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@ARTICLE{Olma:154935,
      author       = {Olma, Sebastian and Ermert, Johannes and Sihver, Wiebke and
                      Coenen, Heinrich Hubert},
      title        = {{S}ynthesis and first evaluation of [18{F}]fluorocyano- and
                      [18{F}]fluoronitro-quinoxalinedione as putative {AMPA}
                      receptor antagonists},
      journal      = {Medicinal chemistry},
      volume       = {11},
      number       = {1},
      issn         = {1573-4064},
      address      = {Bussum [u.a.]},
      publisher    = {Bentham Sc. Publ.},
      reportid     = {FZJ-2014-04146},
      pages        = {13 - 20},
      year         = {2015},
      abstract     = {Abstract:Derivatives of quinoxalinedione (QX) were chosen
                      as chemical lead for the development of new radioligands of
                      the AMPA receptor, since there are several examples of
                      QX-derivatives with high affinity. The radiosyntheses of the
                      new compounds 6-[18F]fluoro-7-nitro-QX ([18F]FNQX) and
                      7-[18F]fluoro-6-cyano-QX ([18F]FCQX) with radiochemical
                      yields of 8 ± 2 and 3 ± 2 $\%,$ respectively, as well as
                      the evaluation of their binding properties to the
                      AMPA-receptor were performed. A comparison of the Ki-values
                      of the new QX-derivatives FCQX and FNQX with
                      mono-substituted cyanoand nitro-QX shows negligibly small
                      differences of affinity (within the range of 1.4 to 5 µM),
                      but exhibits a tenfold lower affinity than derivatives with
                      two electron withdrawing groups like the
                      7-cyano-6-nitro-compound CNQX and the 6,7- dinitro compound
                      DNQX. Thus, with respect to the low affinity and a high
                      non-specific binding with in vitro and ex vivo
                      autoradiographic studies, the new compounds do not lend
                      themselves for in vivo imaging.- See more at:
                      http://www.eurekaselect.com/121871/article#sthash.JGpS3IVS.dpuf},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {573 - Neuroimaging (POF3-573) / 573 - Neuroimaging
                      (POF3-573)},
      pid          = {G:(DE-HGF)POF3-573 / G:(DE-HGF)POF3-573},
      typ          = {PUB:(DE-HGF)16},
      doi          = {10.2174/1573406410666140428151318},
      url          = {https://juser.fz-juelich.de/record/154935},
}