Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers

Anders Ettrup; Martin Hansen; Martin A Santini; James Stephen Paine; Nic Gillings; Mikael Palner; Szabolcs Lehel; Matthias Manfred Herth; Jacob Madsen; Jesper Langgaard Kristensen; Mikael Begtrup; Gitte Moos Knudsen

doi:10.1007/s00259-010-1686-8

Radiosynthesis and in vivo evaluation of a series of substituted ¹¹C-phenethylamines as 5-HT_2A agonist PET tracers

Anders Ettrup, Martin Hansen, Martin A Santini, James Stephen Paine, Nic Gillings, Mikael Palner, Szabolcs Lehel, Matthias Manfred Herth, Jacob Madsen, Jesper Langgaard Kristensen, Mikael Begtrup, Gitte Moos Knudsen

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

113 Citations (Scopus)

Abstract

Positron emission tomography (PET) imaging of serotonin 2A (5-HT(2A)) receptors with agonist tracers holds promise for the selective labelling of 5-HT(2A) receptors in their high-affinity state. We have previously validated [(11)C]Cimbi-5 and found that it is a 5-HT(2A) receptor agonist PET tracer. In an attempt to further optimize the target-to-background binding ratio, we modified the chemical structure of the phenethylamine backbone and carbon-11 labelling site of [(11)C]Cimbi-5 in different ways. Here, we present the in vivo validation of nine novel 5-HT(2A) receptor agonist PET tracers in the pig brain.

Original language	English
Journal	European Journal of Nuclear Medicine and Molecular Imaging
Volume	38
Issue number	4
Pages (from-to)	681-693
ISSN	1619-7070
DOIs	https://doi.org/10.1007/s00259-010-1686-8
Publication status	Published - 1 Apr 2011

Keywords

Faculty of Health and Medical Sciences

Access to Document

10.1007/s00259-010-1686-8

Cite this

Ettrup, A., Hansen, M., Santini, M. A., Paine, J. S., Gillings, N., Palner, M., Lehel, S., Herth, M. M., Madsen, J., Kristensen, J. L., Begtrup, M., & Knudsen, G. M. (2011). Radiosynthesis and in vivo evaluation of a series of substituted ¹¹C-phenethylamines as 5-HT_2A agonist PET tracers. European Journal of Nuclear Medicine and Molecular Imaging, 38(4), 681-693. https://doi.org/10.1007/s00259-010-1686-8

Radiosynthesis and in vivo evaluation of a series of substituted ¹¹C-phenethylamines as 5-HT_2A agonist PET tracers. / Ettrup, Anders; Hansen, Martin; Santini, Martin A; Paine, James Stephen; Gillings, Nic; Palner, Mikael; Lehel, Szabolcs; Herth, Matthias Manfred; Madsen, Jacob; Kristensen, Jesper Langgaard; Begtrup, Mikael; Knudsen, Gitte Moos.

In: European Journal of Nuclear Medicine and Molecular Imaging, Vol. 38, No. 4, 01.04.2011, p. 681-693.

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

Ettrup, A, Hansen, M, Santini, MA, Paine, JS, Gillings, N, Palner, M, Lehel, S, Herth, MM, Madsen, J, Kristensen, JL, Begtrup, M & Knudsen, GM 2011, 'Radiosynthesis and in vivo evaluation of a series of substituted ¹¹C-phenethylamines as 5-HT_2A agonist PET tracers', European Journal of Nuclear Medicine and Molecular Imaging, vol. 38, no. 4, pp. 681-693. https://doi.org/10.1007/s00259-010-1686-8

Ettrup, Anders ; Hansen, Martin ; Santini, Martin A ; Paine, James Stephen ; Gillings, Nic ; Palner, Mikael ; Lehel, Szabolcs ; Herth, Matthias Manfred ; Madsen, Jacob ; Kristensen, Jesper Langgaard ; Begtrup, Mikael ; Knudsen, Gitte Moos. / Radiosynthesis and in vivo evaluation of a series of substituted ¹¹C-phenethylamines as 5-HT_2A agonist PET tracers. In: European Journal of Nuclear Medicine and Molecular Imaging. 2011 ; Vol. 38, No. 4. pp. 681-693.

