3-N-(2-[18F]-fluoroethyl)-spiperone: a novel ligand for cerebral dopamine receptor studies with pet |
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| Authors: | H H Coenen P Laufer G St?cklin K Wienhard G Pawlik H G B?cher-Schwarz W D Heiss |
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| Institution: | 1. Institut für Chemie 1 (Nuklearchemie), Kernforschungsanlage Jülich GmbH, D-5170 Jülich, FRG;1. Pediatric Intensive Care Unit, CHU Sainte-Justine, Montreal, Canada;2. University of Montreal, Montreal, Canada;3. University of Ottawa, Children''s Hospital of Eastern Ontario, Ottawa, Canada;1. Department of Forensic Medicine, Medical College of Soochow University, Suzhou, Jiangsu 215123, China;2. Shanghai Key Laboratory of Forensic Medicine, Institute of Forensic Sciences, Ministry of Justice, Shanghai, China;3. Department of Epidemiology, Medical College of Soochow University, Suzhou, China;4. Faculty of Forensic Medicine, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou, Guangdong 510080, China;1. Applied Modelling and Computation Group, Department of Earth Science and Engineering, Imperial College London, SW7 2AZ, UK;2. Division of Engineering Science, School of Engineering and Material Science, Queen Mary University of London, E1 4NS, UK;1. Research Group of Analytical Chemistry and Life Sciences, Department of Analytical Chemistry, Campus of Fuentenueva, University of Granada, E-18071 Granada, Spain;2. Department of Microbiology, Campus Cartuja, University of Granada, E-18071 Granada, Spain |
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| Abstract: | 3-N-(2-18F]-fluoroethyl)-spiperone ( 18F]-FESP) was synthesized at high specific activity by condensation with 2-18F]-fluoroethyltosylate (35 TBq/mmol). In vivo binding studies in baboons by positron emission tomography exhibited regio-selective uptake in the striatum which was saturable with the cold ligand and prevented by pretreatment with (+)-butaclamol. The pharmacokinetic behaviour, i.e. the absolute uptake in tissue and the striatum-to-cerebellum ratio, was very similar to that of methylspiperone. Analysis of the radioactivity in mouse brain after administration of 18F]-FESP indicated a high in-vivo stability (greater than 90% after 210 min in the striatum). Comparative distribution studies of other N-fluoroalkylspiperones in mice suggest that FESP and the N-fluoropropyl analogue are the most potent D2 receptor ligands. |
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