Iodoethylspiperone,a new potential agent for exploration of central dopamine D2 receptors: Synthesis and preliminary in vivo study |
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| Institution: | 1. INSERM U316, Laboratoire de Biophysique Médicate, 2 bis Boulevard Tonnellé, 37032 Tours Cedex, France;2. CIS Industrie, BP 21, 91190 Gif sur Yvette, France;1. Department of Biochemistry, Tohoku University Graduate School of Medicine, Sendai 980-8575, Japan;2. Center for Regulatory Epigenome and Diseases, Tohoku University Graduate School of Medicine, Sendai 980-8575, Japan;3. Department of Chemistry and Biotechnology, Graduate School of Engineering, University of Tokyo, Tokyo 113-8656, Japan;1. Department of Molecular Biology, Science III, University of Geneva, 30 Quai Ernest-Ansermet, CH-1211 Geneva 4, Switzerland;2. European Molecular Biology Laboratory, Grenoble Outstation, 71 Avenue des Martyrs, 38042 Grenoble, France;1. Health Management Center, Sichuan Provincial People''s Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, Sichuan 610072, China;2. The Sichuan Provincial Key Laboratory for Human Disease Gene Study and Department of Laboratory Medicine, Center for Medical Genetics, Sichuan Provincial People''s Hospital, University of Electronic Science and Technology of China, Chengdu, Sichuan 610072, China;3. Henan Eye Institute, Henan Eye Hospital, People''s Hospital of Zhengzhou University, Henan Provincial People''s Hospital, Zhengzhou, Henan 450003, China;4. School of Medicine, University of Electronic Science and Technology of China, Chengdu, Sichuan 610054, China;5. Department of Hepatobiliary & Pancreatic Center, Sichuan Provincial People''s Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, Sichuan 610072, China;6. Department of Hepatobiliary & Pancreatic Center, Chinese Academy of Medical Sciences and Sichuan Translational Medicine Research Hospital, Chengdu, Sichuan 610072, China;7. Department of Urology, Sichuan Provincial People''s Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, Sichuan 610072, China;8. Research Unit for Blindness Prevention of Chinese Academy of Medical Sciences (2019RU026), Sichuan Academy of Medical Sciences and Sichuan Provincial People''s Hospital, Chengdu, Sichuan 610072 China;9. Key Laboratory of Tibetan Medicine Research, Chinese Academy of Sciences and Qinghai Provincial Key Laboratory of Tibetan Medicine Research, Northwest Institute of Plateau Biology, Xining, Qinghai 810008, China;1. Istituto Pasteur Italia, Fondazione Cenci-Bolognetti, Department of Molecular Medicine, Department of Excellence 2018–2022, Sapienza University of Rome, Viale Regina Elena 324, 00161 Rome, Italy;2. Oncohaematology Department, IRCCS Ospedale Pediatrico Bambino Gesù, Viale di San Paolo 15, 00146 Rome, Italy;3. Department of Drug Chemistry and Technologies, Department of Excellence 2018–2022, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy;1. School of Pharmacy, University of Wisconsin-Madison, Madison, WI 53705, USA;2. Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Liaoning 110042, China (current address);3. Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan (current address);4. Department of Chemistry, University of Wisconsin-Madison, Madison, WI 53706, USA |
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| Abstract: | We synthesized a new spiperone derivative: iodoethylspiperone (IES) to perform dopamine D2 receptor exploration by SPECT. IES was prepared from a precursor: tosylethylspiperone, and characterized by i.r. and 1H-NMR analyses. 125I]IES was obtained with 80% yield. In vivo biodistribution in rats showed a high and specific uptake in the striatum. The uptake ratio between the striatum and the cerebellum reached a maximum value 4 h after injection (10.05 ± 2.81). IES labeled with 123I should be a promising new agent to investigate D2 receptors in the living human brain. |
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