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@ARTICLE{Kreft:824539,
      author       = {Kreft, Sabrina and Bier, Dirk and Holschbach, Marcus and
                      Schulze, Annette and Coenen, Heinrich Hubert},
      title        = {{N}ew potent {A}1 adenosine receptor radioligands for
                      positron emission tomography},
      journal      = {Nuclear medicine and biology},
      volume       = {44},
      issn         = {0969-8051},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {FZJ-2016-07111},
      pages        = {69 - 77},
      year         = {2017},
      abstract     = {8-Cyclopentyl-3-(3-[18F]fluoropropyl)-1-propylxanthine
                      ([18F]CPFPX) is meanwhile an accepted receptor ligand to
                      examine the A1 adenosine receptor (A1AR) in humans by
                      positron emission tomography (PET). A major drawback of this
                      compound is its rather fast metabolic degradation in
                      vivo.Therefore two new xanthine derivatives, namely
                      8-cyclobutyl-1-cyclopropymethyl-3-(3-fluoropropyl)xanthine
                      (CBCPM; 5) and
                      1-cyclopropylmethyl-3-(3-fluoropropyl)-8-(1-methylcyclobutyl)xanthine
                      (CPMMCB; 6) were designed and synthesized as potential
                      alternatives to CPFPX. In membrane binding studies both
                      compounds showed nanomolar affinity for the A1AR. In vitro
                      autoradiographic studies of [18F]5 and [18F]6, using rat
                      brain slices, showed the expected accumulation in regions
                      known to have a high adenosine A1 receptor expression while
                      exhibiting the necessary low unspecific binding. However, in
                      vitro metabolite studies using human liver microsomes
                      revealed a comparable metabolic degradation rate for both
                      new xanthine derivatives and CPFPX.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000390836100006},
      doi          = {10.1016/j.nucmedbio.2016.09.004},
      url          = {https://juser.fz-juelich.de/record/824539},
}