Two binding sites for [ H]PBR28 in human brain: implications for TSPO PET imaging of neuroinflammation

[11C]PBR28, a radioligand targeting the translocator protein (TSPO), does not produce a specific binding signal in approximately 14% of healthy volunteers. This phenomenon has not been reported for [11C]PK11195, another TSPO radioligand. We measured the specific binding signals with [3H]PK11195 and...

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Bibliographic Details
Published in:Journal of cerebral blood flow and metabolism 2010-09, Vol.30 (9), p.1608-1618
Main Authors: Owen, David R, Howell, Owain W, Tang, Sac-Pham, Wells, Lisa A, Bennacef, Idriss, Bergstrom, Mats, Gunn, Roger N, Rabiner, Eugenii A, Wilkins, Martin R, Reynolds, Richard, Matthews, Paul M, Parker, Christine A
Format: Article
Language:English
Subjects:
Acetamides - metabolism
Adult
Aged
Aged, 80 and over
Autoradiography
Binding Sites
Binding, Competitive - drug effects
Biological and medical sciences
Brain - diagnostic imaging
Brain Chemistry
Carbon Radioisotopes
Female
Humans
Immunohistochemistry
Investigative techniques, diagnostic techniques (general aspects)
Isoquinolines
Male
Medical sciences
Membranes - diagnostic imaging
Membranes - metabolism
Middle Aged
Nerve Tissue Proteins - analysis
Nerve Tissue Proteins - metabolism
Nervous system
Neuritis - diagnostic imaging
Neurology
Original
Positron-Emission Tomography
Pyridines - metabolism
Radioligand Assay
Receptors, GABA - metabolism
Tissue Banks
Ultrasonic investigative techniques
Vascular diseases and vascular malformations of the nervous system
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Summary:[11C]PBR28, a radioligand targeting the translocator protein (TSPO), does not produce a specific binding signal in approximately 14% of healthy volunteers. This phenomenon has not been reported for [11C]PK11195, another TSPO radioligand. We measured the specific binding signals with [3H]PK11195 and [3H]PBR28 in brain tissue from 22 donors. Overall, 23% of the samples did not generate a visually detectable specific autoradiographic signal with [3H]PBR28, although all samples showed [3H]PK11195 binding. There was a marked reduction in the affinity of [3H]PBR28 for TSPO in samples with no visible [3H]PBR28 autoradiographic signal (Ki=188±15.6 nmol/L), relative to those showing normal signal (Ki=3.4±0.5 nmol/L, P
ISSN:0271-678X
1559-7016
DOI:10.1038/jcbfm.2010.63