Radiosynthesis and evaluation of 11C-CIMBI-5 as a 5-HT2A receptor agonist radioligand for PET

Anders Ettrup; Mikael Palner; Nicolas Gillings; Martin A Santini; Martin Hansen; Birgitte R Kornum; Lars Kildehøj Rasmussen; Kjell Åke Någren; Jacob Madsen; Mikael Begtrup; Gitte M Knudsen

doi:10.2967/jnumed.109.074021

Radiosynthesis and evaluation of 11C-CIMBI-5 as a 5-HT2A receptor agonist radioligand for PET

Anders Ettrup, Mikael Palner, Nicolas Gillings, Martin A Santini, Martin Hansen, Birgitte R Kornum, Lars Kildehøj Rasmussen, Kjell Åke Någren, Jacob Madsen, Mikael Begtrup, Gitte M Knudsen

45 Citations (Scopus)

Abstract

PET brain imaging of the serotonin 2A (5-hydroxytryptamine 2A, or 5-HT(2A)) receptor has been widely used in clinical studies, and currently, several well-validated radiolabeled antagonist tracers are used for in vivo imaging of the cerebral 5-HT(2A) receptor. Access to 5-HT(2A) receptor agonist PET tracers would, however, enable imaging of the active, high-affinity state of receptors, which may provide a more meaningful assessment of membrane-bound receptors. In this study, we radiolabel the high-affinity 5-HT(2A) receptor agonist 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-[(11)C-OCH(3)]methoxybenzyl)ethanamine ((11)C-CIMBI-5) and investigate its potential as a PET tracer.

Original language	English
Journal	Journal of Nuclear Medicine
Volume	51
Issue number	11
Pages (from-to)	1763-70
Number of pages	8
ISSN	0161-5505
DOIs	https://doi.org/10.2967/jnumed.109.074021
Publication status	Published - 1 Nov 2010

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title = "Radiosynthesis and evaluation of 11C-CIMBI-5 as a 5-HT2A receptor agonist radioligand for PET",

abstract = "PET brain imaging of the serotonin 2A (5-hydroxytryptamine 2A, or 5-HT(2A)) receptor has been widely used in clinical studies, and currently, several well-validated radiolabeled antagonist tracers are used for in vivo imaging of the cerebral 5-HT(2A) receptor. Access to 5-HT(2A) receptor agonist PET tracers would, however, enable imaging of the active, high-affinity state of receptors, which may provide a more meaningful assessment of membrane-bound receptors. In this study, we radiolabel the high-affinity 5-HT(2A) receptor agonist 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-[(11)C-OCH(3)]methoxybenzyl)ethanamine ((11)C-CIMBI-5) and investigate its potential as a PET tracer.",

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doi = "10.2967/jnumed.109.074021",

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T1 - Radiosynthesis and evaluation of 11C-CIMBI-5 as a 5-HT2A receptor agonist radioligand for PET

AU - Ettrup, Anders

AU - Palner, Mikael

AU - Gillings, Nicolas

AU - Santini, Martin A

AU - Hansen, Martin

AU - Kornum, Birgitte R

AU - Rasmussen, Lars Kildehøj

AU - Någren, Kjell Åke

AU - Madsen, Jacob

AU - Begtrup, Mikael

AU - Knudsen, Gitte M

PY - 2010/11/1

Y1 - 2010/11/1

N2 - PET brain imaging of the serotonin 2A (5-hydroxytryptamine 2A, or 5-HT(2A)) receptor has been widely used in clinical studies, and currently, several well-validated radiolabeled antagonist tracers are used for in vivo imaging of the cerebral 5-HT(2A) receptor. Access to 5-HT(2A) receptor agonist PET tracers would, however, enable imaging of the active, high-affinity state of receptors, which may provide a more meaningful assessment of membrane-bound receptors. In this study, we radiolabel the high-affinity 5-HT(2A) receptor agonist 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-[(11)C-OCH(3)]methoxybenzyl)ethanamine ((11)C-CIMBI-5) and investigate its potential as a PET tracer.

AB - PET brain imaging of the serotonin 2A (5-hydroxytryptamine 2A, or 5-HT(2A)) receptor has been widely used in clinical studies, and currently, several well-validated radiolabeled antagonist tracers are used for in vivo imaging of the cerebral 5-HT(2A) receptor. Access to 5-HT(2A) receptor agonist PET tracers would, however, enable imaging of the active, high-affinity state of receptors, which may provide a more meaningful assessment of membrane-bound receptors. In this study, we radiolabel the high-affinity 5-HT(2A) receptor agonist 2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-[(11)C-OCH(3)]methoxybenzyl)ethanamine ((11)C-CIMBI-5) and investigate its potential as a PET tracer.

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SN - 0161-5505

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SP - 1763

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JO - Journal of Nuclear Medicine

JF - Journal of Nuclear Medicine

IS - 11

ER -

Radiosynthesis and evaluation of 11C-CIMBI-5 as a 5-HT2A receptor agonist radioligand for PET

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