Nuclear imaging of neuroinflammation: a comprehensive review of [C-11]PK11195 challengers

Fabien Chauveau; Herve Boutin; Nadja Van Camp; Frederic Dolle; Bertrand Tavitian

doi:10.1007/s00259-008-0908-9

Nuclear imaging of neuroinflammation: a comprehensive review of [C-11]PK11195 challengers

Fabien Chauveau, Herve Boutin, Nadja Van Camp, Frederic Dolle, Bertrand Tavitian^*

^*Corresponding author for this work

University of Groningen

Research output: Contribution to journal › Review article › peer-review

363 Citations (Scopus)

Abstract

Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [C-11]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radio-labelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [C-11]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.

Original language	English
Pages (from-to)	2304-2319
Number of pages	16
Journal	European Journal of Nuclear Medicine and Molecular Imaging
Volume	35
Issue number	12
DOIs	https://doi.org/10.1007/s00259-008-0908-9
Publication status	Published - Dec-2008

Keywords

Neuroinflammation
PET
[C-11]PK11195
Peripheral benzodiazepine receptor (PBR)
Translocator protein 18kDa (TSPO)
PERIPHERAL BENZODIAZEPINE-RECEPTOR
POSITRON-EMISSION-TOMOGRAPHY
IN-VIVO EVALUATION
CENTRAL-NERVOUS-SYSTEM
PROTEIN 18 KDA
EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS
EARLY ENDOTHELIAL ACTIVATION
OXIDE SYNTHASE INHIBITORS
FOCAL CEREBRAL-ISCHEMIA
MULTIPLE-SCLEROSIS

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title = "Nuclear imaging of neuroinflammation: a comprehensive review of [C-11]PK11195 challengers",

abstract = "Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [C-11]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radio-labelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [C-11]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.",

keywords = "Neuroinflammation, PET, [C-11]PK11195, Peripheral benzodiazepine receptor (PBR), Translocator protein 18kDa (TSPO), PERIPHERAL BENZODIAZEPINE-RECEPTOR, POSITRON-EMISSION-TOMOGRAPHY, IN-VIVO EVALUATION, CENTRAL-NERVOUS-SYSTEM, PROTEIN 18 KDA, EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS, EARLY ENDOTHELIAL ACTIVATION, OXIDE SYNTHASE INHIBITORS, FOCAL CEREBRAL-ISCHEMIA, MULTIPLE-SCLEROSIS",

author = "Fabien Chauveau and Herve Boutin and {Van Camp}, Nadja and Frederic Dolle and Bertrand Tavitian",

year = "2008",

month = dec,

doi = "10.1007/s00259-008-0908-9",

language = "English",

volume = "35",

pages = "2304--2319",

journal = "European Journal of Nuclear Medicine and Molecular Imaging",

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TY - JOUR

T1 - Nuclear imaging of neuroinflammation

T2 - a comprehensive review of [C-11]PK11195 challengers

AU - Chauveau, Fabien

AU - Boutin, Herve

AU - Van Camp, Nadja

AU - Dolle, Frederic

AU - Tavitian, Bertrand

PY - 2008/12

Y1 - 2008/12

N2 - Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [C-11]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radio-labelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [C-11]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.

AB - Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [C-11]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radio-labelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [C-11]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.

KW - Neuroinflammation

KW - PET

KW - [C-11]PK11195

KW - Peripheral benzodiazepine receptor (PBR)

KW - Translocator protein 18kDa (TSPO)

KW - PERIPHERAL BENZODIAZEPINE-RECEPTOR

KW - POSITRON-EMISSION-TOMOGRAPHY

KW - IN-VIVO EVALUATION

KW - CENTRAL-NERVOUS-SYSTEM

KW - PROTEIN 18 KDA

KW - EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS

KW - EARLY ENDOTHELIAL ACTIVATION

KW - OXIDE SYNTHASE INHIBITORS

KW - FOCAL CEREBRAL-ISCHEMIA

KW - MULTIPLE-SCLEROSIS

U2 - 10.1007/s00259-008-0908-9

DO - 10.1007/s00259-008-0908-9

M3 - Review article

SN - 1619-7070

VL - 35

SP - 2304

EP - 2319

JO - European Journal of Nuclear Medicine and Molecular Imaging

JF - European Journal of Nuclear Medicine and Molecular Imaging

IS - 12

ER -

Nuclear imaging of neuroinflammation: a comprehensive review of [C-11]PK11195 challengers

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