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

Research output: Contribution to journalJournal articleResearchpeer-review

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

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 languageEnglish
JournalJournal of Nuclear Medicine
Volume51
Issue number11
Pages (from-to)1763-1770
ISSN0161-5505
DOIs
Publication statusPublished - 1 Nov 2010

ID: 33532568