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标题：Effect of Carboxylation of N-Terminal Phenylalanine of 111In-DTPA (Diethylenetriaminepentaacetic Acid)-Octreotide on Accumulation of Radioactivity in Kidney
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作者：Hiromichi Akizawa ; Hirokazu Takimoto ; Madoka Saito 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：2004
卷号：27
期号：2
页码：271-272
DOI：10.1248/bpb.27.271
出版社：The Pharmaceutical Society of Japan
摘要：For purpose of reducing renal accumulation of radioactivity of a known radiopharmaceutical agent, i.e. , ¹¹¹In-DTPA (diethylenetriaminepentaacetic acid)- D -Phe¹-octreotide, a derivative in which p -carboxy- L -phenylalanine is substituted for D -Phe¹ was synthesized. Biodistribution study of the resultant compound having carboxy-substituted L -Phe¹ revealed that the renal accumulation was significantly lower than that of control compound having unsubstituted L -Phe¹, demonstrating that the presence of negative charge on the N-terminal amino acid of octreotide is effective to reduce the renal accumulation. This effect can be attributed to the reduction of lipophilicity and also the repulsive force arisen from the negative charge of renal brush border membrane.
关键词：111In-DTPA-octreotide;p-carboxy-phenylalanine;renal accumulation