Nuclear Medicine and Biology
Volume 35, Issue 3 , Pages 305-314 , April 2008

Radiosynthesis and initial evaluation of [18F]-FEPPA for PET imaging of peripheral benzodiazepine receptors

  • Alan A. Wilson

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • Department of Psychiatry, University of Toronto, Toronto, Ontario, Canada M5T 1R8
    • Corresponding Author InformationCorresponding author. PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8. Tel.: +1 416 979 4286; fax: +1 416 979 4656.
    • ,
  • Armando Garcia

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • ,
  • Jun Parkes

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • ,
  • Patrick McCormick

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • Institute of Medical Science, University of Toronto, Toronto, Ontario, Canada M5S 1A8
    • ,
  • Karin A. Stephenson

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • ,
  • Sylvain Houle

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • Department of Psychiatry, University of Toronto, Toronto, Ontario, Canada M5T 1R8
    • ,
  • Neil Vasdev

      Affiliations

    • PET Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada M5T 1R8
    • Department of Psychiatry, University of Toronto, Toronto, Ontario, Canada M5T 1R8

Received 9 November 2007 ,Revised 13 December 2007 ,Accepted 17 December 2007.

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  41. Rigorous kinetic modeling is required for a proper assessment of the displacement of [18F]-FEPPA and [11C]-PRB28 by the cold FEPPA or PRB28, however the following arguement can be made to support specific displacement of these two radioligands from the brain PBRs. Although a stable equilibrium state between brain and plasma was not achieved during our studies, the region to plasma ratios do remain proportional to the distribution volumes of the two compounds. With increasing plasma levels, the brain to blood ratios should not be affected under tracer conditions. In our experiments, this ratio actually decreased with increased blocking doses while the plasma levels increased due to blocking of the peripheral PBR binding sites. One can infer from these lower ratios that the specific brain binding to PBRs is significantly reduced in the blocked conditions.
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PII: S0969-8051(08)00007-3

doi: 10.1016/j.nucmedbio.2007.12.009

Nuclear Medicine and Biology
Volume 35, Issue 3 , Pages 305-314 , April 2008

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