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


CONCLUSIONS
18F-ZK811460 did not fulfill the expectation as diagnostic tracer in PET imaging of AD.
Klinik und Poliklinik für Nuklearmedizin, Universitätsklinikum Carl Gustav Carus, Fetscherstraße 74, 01307 Dresden, Germany. b.beuthien@hzdr.de
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Beuthien-Baumann
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Holthoff
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Mäding
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Bergmann
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Pawelke
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Holl
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von Kummer
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Kotzerke
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van den Hoff
D000368:Aged; D000544:Alzheimer Disease / Q000000981:diagnostic imaging* / Q000378:metabolism; D005260:Female; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D010671:Phenylurea Compounds / Q000138:chemical synthesis; D010879:Piperazines / Q000138:chemical synthesis; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D054389:Receptors, CCR1 / Q000037:antagonists & inhibitors*; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity
D005462:Fluorine Radioisotopes; D010671:Phenylurea Compounds; D010879:Piperazines; D019275:Radiopharmaceuticals; D054389:Receptors, CCR1; C582096:ZK811460