@article{b7c5930be4414d0eb916a18e227b457c,

title = "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers",

abstract = "Positron emission tomography (PET) imaging of serotonin 2A (5-HT(2A)) receptors with agonist tracers holds promise for the selective labelling of 5-HT(2A) receptors in their high-affinity state. We have previously validated [(11)C]Cimbi-5 and found that it is a 5-HT(2A) receptor agonist PET tracer. In an attempt to further optimize the target-to-background binding ratio, we modified the chemical structure of the phenethylamine backbone and carbon-11 labelling site of [(11)C]Cimbi-5 in different ways. Here, we present the in vivo validation of nine novel 5-HT(2A) receptor agonist PET tracers in the pig brain.",

keywords = "Faculty of Health and Medical Sciences",

author = "Anders Ettrup and Martin Hansen and Santini, {Martin A} and Paine, {James Stephen} and Nic Gillings and Mikael Palner and Szabolcs Lehel and Herth, {Matthias Manfred} and Jacob Madsen and Kristensen, {Jesper Langgaard} and Mikael Begtrup and Knudsen, {Gitte Moos}",

note = "Keywords: PET tracer development, 5-HT(2A), agonist, porcine, serotonin receptors, [11C]Cimbi-36",

year = "2011",

month = apr,

day = "1",

doi = "10.1007/s00259-010-1686-8",

language = "English",

volume = "38",

pages = "681--693",

journal = "European Journal of Nuclear Medicine and Molecular Imaging",

issn = "1619-7070",

publisher = "Springer",

number = "4",

}

TY - JOUR

T1 - Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers

AU - Ettrup, Anders

AU - Hansen, Martin

AU - Santini, Martin A

AU - Paine, James Stephen

AU - Gillings, Nic

AU - Palner, Mikael

AU - Lehel, Szabolcs

AU - Herth, Matthias Manfred

AU - Madsen, Jacob

AU - Kristensen, Jesper Langgaard

AU - Begtrup, Mikael

AU - Knudsen, Gitte Moos

N1 - Keywords: PET tracer development, 5-HT(2A), agonist, porcine, serotonin receptors, [11C]Cimbi-36

PY - 2011/4/1

Y1 - 2011/4/1

N2 - Positron emission tomography (PET) imaging of serotonin 2A (5-HT(2A)) receptors with agonist tracers holds promise for the selective labelling of 5-HT(2A) receptors in their high-affinity state. We have previously validated [(11)C]Cimbi-5 and found that it is a 5-HT(2A) receptor agonist PET tracer. In an attempt to further optimize the target-to-background binding ratio, we modified the chemical structure of the phenethylamine backbone and carbon-11 labelling site of [(11)C]Cimbi-5 in different ways. Here, we present the in vivo validation of nine novel 5-HT(2A) receptor agonist PET tracers in the pig brain.

AB - Positron emission tomography (PET) imaging of serotonin 2A (5-HT(2A)) receptors with agonist tracers holds promise for the selective labelling of 5-HT(2A) receptors in their high-affinity state. We have previously validated [(11)C]Cimbi-5 and found that it is a 5-HT(2A) receptor agonist PET tracer. In an attempt to further optimize the target-to-background binding ratio, we modified the chemical structure of the phenethylamine backbone and carbon-11 labelling site of [(11)C]Cimbi-5 in different ways. Here, we present the in vivo validation of nine novel 5-HT(2A) receptor agonist PET tracers in the pig brain.

KW - Faculty of Health and Medical Sciences

U2 - 10.1007/s00259-010-1686-8

DO - 10.1007/s00259-010-1686-8

M3 - Journal article

C2 - 21174090

VL - 38

SP - 681

EP - 693

JO - European Journal of Nuclear Medicine and Molecular Imaging

JF - European Journal of Nuclear Medicine and Molecular Imaging

SN - 1619-7070

IS - 4

ER -