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The level of the translocator protein (TSPO) increases dramatically in microglial cells when the cells are activated in response to neuronal injury and insult. The radiotracer [(18) F]GE-180 binds selectively and with high affinity to TSPO and can therefore be used to measure neuroinflammation in a variety of disease states. An optimized, automated synthesis of [(18) F]GE-180 has been developed for the GE FASTlab™ synthesizer. The entire process takes place on the single-use cassette. The radiolabelling is performed by nucleophilic fluorination of the S- enantiomer mesylate precursor. The crude product is purified post-radiolabelling using two solid-phase extraction cartridges integrated on the cassette. Experimental design and multivariate data analysis were used to assess the robustness, and critical steps were optimized with respect to efficacy and quality. The average radiochemical yield is 48% (RSD 6%, non-decay corrected), and the synthesis time including purification is approximately 43 min. The radiochemical purity is ≥95% for radioactive concentration ≤1100 MBq/mL. The total amount of precursor-related chemical impurities is 1-2 µg/mL. The use of solid-phase extraction purification results in a robust GMP compliant process with a product of high chemical and radiochemical purity and consistent performance across positron emission tomography (PET) centers.

No abstract

Developing racemic radiotracers, as for racemic therapeutics, is a considerable challenge due to differences of the enantiomers in pharmacokinetics, efficacy and potential toxicity. We have shown that the enantiomers of the promising racemic PET ligand [(18)F]GE-180 do not share identical performance, with S-[(18)F]GE-180 demonstrating higher TSPO affinity, higher brain uptake and better retention to the high TSPO-expressing lungs. Furthermore, S-[(18)F]GE-180 has also been shown to be enantiomerically stable in vivo, with no observed conversation of the eutomer to the distomer. As a single enantiomer, S-[(18)F]GE-180 retains the beneficial characteristics of the racemate and is a promising imaging agent for imaging neuroinflammation in vivo.

Environment Canada's Emergencies Engineering Division is spearheading a program in conjunction with the Canadian General Standards Board that would see the development of a certification and listing program in addition to a national standard for the testing of sorbent materials. Funding for this program is provided by Environment Canada (EC), Canadian Coast Guard (CCG), Marine Spill Response Corporation (MSRC), U.S. Coast Guard (USCG), and U.S. Minerals Management Service (MMS). The test methods are based upon those defined by the American Society for Testing and Materials and previous test methods developed by Environment Canada for our series of reports entitled Selection Criteria and Laboratory Evaluation of Oil Spill Sorbents. This series, which was started in 1975, encompasses a number of commercially available oil spill sorbents tested with different petroleum products and hydrocarbon solvents. The testing program will categorize the sorbents according to their operating characteristics. The main categories are oil spills on water, oil spills on land, and industrial use. The characteristics we will be evaluating with the new test protocols include initial and maximum sorption capacities, water pickup, buoyancy, reuse potential, retention profile, disintegration (material integrity), and ease of application and retrieval. In the near future we plan to incorporate changes to the test that would involve increasing our list of test liquids to encompass spills in an industrial setting, in addition to testing sorbent booms and addressing the disposal problem.