Preparation and evaluation of 3-[125I]iodo-4-aminophentermine as a brain perfusion imaging agent. Comparison with labeled phentermine derivatives |
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| Authors: | R N Hanson G S Jones L Franke H Kizuka D R Elmaleh |
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| Affiliation: | 1. Department of Medicinal Chemistry, College of Pharmacy and Allied Health Professions, Northeastern University, Boston, MA 02115,USA;2. Department of Radiology, The Children''s Hospital, Boston, MA 02115, USA;3. Physics Research Laboratory, Massachusetts General Hospital, Boston, MA 02114, USA;1. Invicro, Boston, MA, USA;2. GE Healthcare;3. Sir Peter Mansfield Imaging Centre, School of Medicine, University of Nottingham;4. MR Neurophysics and Translational Neuroscience, Queen Square UCL Institute of Neurology, University College London;5. Laboratory of FMRI Technology (LOFT), Mark & Mary Stevens Neuroimaging and Informatics Institute, Keck School of Medicine, University of Southern California (USC);6. Gold Standard Phantoms;1. National Nanotechnology Center, National Science and Technology Development Agency, Thailand Science Park, Pathum Thani, 12120, Thailand;2. Department of Radiology, Biomedical Research Imaging Center, and Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA;3. Department of Chemistry, School of Science, King Mongkut''s Institute of Technology Ladkrabang, Bangkok, 10520, Thailand;4. Integrated Applied Chemistry Research Unit, School of Science, King Mongkut''s Institute of Technology Ladkrabang, Bangkok, 10520, Thailand;5. School of Chemistry, Institute of Science, Suranaree University of Technology, Nakhon Ratchasima, 30000, Thailand;6. Department of Materials Engineering, Faculty of Engineering, Kasetsart University, Ladyao, Chatuchak, Bangkok 10900, Thailand;7. Department of Materials Science and Engineering, School of Molecular Science and Engineering, Vidyasirimedhi Institute of Science and Technology, Wangchan, Rayong, 21210, Thailand;1. National Organization for Drug Control and Research (NODCAR), Cairo, Egypt;2. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt;3. College of Pharmacy, Gulf Medical University, Ajman, United Arab Emirates;4. Egyptian Atomic Energy Authority (EAEA), Cairo, Egypt;1. Department of Neuroscience, Institute for Chinese Medicine, Heilongjiang University of Chinese Medicine, 24 Hepinglu, Xiangfang-qu, Harbin 150040, China;2. Research Center of Medical Science, Qiqihar Medical University, Jianhua District, Qiqihar 161006, China |
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| Abstract: | A radioiodinated derivative of the anorexinergic drug phentermine was synthesized and evaluated as a potential brain imaging agent. Stoichiometric iodination of the intermediate 4-aminophentermine (AmP) gave a mixture of mono and diiodo products, while the radioiodination at the no-carrier-added (NCA) level gave 73% isolated yield of the 3-[125I]iodo-4-aminophentermine with less than 2% of the diiodo derivative. The tissue distribution of the radiochemical in rats showed that it was readily extracted by the brain followed by relatively slow clearance from that organ. However, a comparison with other labeled phentermine derivatives indicated that the total brain uptake, retention and selectivity of the new agent were poorer, probably as a result of the presence of the 4-amino substituent. |
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