Back to Search
Start Over
Design and Synthesis of 99mTcN-Labeled Dextran-Mannose Derivatives for Sentinel Lymph Node Detection
- Source :
- Pharmaceuticals, Volume 11, Issue 3, Pharmaceuticals, Vol 11, Iss 3, p 70 (2018)
- Publication Year :
- 2018
- Publisher :
- MDPI, 2018.
-
Abstract
- Background: New approaches based on the receptor-targeted molecular interaction have been recently developed with the aim to investigate specific probes for sentinel lymph nodes. In particular, the mannose receptors expressed by lymph node macrophages became an attractive target and different multifunctional mannose derivate ligands for the labeling with 99mTc have been developed. In this study, we report the synthesis of a specific class of dextran-based, macromolecular, multifunctional ligands specially designed for labeling with the highly stable [99mTc&equiv<br />N]2+ core. Methods: The ligands have been obtained by appending to a macromolecular dextran scaffold pendant arms bearing a chelating moiety for the metallic group and a mannosyl residue for allowing the interaction of the resulting macromolecular 99mTc conjugate with specific receptors on the external membrane of macrophages. Two different chelating systems have been selected, S-methyl dithiocarbazate [H2N‒NH‒C(=S)SCH3=HDTCZ] and a sequence of two cysteine residues, that in combination with a monophosphine coligand, are able to bind the [99mTc&equiv<br />N]2+ core. Conclusions: High-specific-activity labeling has been obtained by simple mixing and heating of the [99mTc&equiv<br />N]2+ group with the new mannose-dextran derivatives.
- Subjects :
- Stereochemistry
99mTc-radiopharmaceuticals
lcsh:Medicine
lcsh:RS1-441
Pharmaceutical Science
Mannose
Article
030218 nuclear medicine & medical imaging
NO
lcsh:Pharmacy and materia medica
03 medical and health sciences
chemistry.chemical_compound
Residue (chemistry)
0302 clinical medicine
sentinel lymph node
Drug Discovery
Moiety
Chelation
Dextran
Sentinel lymph node
Molecular Medicine
3003
mannose
lcsh:R
chemistry
030220 oncology & carcinogenesis
dextran
Macromolecule
Cysteine
Conjugate
Subjects
Details
- Language :
- English
- ISSN :
- 14248247
- Volume :
- 11
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Pharmaceuticals
- Accession number :
- edsair.doi.dedup.....b4207aed6a5b575ce930d28a598b5cc3