Investigation of Radiopharmaceuticals for Pancreatic Imaging : Accumulation of Amines in the Pancreas

  • 佐治 英郎
    Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
  • 久下 裕司
    Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
  • 間賀田 泰寛
    Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
  • 藤林 靖久
    Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
  • 横山 陽
    Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University

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To develop radiopharmaceuticals for pancreatic imaging, radioiodinated ethyl benzene derivatives contaning various functional groups (amino, carboxyl, and methyl groups) were synthesized and the effects of these functional groups were compared in vitro and in vivo. At 2 min after intravenous injection, the amino derivative, 2-(4-iodophenyl)-N, N-dimethyl ethylamine, displayed about twice the pancreatic uptake and a more than 8-fold higher pancreas/liver ratio than the carboxyl and methyl derivatives. This high and selective in vivo accumulation on the amino derivative in the pancreas was well supported by in vitro studies on the uptake by pancreatic tissue slices. The mechanism promoting pancreatic accumulation of radiopharmaceuticals with an amino group is also discussed.

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