The chemical structure of T99mc
-GSH has been estabilished using the T99c
isotope.
Labeling of glutathione with technetium in the presence of stanous chloride gave a high yield
result. In a comparative study between T99c
and T99mc
glutathione, the Tc-GSH complex obtained
was purified and characterized by uv, visible spectroscopy, HPLC, Biogel chromatography, mass
and NMR spectroscopy. Stoichiometric analysis showed a 2 : 1 molar ratio of GSH/Tc for the
reaction. The molecular mass assessed by mass spectroscopy was 727 Da corresponding to an
oxo(bis) glutathione technetate. NMR studies demonstrated that each glutathione molecule was
coordinated to technetium via cysteinyl sulfur and nitrogen atoms. The biodistribution of the
complex was studied in normal rats. Blood clearance was rapid during the first hour involving a
biexponential curve ( t1/2
(1) : 50 min, t1/2
(2) : 400 min ). No radioactive accumulation was found in
any specific organ except kidney and bladder. All the activity excreted was found unchanged in
urine. In conclusion, Tc-GSH displayed an anionic dimer form as GSH-Tc-GSH. We assume that the
complex is a tetradentate (2N,2S) complex containing a pentavalent technetium coordinated by two
thiol and nitrogen atoms of both GSH ligands, and an apical oxo group.