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 Resjournal_title
EJNMMI researchauthors
Fujita M,Kobayashi M,Ikawa M,Gunn RN,Rabiner EA,Owen DR,Zoghbi SS,Haskali MB,Telu S,Pike VW,Innis RBdoi
10.1186/s13550-017-0334-8subject
Has Abstractpub_date
2017-10-16 00:00:00pages
84issue
1issn
2191-219Xpii
10.1186/s13550-017-0334-8journal_volume
7pub_type
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