P2X7 PET Radioligand ¹⁸F-PTTP for Differentiation of Lung Tumor from Inflammation.

ABSTRACT: Site-specific imaging agents play a key role in tumor targeting, but only a few agents are currently available for inflammation targeting. Since the P2X7 receptor (P2X7R) is a promising molecular target for inflammation, we evaluated the potential value of the ¹⁸F-labeled tracer ¹⁸F-PTTP (5-{[2-Chloro-3-(trifluoromethyl)phenyl]carbonyl}-1-pyrimidin-2-yl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridin) for targeting P2X7Rs and thus differentiating inflammation from tumors. Methods: The radioligand ¹⁸F-PTTP was achieved by a 1-step ¹⁸F-trifluoromethylation reaction. The binding affinity of the ligand for P2X7R and its stability were evaluated in vitro. Blood pharmacokinetics tests and biodistribution studies were performed in vivo. Dynam

SUBMITTER: Fu Z 

PROVIDER: S-EPMC6604685 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature