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Development of a Novel 68 Ga-Dextran Carboxylate Derivative for Blood Pool Imaging Publisher



Gholipour N1, 2 ; Akhlaghi M3 ; Mokhtari Kheirabadi A3 ; Fasihi Ramandi M4 ; Farashahi A5 ; Beiki D3 ; Jalilian AR6
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Authors Affiliations
  1. 1. Chemical Injuries Research Center, Systems Biology and Poisonings Institute, Baqiyatallah University of Medical Sciences, Tehran, Iran
  2. 2. Faculty of Pharmacy, Baqiyatallah University of Medical Sciences, Tehran, Iran
  3. 3. Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Molecular Biology Research Center, System Biology and Poisonings Institute, Baqiyatallah University of Medical Sciences, Tehran, Iran
  5. 5. Tehran Heart Center, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Tehran University of Medical Sciences, Research Center for Nuclear Medicine, Shariati Hospital, North Kargar Ave., Tehran, Iran

Source: Radiochimica Acta Published:2019


Abstract

To develop a possible PET blood pool imaging agent, a series 68 Ga-dextran carboxylate derivatives were prepared. Dextran carboxylates with different degree of oxidations (DO) were prepared through stepwise dextran oxidation using NaIO 4 and CH 3 COOOH. The products were characterized by FT-IR and GPC, followed by solubility and toxicity tests on Hella cells (viability=98.6, 97.4 and 95.6% for 3 dextran carboxylates with DOs: 8.3, 24.6 and 39.8%, respectively. The products were labeled with 68 Ga (radiochemical purity>98%; ITLC) followed by stability tests in final solution as well as in presence of cycteine and human serum. Two stable tracers (DOs; 24.6 and 39.8%) were adminstered intravenously into wild type rat tail vein separately demonstrating suitable retention in circulation as expected from blood pool imaging agents. Liver and spleen also contained activities. The major excretion was through urinary pathway esp. for derivative with DO. 39.8%. Unlike 68 Ga-dextran, lungs showed lower uptake. The dextran carboxylate with the highest 39.8% showed the best characteristics for a blood pool agent, though more studies including PET imaging in larger mammals are required. © 2019 Walter de Gruyter GmbH, Berlin/Boston.
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