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Synthesis and preliminary evaluation of Tc-99m-labeled somatostatin analog (RC-160) using "3+1" mixed ligand approach.
- Source :
-
Nuclear medicine and biology [Nucl Med Biol] 2001 Apr; Vol. 28 (3), pp. 225-33. - Publication Year :
- 2001
-
Abstract
- The success of (111)In-pentetreotide as a cancer-imaging agent has given impetus to the search for other peptide-based radiopharmaceuticals. The labeling with Tc-99m has become even more attractive because of the ready availability and near ideal physical properties. Additionally, the kinetics of the peptide-receptor interactions favors the radiolabeling with technetium-99m. A somatostatin analog RC-160 has been labeled with Tc-99m using the "3+1" mixed ligand approach utilizing the NNS/S coordination sites. The ternary complex was formed in greater than 95% within 30 min by simultaneous reduction and complexation of technetium-99m pertechnetate. The Tc-99m and the surrogate rhenium complexes showed similar chromatographic behavior. The complex was evaluated by in vitro receptor binding studies carried out on HTB-121 breast cancer cell line and biodistribution studies performed in normal mice. Our findings suggest that RC-160 can be labeled by the mixed ligand approach with the complex retaining its biological activity and warrants further studies.
- Subjects :
- Animals
Breast Neoplasms metabolism
Female
Humans
Ligands
Mice
Radioligand Assay
Somatostatin analogs & derivatives
Somatostatin pharmacokinetics
Technetium Compounds chemistry
Tissue Distribution
Tumor Cells, Cultured metabolism
Radiopharmaceuticals chemical synthesis
Somatostatin chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0969-8051
- Volume :
- 28
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 11323231
- Full Text :
- https://doi.org/10.1016/s0969-8051(00)00183-9