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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Radiolabeled Glucocorticoids as Molecular Probes for Imaging Brain Glucocorticoid Receptors by Means of Positron Emission Tomography (PET)

Author(s): Bjorn Steiniger, Torsten Kniess, Ralf Bergmann, Jens Pietzsch and Frank R. Wuest

Volume 8, Issue 7, 2008

Page: [728 - 739] Pages: 12

DOI: 10.2174/138955708784567403

Price: $65


Over the last two decades, numerous attempts have been made to develop 11C- and 18F-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.

Keywords: Glucocorticoid receptor, PET, radioligands, carbon-11, fluorine-18

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