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Synthesis and biological evaluation of Tc-99m-cyclopentadienyltricarbonyltechnetium-labeled octreotide.
- Source :
-
Nuclear medicine and biology [Nucl Med Biol] 1999 Jan; Vol. 26 (1), pp. 1-7. - Publication Year :
- 1999
-
Abstract
- Octreotide was labeled at its N-terminus with Tc-99m-cyclopentadienyltricarbonyltechnetium, and the biodistribution of the labeled conjugate was studied in adult female Sprague-Dawley rats. The synthesis began with the preparation of Tc-99m-(methoxycarbonylcyclopentadienyl) tricarbonyltechnetium from Tc-99m-pertechnetate using a novel double ligand transfer reaction; it was completed in a total of five steps, with an 8% overall radiochemical yield (15% decay-corrected). The 99mTc-cyclopentadienyltricarbonyltechnetium-labeled octreotide conjugate (99mTc-CpTT-octreotide) showed receptor-mediated uptake in the pancreas and adrenals, which was blocked (80% and 93%, respectively) by excess unlabeled octreotide. These studies illustrate a new method for labeling a peptide with Tc-99m through an organometallic linkage that is stable, nonpolar, and low molecular weight; it complements labeling approaches that utilize inorganic metal complexes.
- Subjects :
- Animals
Female
Humans
Intestinal Mucosa metabolism
Isotope Labeling
Ligands
Liver metabolism
Octreotide chemical synthesis
Octreotide metabolism
Octreotide pharmacokinetics
Octreotide pharmacology
Organ Specificity
Organotechnetium Compounds metabolism
Organotechnetium Compounds pharmacokinetics
Radiopharmaceuticals metabolism
Radiopharmaceuticals pharmacokinetics
Rats
Rats, Sprague-Dawley
Receptors, Somatostatin metabolism
Tissue Distribution
Adrenal Glands metabolism
Octreotide analogs & derivatives
Organotechnetium Compounds chemical synthesis
Pancreas metabolism
Radiopharmaceuticals chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0969-8051
- Volume :
- 26
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 10096494
- Full Text :
- https://doi.org/10.1016/s0969-8051(98)00060-2