Development and evaluation of [¹¹C]DPA-813 and [¹⁸F]DPA-814: novel TSPO PET tracers insensitive to human single nucleotide polymorphism rs6971.

ABSTRACT:

Purpose

The translocator protein 18 kDa (TSPO) is a widely used marker for imaging neuroinflammation via Positron Emission Tomography (PET). However, the vast majority of reported TSPO PET tracers display low binding affinity to a common isoform of human TSPO (rs6971; A147T), making them unsuitable for universal use in the general population. In this study, we have developed and preclinically validated two novel tracers designed to image TSPO in patients of all genotypes.

Methods

Novel analogues of known TSPO ligands were synthesised, evaluated for TSPO binding affinity in vitro (membranes prepared from transfected HEK-293T cells expressing wild-type (WT) or A147T TSPO) and radiolabelled with carbon-11 or fluorine-18. They were evaluated in situ (autoradiography on genotyped

SUBMITTER: Beaino W 

PROVIDER: S-EPMC12119672 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature