In Vivo Evaluation of 6 Analogs of ¹¹C-ER176 as Candidate ¹⁸F-Labeled Radioligands for 18-kDa Translocator Protein.

ABSTRACT: Because of its excellent ratio of specific to nondisplaceable uptake, the radioligand ¹¹C-ER176 can successfully image 18-kDa translocator protein (TSPO), a biomarker of inflammation, in the human brain and accurately quantify target density in homozygous low-affinity binders. Our laboratory sought to develop an ¹⁸F-labeled TSPO PET radioligand based on ER176 with the potential for broader distribution. This study used generic ¹¹C labeling and in vivo performance in the monkey brain to select the most promising among 6 fluorine-containing analogs of ER176 for subsequent labeling with longer-lived ¹⁸F. Methods: Six fluorine-containing analogs of ER176-3 fluoro and 3 trifluoromethyl isomers-were synthesized and labeled by ¹¹C meth

SUBMITTER: Lee JH 

PROVIDER: S-EPMC9364345 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature