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

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

doi:10.1186/s13550-017-0334-8

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

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

Research output: Contribution to journal › Comment/debate › peer-review

70 Scopus citations

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.

Original language	English (US)
Article number	84
Journal	EJNMMI Research
Volume	7
DOIs	https://doi.org/10.1186/s13550-017-0334-8
State	Published - 2017

Keywords

BP
Neuroinflammation
Radiometabolites
Single nucleotide polymorphism
Specific-to-non-displaceable ratio

ASJC Scopus subject areas

Radiology Nuclear Medicine and imaging

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10.1186/s13550-017-0334-8

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Fujita, M., Kobayashi, M., Ikawa, M., Gunn, R. N., Rabiner, E. A., Owen, D. R., Zoghbi, S. S., Haskali, M. B., Telu, S., Pike, V. W., & Innis, R. B. (2017). 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. EJNMMI Research, 7, Article 84. https://doi.org/10.1186/s13550-017-0334-8

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. / Fujita, Masahiro; Kobayashi, Masato; Ikawa, Masamichi et al.
In: EJNMMI Research, Vol. 7, 84, 2017.

Research output: Contribution to journal › Comment/debate › peer-review

Fujita, M, Kobayashi, M, Ikawa, M, Gunn, RN, Rabiner, EA, Owen, DR, Zoghbi, SS, Haskali, MB, Telu, S, Pike, VW & Innis, RB 2017, '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', EJNMMI Research, vol. 7, 84. https://doi.org/10.1186/s13550-017-0334-8

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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",

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, BPND (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 BPND 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 BPND. If inclusion of all three genotypes is important for study logistics, ER176 is the best of these four radioligands for studying neuroinflammation.",

keywords = "BP, Neuroinflammation, Radiometabolites, Single nucleotide polymorphism, Specific-to-non-displaceable ratio",

author = "Masahiro Fujita and Masato Kobayashi and Masamichi Ikawa and Gunn, {Roger N.} and Rabiner, {Eugenii A.} and Owen, {David R.} and Zoghbi, {Sami S.} and Haskali, {Mohamad B.} and Sanjay Telu and Pike, {Victor W.} and Innis, {Robert B.}",

note = "Funding Information: This study was funded by the Intramural Research Program of the National Institute of Mental Health, NIH: project numbers ZIAMH002852 and ZIAMH002793 under clinical protocols NCT02147392 [14-M-0117] and NCT02181582 [14-M-0141]). Publisher Copyright: {\textcopyright} 2017, The Author(s).",

year = "2017",

doi = "10.1186/s13550-017-0334-8",

language = "English (US)",

volume = "7",

journal = "EJNMMI Research",

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T1 - Comparison of four 11C-labeled PET ligands to quantify translocator protein 18 kDa (TSPO) in human brain

T2 - (R)-PK11195, PBR28, DPA-713, and ER176—based on recent publications that measured specific-to-non-displaceable ratios

AU - Fujita, Masahiro

AU - Kobayashi, Masato

AU - Ikawa, Masamichi

AU - Gunn, Roger N.

AU - Rabiner, Eugenii A.

AU - Owen, David R.

AU - Zoghbi, Sami S.

AU - Haskali, Mohamad B.

AU - Telu, Sanjay

AU - Pike, Victor W.

AU - Innis, Robert B.

N1 - Funding Information: This study was funded by the Intramural Research Program of the National Institute of Mental Health, NIH: project numbers ZIAMH002852 and ZIAMH002793 under clinical protocols NCT02147392 [14-M-0117] and NCT02181582 [14-M-0141]). Publisher Copyright: © 2017, The Author(s).

PY - 2017

Y1 - 2017

N2 - 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, BPND (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 BPND 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 BPND. If inclusion of all three genotypes is important for study logistics, ER176 is the best of these four radioligands for studying neuroinflammation.

AB - 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, BPND (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 BPND 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 BPND. If inclusion of all three genotypes is important for study logistics, ER176 is the best of these four radioligands for studying neuroinflammation.

KW - BP

KW - Neuroinflammation

KW - Radiometabolites

KW - Single nucleotide polymorphism

KW - Specific-to-non-displaceable ratio

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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