Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents |
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| Institution: | 1. Consortium for Safety Assessment Using Human iPS Cells (CSAHi), HEART Team, Tokyo, Japan;2. InvivoSciences, Inc., Madison, WI 53719, USA;3. Hamamatsu Photonics, K.K. Systems Division, Shizuoka 431-3196, Japan;4. Center for Supporting Drug Discovery and Life Science Research, Graduate School of Pharmaceutical Science, Osaka University, Osaka 565-0871, Japan.;5. FUJIFILM Wako Pure Chemical Corporation, Osaka 540-8605, Japan;6. Sumika Chemical Analysis Service, Ltd. (SCAS), Osaka 554-0022, Japan;7. Mitsubishi Tanabe Pharma Corporation, Kanagawa 251-8555, Japan;8. Daiichi Sankyo RD Novare Co., Ltd., Tokyo 134-8630, Japan;9. Axcelead Drug Discovery Partners, Inc., Kanagawa 251-0012, Japan;1. Faculty of Chemistry, Biotechnology and Food Science, Norwegian University of Life Sciences, NMBU, P.O. Box 5003, N-1432 Ås, Norway;2. TINE SA, P.O. Box 7, Kalbakken, N-0902 Oslo, Norway;1. Health and Environmental Sciences Institute, Washington, DC, USA;2. B2 Pathology Solutions LLC, Cary, NC, USA;3. Food and Drug Administration, Silver Spring, MD, USA;4. Comparative Coagulation Section, Department of Population Medicine and Diagnostic Sciences, Cornell University, Ithaca, NY, USA;5. Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD, USA;6. Toxicology & Safety Pharmacology, Cytokinetics, South San Francisco, CA, USA;7. Pathology, Lilly Research Laboratories, Indianapolis, IN, USA;8. Clyde Biosciences Ltd, Newhouse, UK;9. University of Glasgow, Scotland, UK;10. UCB Biopharma SRL, Development Science, Non-Clinical Safety Evaluation, Braine l''Alleud, Belgium |
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| Abstract: | Iodinated bivalent ligands 3 and 4 and a monovalent ligand 5 were prepared from the cardioselective β-antagonist, practolol. 125I-labeled 3, 4 and 5 were prepared by solid phase isotopic exchange reaction with carrier-free Na125I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that 125I-3 and 125I-4 were localized in the heart similarly to 125I-5 and the 125I]iodobenzoyl practolol (6) that was previously reported. Localization of 125I-3 and 125I-4, was more persistent in the heart than that of 125I-monovalent ligands 5 and 6. Heart-to-blood ratios of 125I-3 and 125I-4 were significantly lower than those of 125I-5 and 125I-6, due mainly to slow blood clearance rates of 125I-3 and 125I-4. |
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