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

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Abstrakt

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.
OriginalsprogEngelsk
TidsskriftJournal of Nuclear Medicine
Vol/bind51
Udgave nummer11
Sider (fra-til)1763-70
Antal sider8
ISSN0161-5505
DOI
StatusUdgivet - 1. nov. 2010
Udgivet eksterntJa

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