Comparison of four 11C-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.

Abstract:

:Translocator protein (TSPO) is a biomarker for detecting neuroinflammation by PET. 11C-(R)-PK11195 has been used to image TSPO since the 1980s. Here, we compared the utility of four 11C-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.

journal_name

EJNMMI Res

journal_title

EJNMMI research

authors

Fujita M,Kobayashi M,Ikawa M,Gunn RN,Rabiner EA,Owen DR,Zoghbi SS,Haskali MB,Telu S,Pike VW,Innis RB

doi

10.1186/s13550-017-0334-8

subject

Has Abstract

pub_date

2017-10-16 00:00:00

pages

84

issue

1

issn

2191-219X

pii

10.1186/s13550-017-0334-8

journal_volume

7

pub_type

信件
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