Effect of carboxyl-group of D-glutamic acid or gamma-carboxy-D-glutamic acid as N-terminal amino acid of (111)in-diethylenetriaminepentaacetic acid-octreotide on accumulation of radioactivity in kidney.

Abstract	To establish a strategy for developing (111)In-diethylenetriaminepentaacetic acid ((111)In-DTPA)-octreotide, a diagnostic radiopharmaceutical agent for tumors, with reduced non-specific renal radio-accumulation, the compounds having D-glutamic acid (Glu) or gamma-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 (111)In-DTPA-octreotides with reduced the renal radio-accumulation.
Authors	Hiromichi Akizawa, Madoka Saito, Ikuko Tsukamoto, Tatsuya Ohkura, Takaya Shimizu, Youji Kitamura, Masaki Mifune, Yutaka Saito, Yasushi Arano, Hideo Saji
Journal	Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 30 Issue 11 Pg. 2226-8 (Nov 2007) ISSN: 0918-6158 [Print] Japan
PMID	17978507 (Publication Type: Journal Article)
Chemical References	(111)indium-DTPA-D-phe octreoide Buffers Indium Radioisotopes Phosphates Radiopharmaceuticals Carbon Dioxide carboxyl radical Glutamic Acid Phenylalanine 1-Carboxyglutamic Acid Pentetic Acid
Topics	1-Carboxyglutamic Acid (chemistry) Animals Buffers Carbon Dioxide (chemistry) Drug Stability Glutamic Acid (chemistry) Hydrogen-Ion Concentration Indium Radioisotopes Infusions, Intravenous Kidney (diagnostic imaging, metabolism) Male Mice Mice, Inbred Strains Pentetic Acid (administration & dosage, analogs & derivatives, chemical synthesis, chemistry) Phenylalanine (chemistry) Phosphates (chemistry) Radionuclide Imaging Radiopharmaceuticals (blood, chemistry, pharmacokinetics) Tissue Distribution

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