Experiments on a new phosphine-peptide chelator for labelling of peptides with Tc-99m.
A phosphine-containing ligand providing a N-[N-[3-(diphenylphosphino)propionyl]glycyl]-L-S-benzyl-cystein (PNNS) donor atomset for the chelation of 99mTc was studied in labelling experiments with a model peptide (tetragastrin, cholecystokinin-fragment). The peptide was conjugated to the ligand chelator by active ester chemistry either before or after radiolabelling. Both the chelator-conjugate and the preformed chelate approaches resulted in the same radiolabelled isomers of the ligand peptide. Sequence and reaction conditions influence yield and purity.
Santimaria
M
M
Department of Radiology, Leiden University Medical Center, The Netherlands.
Blok
D
D
Feitsma
R I
RI
Mazzi
U
U
Pauwels
E K
EK
D002614:Chelating Agents / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D007553:Isotope Labeling / Q000379:methods*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D010455:Peptides / Q000737:chemistry*; D010720:Phosphines / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D013667:Technetium / Q000737:chemistry*; D013758:Tetragastrin / Q000737:chemistry*
D002614:Chelating Agents; D015609:Organotechnetium Compounds; D010455:Peptides; D010720:Phosphines; D019275:Radiopharmaceuticals; D013758:Tetragastrin; D013667:Technetium; C044646:phosphine