Evaluation of 3-[18F]Fluoro-α-fluoromethyl-p-tyrosine as a tracer for striatal tyrosine hydroxylase activity

O. T. Dejesus, D. Murali, R. Kitchen, C. Endres, T. R. Oakes, S. E. Shelton, L. Freund, D. Houser, H. Uno, J. E. Holden, R. J. Nickles

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3-[18F]Fluoro-α-fluoromethyl-p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not significantly alter the ability of FMPT to act as a TH-activated l-aromatic amino acid decarboxylase (l-AAAD) inhibitor. These studies further showed that 3-F-FMPT-induced l-AAAD inhibition was dose-dependent. Furthermore, striatal homogenates prepared from rats pretreated with the potent TH inhibitor α-methyl-p-tyrosine was found to have diminished 3-F-FMPT-induced l-AAAD inhibition. However, despite these promising in vitro results, the biodistribution of this compound in mice showed low brain uptake and fast clearance through the kidneys. A PET study using a Rhesus monkey injected with 3-[18F]F-FMPT confirmed the results obtained in mice, i.e. negligible brain uptake but high localization in the bladder. We conclude that 3-[18F]F-FMPT would not be useful as a tracer for cerebral TH activity.

Original languageEnglish (US)
Pages (from-to)663-667
Number of pages5
JournalNuclear Medicine and Biology
Issue number4
StatePublished - May 1994

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research


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