Visualising neuroinflammation in post-stroke patients: a comparative PET study with the TSPO molecular imaging biomarkers [11C]PK11195 and [11C]vinpocetine

Curr Radiopharm. 2012 Jan;5(1):19-28. doi: 10.2174/1874471011205010019.

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.

Publication types

  • Comparative Study

MeSH terms

  • Aged
  • Binding Sites
  • Biomarkers / metabolism
  • Carbon Radioisotopes
  • Encephalitis / diagnostic imaging*
  • Encephalitis / metabolism
  • Humans
  • Isoquinolines* / chemical synthesis
  • Isoquinolines* / chemistry
  • Male
  • Middle Aged
  • Molecular Imaging
  • Positron-Emission Tomography / methods
  • Radiopharmaceuticals* / chemical synthesis
  • Radiopharmaceuticals* / chemistry
  • Receptors, GABA / metabolism*
  • Stroke / diagnostic imaging*
  • Vinca Alkaloids* / chemical synthesis
  • Vinca Alkaloids* / chemistry
  • Young Adult

Substances

  • Biomarkers
  • Carbon Radioisotopes
  • Isoquinolines
  • Radiopharmaceuticals
  • Receptors, GABA
  • TSPO protein, human
  • Vinca Alkaloids
  • vinpocetine
  • PK 11195