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

doi:10.1248/bpb.30.2226

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

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

Abstract

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 language	English
Pages (from-to)	2226-2228
Number of pages	3
Journal	Biological and Pharmaceutical Bulletin
Volume	30
Issue number	11
DOIs	https://doi.org/10.1248/bpb.30.2226
Publication status	Published - Nov 2007

Keywords

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

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

Access to Document

10.1248/bpb.30.2226

Cite this

Akizawa, H., Saito, M., Tsukamoto, I., Ohkura, T., Shimizu, T., Kitamura, Y., Mifune, M., Saito, Y., Arano, Y., & Saji, H. (2007). 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. Biological and Pharmaceutical Bulletin, 30(11), 2226-2228. https://doi.org/10.1248/bpb.30.2226

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. / Akizawa, Hiromichi; Saito, Madoka; Tsukamoto, Ikuko et al.

In: Biological and Pharmaceutical Bulletin, Vol. 30, No. 11, 11.2007, p. 2226-2228.

Research output: Contribution to journal › Article › peer-review

Akizawa, H, Saito, M, Tsukamoto, I, Ohkura, T, Shimizu, T, Kitamura, Y, Mifune, M, Saito, Y, Arano, Y & Saji, H 2007, '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', Biological and Pharmaceutical Bulletin, vol. 30, no. 11, pp. 2226-2228. https://doi.org/10.1248/bpb.30.2226

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abstract = "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.",

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