Preclinical PET Neuroimaging of [C]Bexarotene

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-...

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Main Authors:	Benjamin H. Rotstein PhD, Michael S. Placzek PhD, Hema S. Krishnan PhD, Aleksandra Pekošak MPharm, Thomas Lee Collier PhD, Changning Wang PhD, Steven H. Liang PhD, Ethan S. Burstein PhD, Jacob M. Hooker PhD, Neil Vasdev PhD
Format:	Article
Language:	English
Published:	Hindawi - SAGE Publishing 2016-08-01
Series:	Molecular Imaging
Online Access:	https://doi.org/10.1177/1536012116663054

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spelling	doaj-725b84346084474882a75638559914f52021-04-02T17:48:47ZengHindawi - SAGE PublishingMolecular Imaging1536-01212016-08-011510.1177/153601211666305410.1177_1536012116663054Preclinical PET Neuroimaging of [C]BexaroteneBenjamin H. Rotstein PhD0Michael S. Placzek PhD1Hema S. Krishnan PhD2Aleksandra Pekošak MPharm3Thomas Lee Collier PhD4Changning Wang PhD5Steven H. Liang PhD6Ethan S. Burstein PhD7Jacob M. Hooker PhD8Neil Vasdev PhD9 Department of Radiology, Harvard Medical School, Boston, MA, USA Department of Psychiatry, McLean Imaging Center, McLean Hospital, Belmont, MA, USA Department of Radiology, Harvard Medical School, Boston, MA, USA Department of Radiology, Harvard Medical School, Boston, MA, USA Advion, Inc, Ithaca, NY, USA Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital, Charlestown, MA, USA Department of Radiology, Harvard Medical School, Boston, MA, USA ACADIA Pharmaceuticals, Inc, San Diego, CA, USA Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital, Charlestown, MA, USA Department of Radiology, Harvard Medical School, Boston, MA, USAActivation 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]CO 2 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.https://doi.org/10.1177/1536012116663054
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Benjamin H. Rotstein PhD Michael S. Placzek PhD Hema S. Krishnan PhD Aleksandra Pekošak MPharm Thomas Lee Collier PhD Changning Wang PhD Steven H. Liang PhD Ethan S. Burstein PhD Jacob M. Hooker PhD Neil Vasdev PhD
spellingShingle	Benjamin H. Rotstein PhD Michael S. Placzek PhD Hema S. Krishnan PhD Aleksandra Pekošak MPharm Thomas Lee Collier PhD Changning Wang PhD Steven H. Liang PhD Ethan S. Burstein PhD Jacob M. Hooker PhD Neil Vasdev PhD Preclinical PET Neuroimaging of [C]Bexarotene Molecular Imaging
author_facet	Benjamin H. Rotstein PhD Michael S. Placzek PhD Hema S. Krishnan PhD Aleksandra Pekošak MPharm Thomas Lee Collier PhD Changning Wang PhD Steven H. Liang PhD Ethan S. Burstein PhD Jacob M. Hooker PhD Neil Vasdev PhD
author_sort	Benjamin H. Rotstein PhD
title	Preclinical PET Neuroimaging of [C]Bexarotene
title_short	Preclinical PET Neuroimaging of [C]Bexarotene
title_full	Preclinical PET Neuroimaging of [C]Bexarotene
title_fullStr	Preclinical PET Neuroimaging of [C]Bexarotene
title_full_unstemmed	Preclinical PET Neuroimaging of [C]Bexarotene
title_sort	preclinical pet neuroimaging of [c]bexarotene
publisher	Hindawi - SAGE Publishing
series	Molecular Imaging
issn	1536-0121
publishDate	2016-08-01
description	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]CO 2 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.
url	https://doi.org/10.1177/1536012116663054
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Preclinical PET Neuroimaging of [C]Bexarotene

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