Design, synthesis and evaluation in an LPS rodent model of neuroinflammation of a novel ¹⁸F-labelled PET tracer targeting P2X7.

ABSTRACT:

Background

The P2X7 receptor has been shown to play a fundamental role in the initiation and sustenance of the inflammatory cascade. The development of a novel fluorine-18 PET tracer superior and with a longer half-life to those currently available is a promising step towards harnessing the therapeutic and diagnostic potential offered by this target. Inspired by the known antagonist A-804598, the present study outlines the design via molecular docking, synthesis and biological evaluation of the novel P2X7 tracer [¹⁸F]EFB. The tracer was radiolabelled via a three-step procedure, in vitro binding assessed in P2X7-transfected HEK293 and in B16 cells by calcium influx assays and an initial preclinical evaluation was performed in a lipopolysaccharide (LPS)-injected rat model

SUBMITTER: Fantoni ER 

PROVIDER: S-EPMC5378566 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature