Year: 2016
Type: article
Abstract: Activation of retinoid X receptors (RXRs) has been proposed as a therapeutic mechanism for the treatment of neurodegeneration, including Alzheimer's and Parkinson's diseases. We previously reported radiolabeling of a Food and Drug Administration-approved RXR agonist, bexarotene, by copper-mediated [(11)C]CO2 fixation and preliminary positron emission tomography (PET) neuroimaging that demonstrated brain permeability in nonhuman primate with regional binding distribution consistent with RXRs. In this study, the brain uptake and saturability of [(11)C]bexarotene were studied in rats and nonhuman primates by PET imaging under baseline and greater target occupancy conditions. [(11)C]Bexarotene displays a high proportion of nonsaturable uptake in the brain and is unsuitable for RXR occupancy measurements in the central nervous system.
Source: Molecular Imaging
Language: English
Subfield: Radiology, Nuclear Medicine and Imaging
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $2,175
Awards: Inveon: A Triple Modality Biomedical Imaging System, Combined MRI/PET Imager for Simultaneous Acquisition of PET/MRI Data, Carbon-11 Radiopharmaceutical Production System, New PET tracers for neuroimaging of FAAH in endocannabinoid signaling, 500 MHz NMR Spectrometer for Molecular Imaging Applications
OpenAlex ID: W2507378769