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The dopamine D 4  receptor has been shown to play important roles in some central nervous system pathologies. Specific radioligands for the D 4  receptor may be useful to understand the function of the D 4  receptor and its correlations with various disorders. 2-(3-(4-(4-[ 18 F]Fluorobenzyl)piperazin-1-yl)propyl)benzo[d]thiazole ([ 18 F] 4 ) was synthesized through a one-pot two-step procedure with total yield 18.6% (decay corrected). The specific activity of the radioligand was 112 GBq/μmol and its radiochemical purity was &gt;95.0%. Its affinity and selectivity for dopamine D 2 -like receptors were measured through  in vitro  receptor binding evaluation and the  K  i  value for the D 4  receptor was determined to be 2.9±0.2 nM, and its selectivity for the dopamine D 4  receptor is 709-fold versus D 2long  receptor, 823-fold versus D 3  receptor. The partition coefficient (Log D) of it was determined to be 2.6±0.1 through octanol-water partition experiment. The ligand presents desirable combination of lipophilicity, affinity and selectivity for the dopamine D 4  receptor. The results suggested that the radioligand shows promises for the  in vivo  study of the dopamine D 4  receptor.

radiochimica acta

Synthesis and  in vitro  evaluation of no-carrier-added 2-(3-(4-(4-[ 18 F]fluorobenzyl)piperazin-1-yl)propyl)benzo[d]thiazole, a potential dopamine D 4  receptor radioligand