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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.
- Source :
-
Biological & pharmaceutical bulletin [Biol Pharm Bull] 2007 Nov; Vol. 30 (11), pp. 2226-8. - Publication Year :
- 2007
-
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.
- Subjects :
- Animals
Buffers
Drug Stability
Hydrogen-Ion Concentration
Indium Radioisotopes
Infusions, Intravenous
Kidney diagnostic imaging
Male
Mice
Mice, Inbred Strains
Pentetic Acid administration & dosage
Pentetic Acid analogs & derivatives
Pentetic Acid chemical synthesis
Pentetic Acid chemistry
Phosphates chemistry
Radionuclide Imaging
Radiopharmaceuticals blood
Radiopharmaceuticals chemistry
Tissue Distribution
1-Carboxyglutamic Acid chemistry
Carbon Dioxide chemistry
Glutamic Acid chemistry
Kidney metabolism
Phenylalanine chemistry
Radiopharmaceuticals pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0918-6158
- Volume :
- 30
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Biological & pharmaceutical bulletin
- Publication Type :
- Academic Journal
- Accession number :
- 17978507
- Full Text :
- https://doi.org/10.1248/bpb.30.2226