Technetium-99m labeling of N-[N-(3-diphenylphosphino propionyl)glycyl]cysteine (PN2S-OH) and its methyl ester derivative (PN2S-OMe).
N-[N-(3-diphenylphosphinopropionyl)glycyl]cysteine and its methyl ester derivative were labeled with (99m)Tc at neutral pH, leading to a single species in high yield (>95%) in 30 min. RP-HPLC comparison with the analogue Re(V)-oxo complexes identified the labeled compounds as the anti isomers of pentacoordinated (99m)TcO[PN(2)S]-OH and (99m)TcO[PN(2)S]-OMe complexes. The compounds are stable from pH 7 to pH 9 when (99m)TcO[PN(2)S]-OH interconverts to related syn isomer, while (99m)TcO[PN(2)S]-OMe undergoes both saponification and interconversion. They exhibit high stability in human plasma and in vivo (mice), and a biodistribution characterized by hepatobiliary excretion.
Visentin
Roberta
R
Department of Pharmaceutical Sciences, University of Padova, 35131 Padova, Italy.
Giron
Maria Cecilia
MC
Bello
Michele
M
Mazzi
Ulderico
U
D000818:Animals; D004151:Dipeptides / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008099:Liver / Q000000981:diagnostic imaging* / Q000378:metabolism*; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D009928:Organ Specificity; D015609:Organotechnetium Compounds / Q000097:blood / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D014018:Tissue Distribution
D004151:Dipeptides; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C493914:technetium 99m N-(N-(3-diphenylphosphinopropionyl)glycyl)cysteine; C493915:technetium 99m N-(N-(3-diphenylphosphinopropionyl)glycyl)cysteine methyl ester