Radiolabeled glucocorticoids as molecular probes for imaging brain glucocorticoid receptors by means of positron emission tomography (PET).
Over the last two decades, numerous attempts have been made to develop (11)C- 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.
Steiniger
Björn
B
Institute of Radiopharmacy, Research Center Dresden-Rossendorf, D-01314 Dresden, Germany.
Kniess
Torsten
T
Bergmann
Ralf
R
Pietzsch
Jens
J
Wuest
Frank R
FR
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D005938:Glucocorticoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D015335:Molecular Probes / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D011965:Receptors, Glucocorticoid / Q000032:analysis* / Q000502:physiology
D005938:Glucocorticoids; D015335:Molecular Probes; D019275:Radiopharmaceuticals; D011965:Receptors, Glucocorticoid