P. Auzeloux et al., Synthesis and biodistribution of a new oxo-technetium-99m bis(aminothiol) complex as a potential melanoma tracer, J MED CHEM, 44(7), 2001, pp. 1116-1121
[I-123]-N-(2-Diethylaminoethyl)-4-iodoben (I-123-BZA) has been the best sci
ntigraphic agent described so far far malignant melanoma and ocular melanom
a diagnosis. We replaced I-123 by the more convenient radioisotope Tc-99m a
nd synthesized four bis(aminoethanethiol) derivatives. We describe the synt
hesis of a new oxo-technetium complex (TcO-Cf), prepared in very high yield
(radiochemical yield > 95%), that exhibits an affinity for the pigmented t
umor cells. This complex was evaluated in vivo in mice,bearing C57B16 murin
e melanoma. After injection, a rapid decrease in the radioactivity levels w
as noted for all tissues and organs except for eyes (1.26 %ID/g at 1 h and
2.69 %ID/g at 24 h postinjection) and the tumor (1.19 %ID/g at 1 h and 0.80
%ID/g at 24 h postinjection), suggesting a specific in vivo binding of thi
s complex to the pigmented cells. These results were compared with those al
ready published for three other technetium-99m bis(aminothiol) complexes wi
th benzamide derivatives.