(11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

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(11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand. / Andersen, Valdemar L; Hansen, Hanne D; Herth, Matthias M; Dyssegaard, Agnete; Knudsen, Gitte M; Kristensen, Jesper Langgaard.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 25, No. 5, 20.01.2015, p. 1053–1056.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Andersen, VL, Hansen, HD, Herth, MM, Dyssegaard, A, Knudsen, GM & Kristensen, JL 2015, '(11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand', Bioorganic & Medicinal Chemistry Letters, vol. 25, no. 5, pp. 1053–1056. https://doi.org/10.1016/j.bmcl.2015.01.017

APA

Andersen, V. L., Hansen, H. D., Herth, M. M., Dyssegaard, A., Knudsen, G. M., & Kristensen, J. L. (2015). (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand. Bioorganic & Medicinal Chemistry Letters, 25(5), 1053–1056. https://doi.org/10.1016/j.bmcl.2015.01.017

Vancouver

Andersen VL, Hansen HD, Herth MM, Dyssegaard A, Knudsen GM, Kristensen JL. (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand. Bioorganic & Medicinal Chemistry Letters. 2015 Jan 20;25(5):1053–1056. https://doi.org/10.1016/j.bmcl.2015.01.017

Author

Andersen, Valdemar L ; Hansen, Hanne D ; Herth, Matthias M ; Dyssegaard, Agnete ; Knudsen, Gitte M ; Kristensen, Jesper Langgaard. / (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand. In: Bioorganic & Medicinal Chemistry Letters. 2015 ; Vol. 25, No. 5. pp. 1053–1056.

Bibtex

@article{ff5e493f5abf420f8f3193ce993ef04f,
title = "(11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand",
abstract = "Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving radiochemical yields in the range of 1-1.7GBq (n=4). In Danish Landrace pigs the radio ligand readily entered the brain and displayed binding in the cortex in accordance with the distribution of 5-HT2ARs. However, this binding could not be blocked by either ketanserin or pimavanserin itself, indicating high nonspecific binding. The lack of displacement by the 5-HT2R antagonist and binding in the thalamus suggests that [(11)C]pimavanserin is not selective for the 5-HT2AR in pigs.",
author = "Andersen, {Valdemar L} and Hansen, {Hanne D} and Herth, {Matthias M} and Agnete Dyssegaard and Knudsen, {Gitte M} and Kristensen, {Jesper Langgaard}",
note = "Copyright {\textcopyright} 2015 Elsevier Ltd. All rights reserved.",
year = "2015",
month = jan,
day = "20",
doi = "10.1016/j.bmcl.2015.01.017",
language = "English",
volume = "25",
pages = "1053–1056",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "5",

}

RIS

TY - JOUR

T1 - (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

AU - Andersen, Valdemar L

AU - Hansen, Hanne D

AU - Herth, Matthias M

AU - Dyssegaard, Agnete

AU - Knudsen, Gitte M

AU - Kristensen, Jesper Langgaard

N1 - Copyright © 2015 Elsevier Ltd. All rights reserved.

PY - 2015/1/20

Y1 - 2015/1/20

N2 - Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving radiochemical yields in the range of 1-1.7GBq (n=4). In Danish Landrace pigs the radio ligand readily entered the brain and displayed binding in the cortex in accordance with the distribution of 5-HT2ARs. However, this binding could not be blocked by either ketanserin or pimavanserin itself, indicating high nonspecific binding. The lack of displacement by the 5-HT2R antagonist and binding in the thalamus suggests that [(11)C]pimavanserin is not selective for the 5-HT2AR in pigs.

AB - Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. Here, we detail the (11)C-labeling and subsequently evaluate pimavanserin as a PET-radioligand in pigs. [(11)C]Pimavanserin was obtained by N-methylation of an appropriate precursor using [(11)C]MeOTf in acetone at 60°C giving radiochemical yields in the range of 1-1.7GBq (n=4). In Danish Landrace pigs the radio ligand readily entered the brain and displayed binding in the cortex in accordance with the distribution of 5-HT2ARs. However, this binding could not be blocked by either ketanserin or pimavanserin itself, indicating high nonspecific binding. The lack of displacement by the 5-HT2R antagonist and binding in the thalamus suggests that [(11)C]pimavanserin is not selective for the 5-HT2AR in pigs.

U2 - 10.1016/j.bmcl.2015.01.017

DO - 10.1016/j.bmcl.2015.01.017

M3 - Journal article

C2 - 25655720

VL - 25

SP - 1053

EP - 1056

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 5

ER -

ID: 131104161