Home > Publications Database > Design, Synthesis and Preclinical Evaluation of a Brain-Permeable PET Tracer for P2Y12 Receptor Imaging in the Brain. > print

001     280959
005     20250921002008.0
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100 1 _ |a Joseph, Emanuel
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245 _ _ |a Design, Synthesis and Preclinical Evaluation of a Brain-Permeable PET Tracer for P2Y12 Receptor Imaging in the Brain.
260 _ _ |a Washington, DC
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520 _ _ |a 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.
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700 1 _ |a Kunze, Lea H
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700 1 _ |a Schaefer, Rebecca
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700 1 _ |a Palumbo, Giovanna
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700 1 _ |a Kugelmann, Benjamin
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700 1 _ |a Wagner, Stephan
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700 1 _ |a Lammich, Sven
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700 1 _ |a Feederle, Regina
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700 1 _ |a Willem, Michael
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700 1 _ |a Werner, Rudolf A
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700 1 _ |a Brendel, Matthias
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700 1 _ |a Lindner, Simon
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773 _ _ |a 10.1021/acs.jmedchem.5c00457
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