Synthesis and biological evaluation of 18F-labelled dopamine D3 receptor selective ligands

Bioorganic & Medicinal Chemistry Letters(2022)

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摘要
•Three novel 18F-labelled phenylpiperazine-like radioligands were synthesized as potential novel PET probes for D3R imaging.•A simple, rapid and efficient 18F-labelling method was developed.•Radioligand [18F]8b could quickly penetrate the blood-brain barrier and showed high affinity and selectivity to the dopamine D3 receptor.•Radioligand [18F]8b showed its good in vivo stability with negligible defluorination.
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关键词
Dopamine D3 receptor,Positron emission tomography (PET),18F-labelling,Biodistribution study
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