99Tcm-labeled Glucose Metabolism Imaging Agents Based on in Vivo Copper-free Click Chemistry

Abstract

In order to develop an ideal 99Tcm-labeled glucose metabolism imaging agent, MAMA-conjugated azadibenzocyclooctyne derivative and four 2-azido glucose derivatives were synthesized. Two potential candidates (N3-DG-1 and N3-DG-2) were selected according to the in vitro kinetic study experiment. The 2-azido glucose derivatives were pretargeted in mice bearing S180 tumor, then 99Tcm-labeled MAMA-azadibenzocyclooctyne derivative was administrated to accomplish the in vivo copper-free click reaction and imaging of glucose metabolism. The biodistribution results showed that the tumor/blood and tumor/muscle ratios of N3-DG-2 were higher than those of N3-DG-1, indicating the combination of 99Tcm-labeled MAMA-azadibenzocyclooctyne derivative and N3-DG-2 was more suitable for glucose metabolism imaging.

Keywords

• glucose imaging
• in vivo copper-free click chemistry
• tumor
• technetium-99m