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

被引：6

作者：

Herth, Matthias M. ^{[1
]}

Kramer, Vasko ^{[2
]}

Gillings, Nic ^{[3
]}

Roesch, Frank ^{[2
]}

Knudsen, Gitte M. ^{[1
]}

机构：

[1] Rigshosp, Ctr Integrated Mol Brain Imaging, Copenhagen Univ Hosp, DK-2100 Copenhagen, Denmark

[2] Johannes Gutenberg Univ Mainz, Inst Nucl Chem, D-55128 Mainz, Germany

[3] Rigshosp, PET & Cyclotron Unit, Copenhagen Univ Hosp, DK-2100 Copenhagen, Denmark

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2012年 / 55卷 / 09期

关键词：

MDL; 100907; 18F]MH; MZ; PET; 5-HT2A receptor; SEROTONIN RECEPTORS; DISORDERS; BEHAVIOR; LIGAND; F-18;

D O I：

10.1002/jlcr.2947

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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 (c) 2012 John Wiley & Sons, Ltd.

引用

页码：354 / 358

页数：5

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