Cysteine, a chelating moiety for synthesis of 99Tcm radiopharmaceuticals. III: Functionalization of hydroxy group for 99Tcm chelation.
A method is offered for converting an organic hydroxy compound to a 99Tcm-binding ligand under mild experimental conditions. Cyclohexanol was selected as a typical hydroxy compound and to this molecule cysteine was attached through substitution at the sulphur atom by a two-step chemical synthesis. The ligand thus obtained could be successfully radiolabelled with 99Tcm. The biodistribution of the resulting radiolabelled compound had the characteristic of a mixed hydrophilic-lipophilic 99Tcm chelate and was similar to that of 99Tcm-HIDA derivatives, a well established class of 99Tcm-chelates. So it may be concluded that the above method of functionalization of a hydroxy compound does not generate any unusual physiological properties and may be recommended as a general method for radiolabelling an organic compound at the alcoholic site with 99Tcm.
Chatterjee
M
M
Department of Nuclear Medicine, Indian Institute of Chemical Biology, Calcutta.
Banerjee
S
S
D000818:Animals; D007553:Isotope Labeling / Q000379:methods; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D013667:Technetium; D014018:Tissue Distribution
D015609:Organotechnetium Compounds; D013667:Technetium