18F-labelled CCR1-receptor antagonist is not suitable for imaging of Alzheimer's disease

Nuklearmedizin. 2012;51(6):239-43. doi: 10.3413/Nukmed-0457-12-01. Epub 2012 Jun 11.

Abstract

Diagnosis of Alzheimer's disease (AD) with positron emission tomography (PET) using 18F-fluorodeoxyglucose (FDG) relies on typical alterations of brain glucose metabolism which are, however, not disease specific. Amyloid-β imaging has not entered clinical routine yet. Post mortem histological specimen of brain tissue from AD patients revealed enhanced expression of the chemotactic cytocine receptor 1 (CCR1).

Participants, methods: CCR1-antagonist ZK811460 was labeled with fluorine-18 to explore its possible use as specific diagnostic tool in AD. Tracer characterization comprising PET imaging of brain and metabolite analysis was performed in AD patients and controls.

Results: Neither qualitative evaluation nor quantitative compartment analysis of PET data did show any enhanced binding of the 18F-labeled CCR1-antagonist in the brain of AD patients or controls.

Conclusion: 18F-ZK811460 did not fulfill the expectation as diagnostic tracer in PET imaging of AD.

Publication types

  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Alzheimer Disease / diagnostic imaging*
  • Alzheimer Disease / metabolism
  • Female
  • Fluorine Radioisotopes* / chemistry
  • Humans
  • Isotope Labeling
  • Male
  • Phenylurea Compounds* / chemical synthesis
  • Piperazines* / chemical synthesis
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis
  • Receptors, CCR1 / antagonists & inhibitors*
  • Reproducibility of Results
  • Sensitivity and Specificity

Substances

  • Fluorine Radioisotopes
  • Phenylurea Compounds
  • Piperazines
  • Radiopharmaceuticals
  • Receptors, CCR1
  • ZK811460