Radiolabeled glucocorticoids as molecular probes for Imaging brain glucocorticoid receptors by means of positron emission tomography (PET)

被引：14
作者：
Steiniger, Bjoern
Kniess, Torsten
Bergmann, Ralf
Pietzsch, Jens
Wuest, Frank R.
机构：
[1] Institute of Radiopharmacy, Research Center Dresden-Rossendorf, D-01314 Dresden
来源：
MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2008年 / 8卷 / 07期
关键词：
glucocorticoid receptor; PET; radioligands; carbon-11; fluorine-18;
D O I：
10.2174/138955708784567403
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Over the last two decades, numerous attempts have been made to develop C-11- and (18) F-labeled radiotracers in order to study glucocorticoid receptor (GR)-mediated abnormalities of the hypothalamus-pituitary-adrenocortical (HPA) axis function and regulation in vivo by means of positron emission tomography (PET). The present review addresses the research efforts dealing with the design, radiosynthesis and radiopharmacological evaluation of PET radiotracers for brain GR imaging. The underlying problems such as metabolic instability, insufficient blood-brain-barrier penetration and/or high non-specific binding will be discussed.
引用
收藏
页码：728 / 739
页数：12
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