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 | |
Publication status | Published - Nov 2007 |
Keywords
- In-diethylenetriaminepentaacetic acid-octreotide
- Kidney
- Negative charge
- Radio-accumulation
ASJC Scopus subject areas
- Pharmacology
- Pharmaceutical Science