Synthesis and in vitro characterization of a P2X7 radioligand [I]TZ6019 and its response to neuroinflammation in a mouse model of Alzheimer disease.

The purinergic receptor P2X ligand-gated ion channel 7 (P2X7 receptor) is a promising imaging target to detect neuroinflammation. Herein, we report development of a potent iodinated radiotracer for P2X7 receptor, [I]TZ6019. The radiosynthesis of [I]TZ6019 was accomplished by allylic-tin precursor iodination using [I]NaI with good radiochemical yield of 85% and high radiochemical purity of > 99%.