhesus monkeys were examined using a high-resolution PET system with (S,S)-[18F]FMeNER-D2 under baseline conditions and after steady-state infusion of different doses of atomoxetine (0.003 to 0.12 mg/kg per hour). NET occupancy of the thalamus, brainstem and anterior cingulate cortex was calculated using BPND obtained with the simplified reference tissue model. Results: NET occupancy increased regionally and uniformly as the plasma concentration of atomoxetine increased. The estimated Kd value (the amount to occupy 50% of NET) in the thalamus was 16 ng/ml. Conclusion: The results indicate that clinical doses of atomoxetine would occupy NET almost completely. © 2009 Springer-Verlag.
Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D
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Saturated norepinephrine transporter occupancy by atomoxetine relevant to clinical doses: A rhesus monkey study with (S, S)-[18F]FMeNER-D
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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 (704 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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Seneca N, Gulyas B, Varrone A, Schou M, Airaksinen A, Tauscher J, Vandenhende F, Kielbasa W, Farde L, Innis R, Halldin C
* Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2 (602 views)
Psychopharmacology (ISSN: 0033-3158), 2006 Sep; 188(1): 119-127.
Impact Factor: 3.625
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* Quantification of dopamine transporter in human brain using PET with 18F-FE-PE2I (704 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
Seneca N, Gulyas B, Varrone A, Schou M, Airaksinen A, Tauscher J, Vandenhende F, Kielbasa W, Farde L, Innis R, Halldin C
* Atomoxetine occupies the norepinephrine transporter in a dose-dependent fashion: A PET study in nonhuman primate brain using (S, S)-[18F] FMeNER-D2 (602 views)
Psychopharmacology (ISSN: 0033-3158), 2006 Sep; 188(1): 119-127.
Impact Factor: 3.625
View Export to BibTeX Export to EndNote
2 Records (2 excluding Abstracts).
Total impact factor: 9.399 (9.399 excluding Abstracts).
Total 5 year impact factor: 10.543 (10.543 excluding Abstracts).
Total impact factor: 9.399 (9.399 excluding Abstracts).
Total 5 year impact factor: 10.543 (10.543 excluding Abstracts).
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