Occupancy of the Serotonin Transporter after Administration of Lu AA21004 and its Relation to Plasma Concentration in Healthy Subjects

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Bibliographic Details
Published inBasic & clinical pharmacology & toxicology Vol. 110; no. 4; pp. 401 - 404
Main Authors Areberg, Johan, Luntang-Jensen, Michael, Søgaard, Birgitte, Nilausen, Dorrit Ø.
Format Journal Article
LanguageEnglish
Published Oxford, UK Blackwell Publishing Ltd 01.04.2012
Blackwell
Subjects
Adult
Biological and medical sciences
Brain - metabolism
Dose-Response Relationship, Drug
Female
Humans
Male
Medical sciences
Pharmacology. Drug treatments
Piperazines - administration & dosage
Piperazines - pharmacokinetics
Piperazines - pharmacology
Serotonin Plasma Membrane Transport Proteins - metabolism
Sulfides - administration & dosage
Sulfides - pharmacokinetics
Sulfides - pharmacology
Tomography, Emission-Computed - methods
Young Adult
Human
Serotonin transporter
Healthy subject
Pharmacokinetics
Online AccessGet full text

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Author Søgaard, Birgitte
Luntang-Jensen, Michael
Nilausen, Dorrit Ø.
Areberg, Johan
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  givenname: Michael
  surname: Luntang-Jensen
  fullname: Luntang-Jensen, Michael
  organization: Division of Clinical and Quantitative Pharmacology, H. Lundbeck A/S, Valby, Denmark
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  givenname: Birgitte
  surname: Søgaard
  fullname: Søgaard, Birgitte
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  givenname: Dorrit Ø.
  surname: Nilausen
  fullname: Nilausen, Dorrit Ø.
  organization: Division of Clinical and Quantitative Pharmacology, H. Lundbeck A/S, Valby, Denmark
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Cites_doi 10.1002/syn.890200107
10.1021/jm101459g
10.1016/S0924-977X(09)70661-3
10.1002/syn.20443
10.1002/syn.20297
10.1016/S0924-977X(08)70440-1
10.1016/j.biopsych.2005.04.038
10.1176/appi.ajp.158.11.1843
10.1007/s00213-006-0540-y
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Keywords Human
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Pharmacokinetics
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References Praschak-Rieder N, Wilson AA, Hussey D, Carella A, Wei C, Ginovart N et al. Effects of tryptophan depletion on the serotonin transporter in healthy humans. Biol Psychiatry 2005;58:825-30.
Lundberg J, Odano I, Olsson H, Halldin C, Farde L. Quantification of 11C-MADAM binding to the serotonin transporter in the human brain. J Nucl Med 2005;46:1505-15.
Elfving B, Madsen J, Knudsen GM. Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Synapse 2007;61:882-8.
Elfving B, Madsen J, Knudsen G-M. Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Synapse 2007;61:882-8.
Catafau AM, Perez V, Plaza P, Pascual J-C, Bullich S, Marina Suarez M et al. Serotonin transporter occupancy induced by paroxetine in patients with major depression disorder: a 123I-ADAM SPECT study. Psychopharmacology 2006;189:145-53.
Lundberg J, Halldin C, Farde L. Measurement of serotonin transporter binding with PET and [11C]MADAM: a test-retest reproducibility study. Synapse 2006;60:256-63.
Meyer JH. Imaging the serotonin transporter during major depressive disorder and antidepressant treatment. Rev Psychiatr Neurosc 2007;32:86-102.
Artigas F, Dragheim M, Loft H, Perez V, Alvarez E. A randomised, double-blind, placebo-controlled, active-referenced study of Lu AA21004 in patients with major depression. Eur Neuropsychopharmacol 2009;19(Suppl. 3):S426-7.
Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG et al. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem 2011;54:3206-21.
Meyer JH, Wilson AA, Ginovart N, Goulding V, Hussey D, Hood K et al. Occupancy of serotonin transporters by paroxetine and citalopram during treatment of depression: a [11C]DASB PET imaging study. Am J Psychiatry 2001;158:1843-9.
Frankle WG, Huang Y, Hwang DR, Talbot PS, Slifstein M, Van Heertum R et al. Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans. J Nucl Med 2004;45:682-94.
