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

Anders Ettrup; Mikael Palner; Nic Gillings; Martin A Santini; Martin Hansen; Birgitte Rahbek Kornum; Lars K Rasmussen; Kjell Någren; Jacob Madsen; Mikael Begtrup; Gitte Moos Knudsen

doi:10.2967/jnumed.109.074021

Radiosynthesis and evaluation of ¹¹C-CIMBI-5 as a 5-HT_2A receptor agonist radioligand for PET

Anders Ettrup, Mikael Palner, Nic Gillings, Martin A Santini, Martin Hansen, Birgitte Rahbek Kornum, Lars K Rasmussen, Kjell Någren, Jacob Madsen, Mikael Begtrup, Gitte Moos Knudsen

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

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	The Journal of Nuclear Medicine
Volume	51
Issue number	11
Pages (from-to)	1763-70
ISSN	0161-5505
DOIs	https://doi.org/10.2967/jnumed.109.074021
Publication status	Published - 1. Nov 2010
Externally published	Yes

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@article{46eaa29485344dab9761ea46cd745999,

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.",

author = "Anders Ettrup and Mikael Palner and Nic Gillings and Santini, {Martin A} and Martin Hansen and Kornum, {Birgitte Rahbek} and Rasmussen, {Lars K} and Kjell N{\aa}gren and Jacob Madsen and Mikael Begtrup and Knudsen, {Gitte Moos}",

year = "2010",

month = nov,

day = "1",

doi = "10.2967/jnumed.109.074021",

language = "English",

volume = "51",

pages = "1763--70",

journal = "The Journal of Nuclear Medicine",

issn = "0161-5505",

number = "11",

}

TY - JOUR

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, Nic

AU - Santini, Martin A

AU - Hansen, Martin

AU - Kornum, Birgitte Rahbek

AU - Rasmussen, Lars K

AU - Någren, Kjell

AU - Madsen, Jacob

AU - Begtrup, Mikael

AU - Knudsen, Gitte Moos

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.

U2 - 10.2967/jnumed.109.074021

DO - 10.2967/jnumed.109.074021

M3 - Journal article

C2 - 20956470

SN - 0161-5505

VL - 51

SP - 1763

EP - 1770

JO - The Journal of Nuclear Medicine

JF - The Journal of Nuclear Medicine

IS - 11