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Open Access 01-12-2017 | Commentary

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

Authors: Masahiro Fujita, Masato Kobayashi, Masamichi Ikawa, Roger N. Gunn, Eugenii A. Rabiner, David R. Owen, Sami S. Zoghbi, Mohamad B. Haskali, Sanjay Telu, Victor W. Pike, Robert B. Innis

Published in: EJNMMI Research | Issue 1/2017

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.

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11.

Ikawa M, Lohith TG, Shrestha S, Telu S, Zoghbi SS, Castellano S, et al. 11C-ER176, a Radioligand for 18-kDa Translocator protein, has adequate sensitivity to robustly image all three affinity genotypes in human brain. J Nucl Med. 2017;58:320–5. doi:10.2967/jnumed.116.178996.CrossRefPubMedPubMedCentral

Title: 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
Authors: Masahiro Fujita
Masato Kobayashi
Masamichi Ikawa
Roger N. Gunn
Eugenii A. Rabiner
David R. Owen
Sami S. Zoghbi
Mohamad B. Haskali
Sanjay Telu
Victor W. Pike
Robert B. Innis
Publication date: 01-12-2017
Publisher: Springer Berlin Heidelberg
Published in: EJNMMI Research / Issue 1/2017
Electronic ISSN: 2191-219X
DOI: https://doi.org/10.1186/s13550-017-0334-8

ACC 2024 Congress

Springer Medicine

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

ACC 2024 Congress

Springer Medicine

Abstract

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