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@ARTICLE{Elmenhorst:134640,
      author       = {Elmenhorst, David and Kroll, Tina and Wedekind, Franziska
                      and Weißhaupt, Angela and Beer, Simone and Bauer, Andreas},
      title        = {{I}n {V}ivo {K}inetic and {S}teady-{S}tate {Q}uantification
                      of 18{F}-{CPFPX} {B}inding to {R}at {C}erebral {A}1
                      {A}denosine {R}eceptors: {V}alidation by {D}isplacement and
                      {A}utoradiographic {E}xperiments},
      journal      = {Journal of nuclear medicine},
      volume       = {54},
      number       = {8},
      issn         = {0161-5505},
      address      = {Reston, Va.},
      publisher    = {SNM84042},
      reportid     = {FZJ-2013-02757},
      pages        = {1411-1419},
      year         = {2013},
      abstract     = {In vivo imaging of the A1 adenosine receptor (A1AR) using
                      (18)F-8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine
                      ((18)F-CPFPX) and PET has become an important tool for
                      studying physiologic and pathologic states of the human
                      brain. However, dedicated experimental settings for
                      small-animal studies are still lacking. The aim of the
                      present study was therefore to develop and evaluate suitable
                      pharmacokinetic models for the quantification of the
                      cerebral A1AR in high-resolution PET. METHODS: On a
                      dedicated animal PET scanner, 15 rats underwent (18)F-CPFPX
                      PET scans of 120-min duration. In all animals, arterial
                      blood samples were drawn and corrected for metabolites. The
                      radioligand was injected either as a bolus or as a bolus
                      plus constant infusion. For the definition of unspecific
                      binding, the A1AR selective antagonist
                      8-cyclopentyl-1,3-dipropylxanthine (DPCPX) was applied.
                      After PET, the brains of 9 animals were dissected and in
                      vitro saturation binding was performed using high-resolution
                      (3)H-DPCPX autoradiography. RESULTS: The kinetics of
                      (18)F-CPFPX were well described by either compartmental or
                      noncompartmental models based on arterial input function.
                      The resulting distribution volume ratio correlated with a
                      low bias toward identity with the binding potential derived
                      from a reference region (olfactory bulb) approach.
                      Furthermore, PET quantification correlated significantly
                      with autoradiographic in vitro data. Blockade of the A1AR
                      with DPCPX identified specific binding of about $45\%$ in
                      the reference region olfactory bulb. CONCLUSION: The present
                      study provides evidence that (18)F-CPFPX PET based on a
                      reference tissue approach can be performed quantitatively in
                      rodents in selected applications. Specific binding in the
                      reference region needs careful consideration for
                      quantitative investigations.},
      cin          = {INM-2 / ZEA-2},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-2-20090406 / I:(DE-Juel1)ZEA-2-20090406},
      pnm          = {333 - Pathophysiological Mechanisms of Neurological and
                      Psychiatric Diseases (POF2-333)},
      pid          = {G:(DE-HGF)POF2-333},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:23740103},
      UT           = {WOS:000322692400055},
      doi          = {10.2967/jnumed.112.115576},
      url          = {https://juser.fz-juelich.de/record/134640},
}