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 - Journal of Nuclear Medicine
JF - Journal of Nuclear Medicine
IS - 11
ER -