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Joseph, E.K.* ; Kunze, L.H.* ; Schaefer, R.* ; Palumbo, G.* ; Kugelmann, B.* ; Wagner, S.* ; Lammich, S.* ; Feederle, R. ; Willem, M.* ; Werner, R.A.* ; Brendel, M.* ; Lindner, S.*

Design, synthesis and preclinical evaluation of a brain-permeable PET tracer for P2Y12 receptor imaging in the brain.

J. Med. Chem. 68, 15543-15562 (2025)

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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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