Radiosynthesis and characterization of [¹⁸F]BS224: a next-generation TSPO PET ligand insensitive to the rs6971 polymorphism.

ABSTRACT:

Purpose

Translocator protein 18-kDa (TSPO) positron emission tomography (PET) is a valuable tool to detect neuroinflammed areas in a broad spectrum of neurodegenerative diseases. However, the clinical application of second-generation TSPO ligands as biomarkers is limited because of the presence of human rs6971 polymorphism that affects their binding. Here, we describe the ability of a new TSPO ligand, [¹⁸F]BS224, to identify abnormal TSPO expression in neuroinflammation independent of the rs6971 polymorphism.

Methods

An in vitro competitive inhibition assay of BS224 was conducted with [³H]PK 11195 using membrane proteins isolated from 293FT cells expressing TSPO-wild type (WT) or TSPO-mutant A147T (Mut), corresponding to a high-affinity binder (HAB) and

SUBMITTER: Lee SH 

PROVIDER: S-EPMC8712300 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature