6533b82ffe1ef96bd12959aa

RESEARCH PRODUCT

Direct radiofluorination of [18F]MH.MZ for 5-HT2A receptor molecular imaging with PET

Gitte M. KnudsenFrank RöschMatthias M. HerthVasko KramerNic Gillings

subject

medicine.diagnostic_testChemistryOrganic ChemistryRadiochemistryAnalytical chemistryBiochemistryAnalytical Chemistrychemistry.chemical_compoundPositron emission tomographyLabellingDrug DiscoveryAltanserinmedicineRadiology Nuclear Medicine and imagingMolecular imagingSelectivitySerotonin 2aSpectroscopy

description

Imaging the serotonin 2A neuroreceptor with positron emission tomography has been carried out with [11C]MDL 100907 and [18F]altanserin for years. Recently, the MDL 100907 analogue [18F]MH.MZ was developed by combining the increased selectivity profile of MDL 100907 and the favourable radiophysical properties of fluorine-18. Here, we want to report the synthesis of [18F]MH.MZ via direct radiofluorination. Unfortunately, the direct radiofluorination did not have any significant benefits over the indirect labelling method. This is mainly because the precursor for the direct labelling approach is not completely stable and slowly decomposes. However, only one HPLC separation is necessary for the direct 18F-nucleophilic labelling procedure, and accordingly, automation is easier. Copyright © 2012 John Wiley & Sons, Ltd.

https://doi.org/10.1002/jlcr.2947