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Current Radiopharmaceuticals

Editor-in-Chief

ISSN (Print): 1874-4710
ISSN (Online): 1874-4729

Visualising Neuroinflammation in Post-Stroke Patients: A Comparative PET Study with the TSPO Molecular Imaging Biomarkers [11C]PK11195 and [11C]vinpocetine

Author(s): Balazs Gulyas, Miklos Toth, Adam Vas, Evgeni Shchukin, Konstantinos Kostulas, Jan Hillert and Christer Halldin

Volume 5, Issue 1, 2012

Page: [19 - 28] Pages: 10

DOI: 10.2174/1874471011205010019

Price: $65

Abstract

With the main objective of comparing the prospective diagnostic power of two 11C-labelled molecular imaging biomarkers with affinity for TSPO and used for the visualisation of activated microglia after a stroke, we measured with positron emission tomography (PET) in four post-stroke patients the regional brain uptake and binding potential of [11C]vinpocetine and [11C]PK11195. Percentage standard uptake values (%SUV) and binding potential (BPND) were used as outcome measures. The total peak brain uptake value and average global brain uptake value were higher for [11C]vinpocetine than for [11C]PK11195. The regional %SUV values were significantly higher for [11C]vinpocetine than for [11C]PK11195 in the hemispheres as well as in almost all standard brain regions. The %SUV values of [11C]vinpocetine were higher in the peri-infarct zone than in the ischaemic core, however, the difference did not prove to be significant. There was basically no difference in %SUV values between the ischaemic core and the peri-infarct zone for [11C]PK11195. The BPND values for [11C]vinpocetine were higher in all standard regions than those for [11C]PK11195, but the difference was not significant between them. The BPND values of [11C]vinpocetine were higher in the peri-infarct zone than in the ischaemic core, however, the difference did not prove to be significant. A comparative analysis of the two ligands indicates that [11C]vinpocetine shows a number of favourable characteristics over [11C]PK11195, but to demonstrate that it may serve as a prospective molecular imaging biomarker of microglia activation in post-stroke patients, further studies are required.

Keywords: (PBR)18 kD translocator protein (TSPO), molecular imaging biomarker, peripheral benzodiazepine receptor, [11C]PK11195, microglia, [11C]vipocetine, radioligand, Positron emission tomography (PET), stroke, peripheral benzodiazepine receptor (PBR)


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