Synthesis and in vivo biodistribution of BPA-Gd-DTPA complex as a potential MRI contrast carrier for neutron capture therapy

Kazunori Takahashi, Hiroyuki Nakamura, Shozo Furumoto, Kazuyoshi Yamamoto, Hiroshi Fukuda, Akira Matsumura, Yoshinori Yamamoto

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)

Abstract

p-Boronophenylalanine (BPA) conjugated Gd-DTPA complex (3) was synthesized from the active methyne compound 6, the allylic carbonate 7, and BPA by the palladium-catalyzed allylation reaction followed by the DCC coupling reaction. The in vivo biodistribution of complex 3 was evaluated by prompt gamma-ray analysis and α-autoradiography using the tumor-bearing rats. High accumulation of gadolinium was observed in the kidney and the %ID values were 0.17 and 0.088 at 20 and 60 min after injection of 3, respectively. The accumulation was also observed in the tumor and the %ID values were 0.010 and 0.0025 at 20 and 60 min after injection, respectively. The visualization experiment of boron distribution in the tumor-bearing rat by α-autoradiography indicates that boron was accumulated in the tumor and the intestines at 20 min after injection.

Original languageEnglish
Pages (from-to)735-743
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number3
DOIs
Publication statusPublished - 2005 Feb 1

Keywords

  • Biodistribution
  • Gadolinium complex
  • Gd-DTPA complex
  • MRI
  • Neutron capture therapy
  • p-Boronophenylalanine

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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