Technetium-99m spiperone dithiocarbamate: A potential radiopharmaceutical for dopamine receptor imaging with SPECT |
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| Affiliation: | 1. Cellular and Neural Engineering Group, Institute for Science and Technology in Medicine, Keele University, Keele, Staffordshire, United Kingdom;2. Department of Surgery, Drexel University College of Medicine, Philadelphia, PA, USA;3. Department of Pharmacology and Physiology, Drexel University College of Medicine, Philadelphia, PA, USA;4. Department of Chemical Engineering, School of Engineering and Physical Sciences, Heriot-Watt University, Edinburgh, United Kingdom;1. Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, NE, Atlanta, GA 30322, USA;2. Center for Systems Imaging, Emory University, Wesley Woods Health Center, 1841 Clifton Road, NE, Atlanta, GA 30329, USA;1. Department of Radiology and Imaging Sciences, University of Utah, 729 Arapeen Drive, Salt Lake City, UT, United States;2. School of Public Health and Health Sciences, University of Massachusetts Amherst, Amherst, Massachusetts;3. Division of Epidemiology, University of Utah, 295 Chipeta Way, Salt Lake City, UT, United States;4. Division of Vascular Surgery, University of Utah, 30 N 1900 E, Salt Lake City, UT, United States;5. Division of Cardiovascular Medicine, University of Utah, 30 N 1900 E, Salt Lake City, UT, United States;6. Verily Life Sciences, 355 Main St, Cambridge, MA, United States;2. Department of Physiology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan;3. Department of Cell Biology, National Cerebral and Cardiovascular Center Research Institute, Osaka, Japan;4. Department of Cardiovascular Surgery, National Cerebral and Cardiovascular Center, Osaka, Japan;5. Department of Molecular Innovation in Lipidology, National Cerebral and Cardiovascular Center Research Institute, Osaka, Japan |
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| Abstract: | Spiperone dithiocarbamate (SPDC) was prepared by reacting spiperone with carbon disulfide followed by sodium hydroxide. SPDC was labelled with 99mTc by reduction of pertechnetate with formamidine sulfinic acid or sodium dithionite at alkaline pH, resulting in ∼40% incorporation of 99mTc. The lipophilic complex was conveniently isolated at high specific activity and high radiochemical purity by extraction into dichloromethane, which was then evaporated and the residue was redissolved in a 1:3 mixture of ethanol and saline containing 0.1 mg/mL gentisic acid. Biodistribution studies following i.p. injection in rats showed low uptake of radioactivity in the brain, but striatum/cortex and striatum/cerebellum ratios were reduced by pretreatment with haloperidol. This agent may allow imaging of dopamine D-2 receptors using single-photon emission computed tomography (SPECT). |
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