Comparison of four (11)C-labeled PET ligands to quantify translocator protein 18 kDa (TSPO) in human brain: (R)-PK11195, PBR28, DPA-713, and ER176-based on recent publications that measured specific-to-non-displaceable ratios.
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Published version
Author(s)
Type
Journal Article
Abstract
Translocator protein (TSPO) is a biomarker for detecting neuroinflammation by PET. (11)C-(R)-PK11195 has been used to image TSPO since the 1980s. Here, we compared the utility of four (11)C-labeled ligands-(R)-PK11195, PBR28, DPA-713, and ER176-to quantify TSPO in healthy humans. For all of these ligands, BP ND (specific-to-non-displaceable ratio of distribution volumes) was measured by partially blocking specific binding with XNBD173 administration. In high-affinity binders, DPA-713 showed the highest BP ND of 7.3 followed by ER176 (4.2), PBR28 (1.2), and PK11195 (0.8). Only ER176 allows the inclusion of low-affinity binders because of little influence of radiometabolites and high BP ND. If inclusion of all three genotypes is important for study logistics, ER176 is the best of these four radioligands for studying neuroinflammation.
Date Issued
2017-10-16
Date Acceptance
2017-10-10
Citation
EJNMMI Research, 2017, 7 (1)
ISSN
2191-219X
Publisher
Springer
Journal / Book Title
EJNMMI Research
Volume
7
Issue
1
Copyright Statement
© The Author(s). 2017 Open Access This article is distributed under the terms of the Creative Commons Attribution 4.0
International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and
reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to
the Creative Commons license, and indicate if changes were made.
International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and
reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to
the Creative Commons license, and indicate if changes were made.
License URL
Identifier
PII: 10.1186/s13550-017-0334-8
Subjects
BP ND
Neuroinflammation
Radiometabolites
Single nucleotide polymorphism
Specific-to-non-displaceable ratio
Publication Status
Published online
Article Number
84