文章基本信息

标题：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
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作者：Hiromichi Akizawa ; Madoka Saito ; Ikuko Tsukamoto 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2007
卷号：30
期号：11
页码：2226-2228
DOI：10.1248/bpb.30.2226
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：111In-diethylenetriaminepentaacetic acid-octreotide;radio-accumulation;negative charge;kidney