Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150

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

Standard

Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150. / Edgar, Fraser Graeme; Hansen, Hanne D; Leth-Petersen, Sebastian; Ettrup, Anders; Kristensen, Jesper L; Knudsen, Gitte M; Herth, Matthias M.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 60, No. 12, 10.2017, p. 586-591.

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

Harvard

Edgar, FG, Hansen, HD, Leth-Petersen, S, Ettrup, A, Kristensen, JL, Knudsen, GM & Herth, MM 2017, 'Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150', Journal of Labelled Compounds and Radiopharmaceuticals, vol. 60, no. 12, pp. 586-591. https://doi.org/10.1002/jlcr.3557

APA

Edgar, F. G., Hansen, H. D., Leth-Petersen, S., Ettrup, A., Kristensen, J. L., Knudsen, G. M., & Herth, M. M. (2017). Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150. Journal of Labelled Compounds and Radiopharmaceuticals, 60(12), 586-591. https://doi.org/10.1002/jlcr.3557

Vancouver

Edgar FG, Hansen HD, Leth-Petersen S, Ettrup A, Kristensen JL, Knudsen GM et al. Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150. Journal of Labelled Compounds and Radiopharmaceuticals. 2017 Oct;60(12):586-591. https://doi.org/10.1002/jlcr.3557

Author

Edgar, Fraser Graeme ; Hansen, Hanne D ; Leth-Petersen, Sebastian ; Ettrup, Anders ; Kristensen, Jesper L ; Knudsen, Gitte M ; Herth, Matthias M. / Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150. In: Journal of Labelled Compounds and Radiopharmaceuticals. 2017 ; Vol. 60, No. 12. pp. 586-591.

Bibtex

@article{1fd11bd99a5540b69696c51300bac4ff,

title = "Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150",

abstract = "An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11 C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18 F-labelled agonist 5-HT2A receptor (5-HT2A R) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2A R. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2A R; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2A R antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2A R.",

keywords = "Journal Article",

author = "Edgar, {Fraser Graeme} and Hansen, {Hanne D} and Sebastian Leth-Petersen and Anders Ettrup and Kristensen, {Jesper L} and Knudsen, {Gitte M} and Herth, {Matthias M}",

note = "Copyright {\textcopyright} 2017 John Wiley & Sons, Ltd.",

year = "2017",

month = oct,

doi = "10.1002/jlcr.3557",

language = "English",

volume = "60",

pages = "586--591",

journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

issn = "0362-4803",

publisher = "JohnWiley & Sons Ltd",

number = "12",

}

RIS

TY - JOUR

T1 - Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18 F]Cimbi-92 and [18 F]Cimbi-150

AU - Edgar, Fraser Graeme

AU - Hansen, Hanne D

AU - Leth-Petersen, Sebastian

AU - Ettrup, Anders

AU - Kristensen, Jesper L

AU - Knudsen, Gitte M

AU - Herth, Matthias M

PY - 2017/10

Y1 - 2017/10

N2 - An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11 C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18 F-labelled agonist 5-HT2A receptor (5-HT2A R) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2A R. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2A R; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2A R antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2A R.

AB - An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11 C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18 F-labelled agonist 5-HT2A receptor (5-HT2A R) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2A R. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2A R; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2A R antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2A R.

KW - Journal Article

U2 - 10.1002/jlcr.3557

DO - 10.1002/jlcr.3557

M3 - Journal article

C2 - 28856700

VL - 60

SP - 586

EP - 591

JO - Journal of Labelled Compounds and Radiopharmaceuticals

JF - Journal of Labelled Compounds and Radiopharmaceuticals

SN - 0362-4803

IS - 12

ER -

ID: 187076476