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Bioorg Med Chem ; 23(4): 729-34, 2015 Feb 15.
Article in English | MEDLINE | ID: mdl-25596169

ABSTRACT

A novel PET probe, 6-[(11)C]methyl-m-tyrosine ([(11)C]6MemTyr), was developed for quantitative imaging of presynaptic dopamine (DA) synthesis in the living brain using positron emission tomography (PET). This probe was evaluated by comparison with conventional 6-[(18)F]fluoro-l-dopa ([(18)F]FDOPA). [(11)C]6MemTyr was labeled using rapid Pd(0)-mediated C-[(11)C]methylation with [(11)C]methyl iodide. The synthesis time was only 35min, and its radiochemical yield was 76%, with radiochemical purity of >99%. PET measurements indicated that [(11)C]6MemTyr could image presynaptic DA synthesis in the striatum of living monkey brain, providing much higher contrast between the striatum and the cerebellum than that with [(18)F]FDOPA.


Subject(s)
Brain/diagnostic imaging , Brain/metabolism , Carbon Radioisotopes/analysis , Dopamine/analysis , Methyltyrosines/analysis , Positron-Emission Tomography/methods , Animals , Carbon Radioisotopes/metabolism , Corpus Striatum/diagnostic imaging , Corpus Striatum/metabolism , Dopamine/metabolism , Fluorine Radioisotopes/analysis , Fluorine Radioisotopes/metabolism , Levodopa/analysis , Macaca fascicularis , Male , Methyltyrosines/chemical synthesis , Methyltyrosines/metabolism , Radiopharmaceuticals/analysis , Radiopharmaceuticals/chemical synthesis , Radiopharmaceuticals/metabolism
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