Synthesis and Biological Evaluation of (S)-Amino-2-methyl-4-[(76)Br]bromo-3-(E)-butenoic Acid (BrVAIB) for Brain Tumor Imaging.

Academic Article

Abstract

  • The novel compound, (S)-amino-2-methyl-4-[(76)Br]bromo-3-(E)-butenoic acid (BrVAIB, [(76)Br]5), was characterized against the known system A tracer, IVAIB ([(123)I]8). [(76)Br]5 was prepared in a 51% ± 19% radiochemical yield with high radiochemical purity (≥98%). The biological properties of [(76)Br]5 were compared with those of [(123)I]8. Results showed that [(76)Br]5 undergoes mixed amino acid transport by system A and system L transport, while [(123)I]8 had less uptake by system L. [(76)Br]5 demonstrated higher uptake than [(123)I]8 in DBT tumors 1 h after injection (3.7 ± 0.4% ID/g vs 1.5 ± 0.3% ID/g) and also showed higher uptake vs [(123)I]8 in normal brain. Small animal PET studies with [(76)Br]5 demonstrated good tumor visualization of intracranial DBTs up to 24 h with clearance from normal tissues. These results indicate that [(76)Br]5 is a promising PET tracer for brain tumor imaging and lead compound for a mixed system A and system L transport substrate.
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    Keywords

  • Alanine, Amination, Animals, Biological Transport, Brain, Brain Neoplasms, Bromine Radioisotopes, Crotonates, Glioma, Iodine Radioisotopes, Male, Mice, Inbred BALB C, Positron-Emission Tomography, Radiopharmaceuticals, Tissue Distribution
  • Digital Object Identifier (doi)

    Authorlist

  • Burkemper JL; Huang C; Li A; Yuan L; Rich K; McConathy J; Lapi SE
  • Start Page

  • 8542
  • End Page

  • 8552
  • Volume

  • 58
  • Issue

  • 21