Synthesis, radiolabeling and preliminary in vivo evaluation of [ 18F]FE-PE2I, a new probe for the dopamine transporter

• Published in: Bioorganic & medicinal chemistry letters Vol. 19; no. 16; pp. 4843 - 4845
• Main Authors: Schou, Magnus, Steiger, Carsten, Varrone, Andrea, Guilloteau, Denis, Halldin, Christer
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.08.2009; Elsevier
• Subjects: Animals; Biological and medical sciences; Brain - metabolism; Contrast media. Radiopharmaceuticals; Dopamine Plasma Membrane Transport Proteins - antagonists & inhibitors; Dopamine Plasma Membrane Transport Proteins - metabolism; Dopamine transporter; Fluorine Radioisotopes - chemistry; Haplorhini; Humans; Isotope Labeling; Kinetics; Medical sciences; Nortropanes - chemical synthesis; Nortropanes - chemistry; Nortropanes - pharmacology; PE2I; PET; Pharmacology. Drug treatments; Positron-Emission Tomography; Radioligand; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - pharmacology; Rats; Tropane; Dopamine transporter; PE2I; Radioligand; Tropane; PET; Fluorine 18; Ligand; Monkey; Central nervous system; Tissue; Membrane transport; Primates; Chemical synthesis; Dopamine; Fluorine Isotopes; Radiolabelling; Rodentia; Catecholamine; In vivo; Vertebrata; Mammalia; Animal; Biogenic amine; Distribution; Neurotransmitter

The synthesis, radiosynthesis and preliminary PET evaluation of [18F]6 ( K i = 17 nM) is reported. A new dopamine transporter (DAT) ligand, ( E)- N-(3-iodoprop-2-enyl)-2β-carbofluoroethoxy-3β-(4′-methyl-phenyl) nortropane (FE-PE2I, 6), derived from PE2I ( 1), was prepared and found to be a potent in...