Abstract
AbstractStarting from the central benzodiazepine receptor (CBR) ligand CGS‐13767, we designed a series of imidazoquinazolinone derivatives acting as 18 kDa translocator protein (TSPO) ligands, and deprived of affinity for CBR. These compounds, as well as ligands of reference (Ro5‐4864, XBD173, SSR180575), were assessed for their ability to restore neurosteroidogenesis and energy production in SH‐SY5Y neuroblastoma cell lines expressing amyloid protein precursor (APP). Our results show the potential neuroprotective effect of TSPO ligands, but highlight a strong discrepancy in the active concentrations, nanomolar for ATP production while pregnenolone production is restored in the micromolar range.
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