Effect of carboxyl-group of D-glutamic acid or γ-carboxy-D-glutamic acid as N-terminal amino acid of 111In-diethylenetriaminepentaacetic acid-octreotide on accumulation of radioactivity in kidney

Hiromichi Akizawa, Madoka Saito, Ikuko Tsukamoto, Tatsuya Ohkura, Takaya Shimizu, Youji Kitamura, Masaki Mifune, Yutaka Saito, Yasushi Arano, Hideo Saji

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To establish a strategy for developing 111In- diethylenetriaminepentaacetic acid (111In-DTPA)-octreotide, a diagnostic radiopharmaceutical agent for tumors, with reduced non-specific renal radio-accumulation, the compounds having D-glutamic acid (Glu) or γ-carboxy-D-glutamic acid (carboxy-Glu) as the N-terminal amino acid were examined for in vivo radio-distribution. Compounds carrying Glu and carboxy-Glu containing one and two negative charges, respectively, showed lower renal radio-accumulation than that carrying D-phenylalanine. It was revealed that the introduction of a negative charge reduces the renal radio-accumulation independently from the number of negative charges. The present result can be a clue for the development of 111In-DTPA-octreotides with reduced the renal radio-accumulation.

Original languageEnglish
Pages (from-to)2226-2228
Number of pages3
JournalBiological and Pharmaceutical Bulletin
Issue number11
Publication statusPublished - Nov 2007



  • In-diethylenetriaminepentaacetic acid-octreotide
  • Kidney
  • Negative charge
  • Radio-accumulation

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

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