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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.

Aim: Replacement of the ecologically harmful solvent Freon 11 (CFCl(3)) by chloroform for the module-assisted preparation of 6-[(18)F]fluoro-L-DOPA based on the electrophilic radiofluorodestannylation of the precursor N-formyl-3,4-di-tert-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester., Materials, Methods: The TRACERlab Fx FDOPA module (GE Medical Systems) was used for the preparation of 6-[(18)F]fluoro-L-DOPA. Cyclotron-produced [(18)F]F(2) gas (5 GBq) was passed through a cooled solution (5 degrees C) of the stannyl precursor (45 mg) in CDCl(3) (10 ml). After the [(18)F]fluorination step, HCl (2 ml, 6 mol/l) was added to the solution. Then the reaction mixture was heated at 80 degrees C for 5 min under vacuum to evaporate the chloroform. The hydrolysis to remove the protecting groups was completed by heating the closed reactor at 130 degrees C for 8 min. After cooling to 20 degrees C the reaction mixture was purified by HPLC with two polymer-based RP columns (PRP-1, 7 microm, 10 x 250 mm, Hamilton) using a solution of AcOH/AcONa (pH 4.7) as eluent. The 6-[(18)F]fluoro-L-DOPA fraction was collected and sterile filtrated., Results: Three types of stabilised chloroform were tested for the radiofluorination of the precursor. Only by use of deuterochloroform stabilised with silver no significant losses of radioactivity were observed. Thus, 6-[(18)F]fluoro-L-DOPA purified by HPLC was obtained in decay-corrected radiochemical yields of 25+/-3%, ready for human use., Conclusion: CDCl(3) has proved to be a convenient solvent for the module-assisted preparation of 6-[(18)F]fluoro-L-DOPA. In this way the use of the polluting Freon 11 can be avoided.

Aim: Characterisation of the influence of different polymeric tube materials of a water target system, used for the production of 18F activity, on the specific activity of radiotracers., Material, Methods: Target water samples taken from different locations of the 18F water target system of a Cyclone 18/9 cyclotron, equipped with Teflon (PTFE) or polypropylene (PP) tubes, were analyzed for non-radioactive [19F]fluoride content. [19F]Fluoride content was measured by ion chromatography (IC20, Dinoex) with suppressed conductivity detection. Both the ion chromatographic results and the amount of 18F activity produced were used for the calculation of the specific activity (SA) of [18F]fluoride at the start of the labelling synthesis. To check these results, the SA of the labelled receptor ligand [18F]ZK811460 was also determined by using the different tubing materials., Results: Dose-exposed PTFE tubes of the target dispensing (loading) system were identified to be a major source of [19F]fluoride contamination., Conclusion: By replacing PTFE tubes of the target dispensing system with PP tubes, the content of 19F was reduced considerably resulting in an increase of SA of the radiotracer [18F]ZK811460 by factor of two.

It is well known that after application of radioactive complexes for tumour diagnosis or therapy, such as 67Ga-citrate or radiolanthanide complexes (167Tm- or 169Yb-nitrilotriacetate, -citrate, -alpha-hydroxyisobutyrate, 90Y-citrate, etc.) activity is accumulated not only in the tumour but also in other organs, above all liver and bone. This is the main obstacle to their medical use. Recently published results encouraged us to use ethylenediaminetetramethylene phosphonate (EDTMP) for the reduction of extratumoural liver activity. The results show that even small amounts of EDTMP (1-2 mg/kg BW) reduce the activity deposition in the liver by about one order of magnitude. EDTMP provoked elimination of activity from tumour, skeleton and other tissues but not to the same extent as from the liver. Tumor/liver activity ratios > 5 are achievable in this manner.