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@ARTICLE{Hoffmann:894996,
      author       = {Hoffmann, Chris and Evcüman, Sibel and Neumaier, Felix and
                      Zlatopolskiy, Boris D. and Humpert, Swen and Bier, Dirk and
                      Holschbach, Marcus and Schulze, Annette and Endepols, Heike
                      and Neumaier, Bernd},
      title        = {[18{F}]{ALX}5406: {A} {B}rain-{P}enetrating {P}rodrug for
                      {G}ly{T}1-{S}pecific {PET} {I}maging},
      journal      = {ACS chemical neuroscience},
      volume       = {12},
      number       = {18},
      issn         = {1948-7193},
      address      = {Washington, DC},
      publisher    = {ACS Publ.},
      reportid     = {FZJ-2021-03517},
      pages        = {3335 - 3346},
      year         = {2021},
      abstract     = {Selective inhibition of glycine transporter 1 (GlyT1) has
                      emerged as a potential approach to alleviate
                      N-methyl-D-aspartate receptor (NMDAR) hypofunction in
                      patients with schizophrenia and cognitive decline. ALX5407
                      is a potent and selective inhibitor of GlyT1 derived from
                      the metabolic intermediate sarcosine (N-methylglycine) that
                      showed antipsychotic potential in a number of animal models.
                      Whereas clinical application of ALX5407 is limited by
                      adverse effects on motor performance and
                      respiratoryfunction, a suitably radiolabeled drug could
                      represent a promising PET tracer for the visualization of
                      GlyT1 in the brain. Herein, [18F]ALX5407 and the
                      corresponding methyl ester, [18F]ALX5406, were prepared by
                      alcoholenhanced copper mediated radiofluorination and
                      studied in vitro in rat brain slices and in vivo in normal
                      rats. [18F]ALX5407 demonstrated accumulation consistent with
                      the distribution of GlyT1 in in vitro autoradiographic
                      studies but no brain uptake in μPET experiments in naıv̈
                      e rats. In contrast, the methyl ester [18F]ALX5406 rapidly
                      entered the brain and was enzymatically transformed into
                      [18F]ALX5407, resulting in a regional accumulation pattern
                      consistent with GlyT1 specific binding. We conclude that
                      [18F]ALX5406 is a promising and easily accessible PET probe
                      for preclinical in vivo imaging of GlyT1 in the brain.},
      cin          = {INM-5},
      ddc          = {540},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {34449193},
      UT           = {WOS:000697282400006},
      doi          = {10.1021/acschemneuro.1c00284},
      url          = {https://juser.fz-juelich.de/record/894996},
}