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@ARTICLE{Joseph:280959,
      author       = {Joseph, Emanuel and Kunze, Lea H and Schaefer, Rebecca and
                      Palumbo, Giovanna and Kugelmann, Benjamin and Wagner,
                      Stephan and Lammich, Sven and Feederle, Regina and Willem,
                      Michael and Werner, Rudolf A and Brendel, Matthias and
                      Lindner, Simon},
      title        = {{D}esign, {S}ynthesis and {P}reclinical {E}valuation of a
                      {B}rain-{P}ermeable {PET} {T}racer for {P}2{Y}12 {R}eceptor
                      {I}maging in the {B}rain.},
      journal      = {Journal of medicinal chemistry},
      volume       = {68},
      number       = {15},
      issn         = {0095-9065},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DZNE-2025-01041},
      pages        = {15543 - 15562},
      year         = {2025},
      abstract     = {Microglia, the innate immune cells of the central nervous
                      system (CNS), act as first responders to brain injury. Their
                      ability to switch between different neuroprotective and
                      neurotoxic phenotypes, plays a central role in maintaining
                      brain homeostasis. Recently, the P2Y12 receptor (P2Y12R) has
                      been identified as a promising molecular biomarker for
                      microglia activity, as its expression level is dependent on
                      microglia phenotype and function. P2Y12R positron emission
                      tomography (PET) might be a valuable diagnostic tool,
                      however, tracers with sufficient brain retention have not
                      been reported so far. Herein, we report a brain-permeable
                      P2Y12R PET tracer for in vivo imaging of P2Y12R-positive
                      microglia. Nicotinate [18F]12 exhibited nanomolar affinity
                      and specificity for the target receptor and showed a reduced
                      uptake in microglia-depleted (PLX) mice, in comparison to WT
                      and Trem2 knockout (Trem2-/-) mice. Ex vivo
                      immunohistochemistry (IHC) and PET data revealed a strong
                      correlation between microglia abundance, P2Y12R expression
                      levels and tracer uptake.},
      cin          = {AG Herms / AG Feederle / AG Haass},
      ddc          = {610},
      cid          = {I:(DE-2719)1110001 / I:(DE-2719)1140004 /
                      I:(DE-2719)1110007},
      pnm          = {352 - Disease Mechanisms (POF4-352) / 899 - ohne Topic
                      (POF4-899)},
      pid          = {G:(DE-HGF)POF4-352 / G:(DE-HGF)POF4-899},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:40713021},
      pmc          = {pmc:PMC12362594},
      doi          = {10.1021/acs.jmedchem.5c00457},
      url          = {https://pub.dzne.de/record/280959},
}