Preclinical evaluation of (S)-[¹⁸F]GE387, a novel 18-kDa translocator protein (TSPO) PET radioligand with low binding sensitivity to human polymorphism rs6971.

ABSTRACT:

Purpose

Positron emission tomography (PET) studies with radioligands for 18-kDa translocator protein (TSPO) have been instrumental in increasing our understanding of the complex role neuroinflammation plays in disorders affecting the brain. However, (R)-[¹¹C]PK11195, the first and most widely used TSPO radioligand has limitations, while the next-generation TSPO radioligands have suffered from high interindividual variability in binding due to a genetic polymorphism in the TSPO gene (rs6971). Herein, we present the biological evaluation of the two enantiomers of [¹⁸F]GE387, which we have previously shown to have low sensitivity to this polymorphism.

Methods

Dynamic PET scans were conducted in male Wistar rats and female rhesus macaques to investigate the

SUBMITTER: Ramakrishnan NK 

PROVIDER: S-EPMC8712295 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature