Evaluation of positron-emitting SCH 23390 analogs as tracers for CNS dopamine D1 receptors |
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| Affiliation: | 1. Department of Nuclear Medicine, University of Leipzig, Liebigstraße 18, 04103 Leipzig, Germany;2. Integrated Research and Treatment Centre (IFB) Adiposity Diseases, University of Leipzig, Philipp-Rosenthal-Straße 27, 04103 Leipzig, Germany;3. Department of Psychiatry, University of Leipzig, Semmelweisstraße 10, 04103 Leipzig, Germany;4. Max-Planck-Institute for Human Cognitive and Brain Sciences, Stephanstraße 1a, 04103 Leipzig, Germany;5. Electronic Systems (ZEA-2), Central Institute for Engineering, Electronics and Analytics, Research Centre Juelich, Wilhelm-Johnen-Straße, 52428 Juelich, Germany;6. ABX Advanced Biochemical Compounds GmbH, Heinrich-Gläser-Straße 10, 01454 Radeberg, Germany;7. Clinical Trial Centre Leipzig, Härtelstraße 16–18, 04107 Leipzig, Germany;8. Helmholtz-Zentrum Dresden-Rossendorf, Research Site Leipzig, Permoserstraße 15, 04318 Leipzig, Germany;1. Pharmacology, Merck &Co. Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA;2. Genetics and Pharmacogenomics, Merck & Co. Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA;3. Cardiometabolic Disease, Merck & Co. Inc., 2000 Galloping Hill Rd., Kenilworth, NJ 07033, USA;4. Biostatistics, Merck & Co. Inc., 351 North Sumneytown Pike, North Wales, PA 19454, USA;5. Biostatistics, Merck & Co. Inc., 126 E. Lincoln Avenue, PO Box 2000, Rahway, NJ 07065, USA |
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| Abstract: | Two positron-emitting analogs of SCH 23390, one labelled with 75Br (or 76Br) and another with 11C, were evaluated as potential PET tracers for central dopamine D1 receptors. In vivo studies were performed to assess the time course of the biodistribution of these tracers in mice and to determine whether dopamine receptors mediated their uptake in the brains of these animals. Results show that indeed cerebral uptake was consistent with dopamine receptor innervation, i.e. uptake and clearance was regionally consistent with the target receptors and that specific uptake was saturable. Because of the relatively rapid pharmacokinetics of this drug, 11C-labelled SCH 23390 would be best suited for PET imaging although the metabolism of this compound needs to be further examined. |
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