Szabo Z, Kao PF, Scheffel U, Suehiro M, Mathews WB, Ravert HT et al. Positron emission tomography imaging of serotonin transporters in the human brain using [11C](+)McN5652. Synapse 1995;20:37-43.
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References_xml – reference: Elfving B, Madsen J, Knudsen GM. Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Synapse 2007;61:882-8.
– reference: Frankle WG, Huang Y, Hwang DR, Talbot PS, Slifstein M, Van Heertum R et al. Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans. J Nucl Med 2004;45:682-94.
– reference: Catafau AM, Perez V, Plaza P, Pascual J-C, Bullich S, Marina Suarez M et al. Serotonin transporter occupancy induced by paroxetine in patients with major depression disorder: a 123I-ADAM SPECT study. Psychopharmacology 2006;189:145-53.
– reference: Lundberg J, Halldin C, Farde L. Measurement of serotonin transporter binding with PET and [11C]MADAM: a test-retest reproducibility study. Synapse 2006;60:256-63.
– reference: Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG et al. Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem 2011;54:3206-21.
– reference: Meyer JH, Wilson AA, Ginovart N, Goulding V, Hussey D, Hood K et al. Occupancy of serotonin transporters by paroxetine and citalopram during treatment of depression: a [11C]DASB PET imaging study. Am J Psychiatry 2001;158:1843-9.
– reference: Artigas F, Dragheim M, Loft H, Perez V, Alvarez E. A randomised, double-blind, placebo-controlled, active-referenced study of Lu AA21004 in patients with major depression. Eur Neuropsychopharmacol 2009;19(Suppl. 3):S426-7.
– reference: Elfving B, Madsen J, Knudsen G-M. Neuroimaging of the serotonin reuptake site requires high-affinity ligands. Synapse 2007;61:882-8.
– reference: Meyer JH. Imaging the serotonin transporter during major depressive disorder and antidepressant treatment. Rev Psychiatr Neurosc 2007;32:86-102.
– reference: Moore NA, Bang-Andersen B, Brennum LT, Frederiksen K, Hogg S, Mørk A et al. Lu AA21004: a novel potential treatment for mood disorders. Eur Neuropsychopharmacol 2008;18(Suppl. 4):S321.
– reference: Praschak-Rieder N, Wilson AA, Hussey D, Carella A, Wei C, Ginovart N et al. Effects of tryptophan depletion on the serotonin transporter in healthy humans. Biol Psychiatry 2005;58:825-30.
– reference: Lundberg J, Odano I, Olsson H, Halldin C, Farde L. Quantification of 11C-MADAM binding to the serotonin transporter in the human brain. J Nucl Med 2005;46:1505-15.
– reference: Szabo Z, Kao PF, Scheffel U, Suehiro M, Mathews WB, Ravert HT et al. Positron emission tomography imaging of serotonin transporters in the human brain using [11C](+)McN5652. Synapse 1995;20:37-43.
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  article-title: Comparative evaluation of serotonin transporter radioligands 11C‐DASB and 11C‐McN 5652 in healthy humans
  publication-title: J Nucl Med
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– volume: 32
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  publication-title: Rev Psychiatr Neurosc
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Enrichment Source
Publisher
StartPage 401
SubjectTerms Adult
Biological and medical sciences
Brain - metabolism
Dose-Response Relationship, Drug
Female
Humans
Male
Medical sciences
Pharmacology. Drug treatments
Piperazines - administration & dosage
Piperazines - pharmacokinetics
Piperazines - pharmacology
Serotonin Plasma Membrane Transport Proteins - metabolism
Sulfides - administration & dosage
Sulfides - pharmacokinetics
Sulfides - pharmacology
Tomography, Emission-Computed - methods
Young Adult
Title Occupancy of the Serotonin Transporter after Administration of Lu AA21004 and its Relation to Plasma Concentration in Healthy Subjects
URI https://api.istex.fr/ark:/67375/WNG-28RKZXQT-0/fulltext.pdf
https://onlinelibrary.wiley.com/doi/abs/10.1111%2Fj.1742-7843.2011.00810.x
https://www.ncbi.nlm.nih.gov/pubmed/21985522
https://www.proquest.com/docview/928906453
Volume 110
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