作者: Stephen M. Moerlein , Joel S. Perlmutter
DOI: 10.1016/0304-3940(91)90149-N
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摘要: Abstract N-ω-[ 18 F]fluoroethylketanserin ([18F]FEK), an 18F-labeled analogue of the serotonin S2 antagonist ketanserin, was evaluated for use with positron emission tomography (PET). PET imaging a baboon brain following injection [18F]FEK indicated that fluorinated ligand rapidly localized in vivo within receptor-rich tissues ( frontal cortex cerebellum radioactivity ratio = 2.5 after 15 min), and selective localization retained as long 3 h post injection. Pretreatment unlabeled ketanserin (15 mg/kg, i.v.) 1 prior to completely abolished radiotracer, whereas regional cerebral blood flow, volume, free fraction arterial were unaltered. has several advantages compared previously used radiopharmaceuticals, may be excellent radioligand non-invasive evaluation binding vivo.