Synthesis and Characterization of Fluorine-18-Labeled N-(4-Chloro-3-((fluoromethyl-d₂)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain.

ABSTRACT: We have synthesized and characterized [¹⁸F]-N-(4-chloro-3-((fluoromethyl-d₂)thio)phenyl)-picolinamide ([¹⁸F]15) as a potential ligand for the positron emission tomography (PET) imaging of mGluR4 in the brain. Radioligand [¹⁸F]15 displays central nervous system drug-like properties, including mGluR4 affinity, potent mGluR4 PAM activity, and selectivity against other mGluRs, as well as sufficient metabolic stability. Radiosynthesis was carried out in two steps. The radiochemical yield of [¹⁸F]15 was 11.6 ± 2.9% (n = 7, decay corrected) with a purity of 99% and a molar activity of 84.1 ± 11.8 GBq/μmol. Ex vivo biodistribution studies showed reversible binding of [¹⁸F]15 in all in

SUBMITTER: Wang J 

PROVIDER: S-EPMC7261135 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature