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; Nicolas Gillings; Mikael Palner; S Lehel; Matthias M Herth; Jacob Madsen; Jesper Kristensen; Mikael Erik Begtrup; Gitte M 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, Nicolas Gillings, Mikael Palner, S Lehel, Matthias M Herth, Jacob Madsen, Jesper Kristensen, Mikael Erik Begtrup, Gitte M Knudsen

117 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)	681-93
Number of pages	13
ISSN	1619-7070
DOIs	https://doi.org/10.1007/s00259-010-1686-8
Publication status	Published - 2011

Keywords

Animals
Biological Transport
Brain
Carbon Radioisotopes
Female
Humans
Hydrolysis
Injections, Intravenous
Ketanserin
Phenethylamines
Phosphatidylinositols
Positron-Emission Tomography
Radioactive Tracers
Radiochemistry
Receptor, Serotonin, 5-HT2A
Serotonin 5-HT2 Receptor Agonists
Swine

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Ettrup, A., Hansen, M., Santini, M. A., Paine, J. S., Gillings, N., Palner, M., Lehel, S., Herth, M. M., Madsen, J., Kristensen, J., Begtrup, M. E., & 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), 681-93. https://doi.org/10.1007/s00259-010-1686-8

Ettrup, A, Hansen, M, Santini, MA, Paine, JS, Gillings, N, Palner, M, Lehel, S, Herth, MM, Madsen, J, Kristensen, J, Begtrup, ME & 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. 681-93. https://doi.org/10.1007/s00259-010-1686-8

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title = "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT (2A) 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.",

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author = "Anders Ettrup and Martin Hansen and Santini, \{Martin A\} and Paine, \{James Stephen\} and Nicolas Gillings and Mikael Palner and S Lehel and Herth, \{Matthias M\} and Jacob Madsen and Jesper Kristensen and Begtrup, \{Mikael Erik\} and Knudsen, \{Gitte M\}",

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

language = "English",

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AU - Ettrup, Anders

AU - Hansen, Martin

AU - Santini, Martin A

AU - Paine, James Stephen

AU - Gillings, Nicolas

AU - Palner, Mikael

AU - Lehel, S

AU - Herth, Matthias M

AU - Madsen, Jacob

AU - Kristensen, Jesper

AU - Begtrup, Mikael Erik

AU - Knudsen, Gitte M

PY - 2011

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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 - Animals

KW - Biological Transport

KW - Brain

KW - Carbon Radioisotopes

KW - Female

KW - Humans

KW - Hydrolysis

KW - Injections, Intravenous

KW - Ketanserin

KW - Phenethylamines

KW - Phosphatidylinositols

KW - Positron-Emission Tomography

KW - Radioactive Tracers

KW - Radiochemistry

KW - Receptor, Serotonin, 5-HT2A

KW - Serotonin 5-HT2 Receptor Agonists

KW - Swine

UR - https://www.scopus.com/pages/publications/79953727230

U2 - 10.1007/s00259-010-1686-8

DO - 10.1007/s00259-010-1686-8

M3 - Journal article

C2 - 21174090

SN - 1619-7070

VL - 38

SP - 681

EP - 693

JO - European Journal of Nuclear Medicine and Molecular Imaging

JF - European Journal of Nuclear Medicine and Molecular Imaging

IS - 4

ER -

Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT (2A) agonist PET tracers

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