PMID- 27553293
OWN - NLM
STAT- MEDLINE
DCOM- 20170605
LR  - 20181202
IS  - 1536-0121 (Electronic)
IS  - 1535-3508 (Print)
IS  - 1535-3508 (Linking)
VI  - 15
DP  - 2016
TI  - Preclinical PET Neuroimaging of [11C]Bexarotene.
LID - 10.1177/1536012116663054 [doi]
LID - 1536012116663054
AB  - 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.
CI  - (c) The Author(s) 2016.
FAU - Rotstein, Benjamin H
AU  - Rotstein BH
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA vasdev.neil@mgh.harvard.edu 
      benjamin.rotstein@uottawa.ca.
FAU - Placzek, Michael S
AU  - Placzek MS
AD  - Department of Radiology, Harvard Medical School, Boston, MA, USA Athinoula A. 
      Martinos Center for Biomedical Imaging, Massachusetts General Hospital, 
      Charlestown, MA, USA Department of Psychiatry, McLean Imaging Center, McLean 
      Hospital, Belmont, MA, USA.
FAU - Krishnan, Hema S
AU  - Krishnan HS
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA.
FAU - Pekosak, Aleksandra
AU  - Pekosak A
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA.
FAU - Collier, Thomas Lee
AU  - Collier TL
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA Advion, Inc, Ithaca, NY, USA.
FAU - Wang, Changning
AU  - Wang C
AD  - Department of Radiology, Harvard Medical School, Boston, MA, USA Athinoula A. 
      Martinos Center for Biomedical Imaging, Massachusetts General Hospital, 
      Charlestown, MA, USA.
FAU - Liang, Steven H
AU  - Liang SH
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA.
FAU - Burstein, Ethan S
AU  - Burstein ES
AD  - ACADIA Pharmaceuticals, Inc, San Diego, CA, USA.
FAU - Hooker, Jacob M
AU  - Hooker JM
AD  - Department of Radiology, Harvard Medical School, Boston, MA, USA Athinoula A. 
      Martinos Center for Biomedical Imaging, Massachusetts General Hospital, 
      Charlestown, MA, USA.
FAU - Vasdev, Neil
AU  - Vasdev N
AD  - Division of Nuclear Medicine and Molecular Imaging, Gordon Center for Molecular 
      Imaging, Massachusetts General Hospital, Boston, MA, USA Department of Radiology, 
      Harvard Medical School, Boston, MA, USA vasdev.neil@mgh.harvard.edu 
      benjamin.rotstein@uottawa.ca.
LA  - eng
GR  - S10 RR022976/RR/NCRR NIH HHS/United States
GR  - S10 RR029495/RR/NCRR NIH HHS/United States
GR  - K01 DA038000/DA/NIDA NIH HHS/United States
GR  - S10 RR026666/RR/NCRR NIH HHS/United States
GR  - S10 RR023385/RR/NCRR NIH HHS/United States
PT  - Journal Article
DEP - 20160823
PL  - England
TA  - Mol Imaging
JT  - Molecular imaging
JID - 101120118
RN  - 0 (Carbon Radioisotopes)
RN  - 0 (Radiopharmaceuticals)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Tetrahydronaphthalenes)
RN  - A61RXM4375 (Bexarotene)
SB  - IM
MH  - Animals
MH  - Bexarotene
MH  - Brain/*diagnostic imaging/metabolism
MH  - Carbon Radioisotopes/chemistry
MH  - Male
MH  - Neuroimaging/*methods
MH  - Positron-Emission Tomography
MH  - Primates
MH  - Radiopharmaceuticals/chemistry
MH  - Rats
MH  - Retinoid X Receptors/agonists/metabolism
MH  - Tetrahydronaphthalenes/chemistry/*pharmacology
PMC - PMC5011434
MID - NIHMS813289
OTO - NOTNLM
OT  - bexarotene
OT  - carbon-11
OT  - neuroimaging
OT  - positron emission tomography
OT  - retinoid X receptor
COIS- Declaration of Conflicting Interests: The author(s) declared no potential 
      conflicts of interest with respect to the research, authorship, and/or 
      publication of this article.
EDAT- 2016/08/25 06:00
MHDA- 2017/06/06 06:00
PMCR- 2016/08/23
CRDT- 2016/08/25 06:00
PHST- 2016/03/31 00:00 [received]
PHST- 2016/07/06 00:00 [accepted]
PHST- 2016/08/25 06:00 [entrez]
PHST- 2016/08/25 06:00 [pubmed]
PHST- 2017/06/06 06:00 [medline]
PHST- 2016/08/23 00:00 [pmc-release]
AID - 15/0/1536012116663054 [pii]
AID - 10.1177_1536012116663054 [pii]
AID - 10.1177/1536012116663054 [doi]
PST - epublish
SO  - Mol Imaging. 2016 Aug 23;15:1536012116663054. doi: 10.1177/1536012116663054. 
      Print 2016.