Angewandte
Chemie
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some organs of tumor-bearing mice, with no macroscopic
tumor involvement, activity uptake was greater than the mean
uptake of corresponding organs of nongrafted mice. Histo-
logical analysis revealed tumor involvement in four of these
samples, two brain samples with values of 0.78 and 0.57 D
versus (0.07 Æ 0.03) D in ungrafted mice and two adrenal
tissue samples with values of 1.91 and 9.33 D versus (1.07 Æ
0.39) D in ungrafted mice. These results further demonstrated
the specificity of tumor uptake of 111In-AR60.
In conclusion, the fast plasma clearance, the elevated
tumor labeling, and the low nonspecific uptake of 111In-
labeled NEP ligand AR60 in normal organs provide high
uptake ratios between tumor and normal organs except for
the kidneys and lungs, which express high NEP levels.
Noninvasive scintigraphic imaging of NEP expression with
this compound may be a potential tool for the diagnosis and/
or prognosis of different tumor types.
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Received: February 24, 2005
Published online: May 31, 2005
Keywords: imaging agents · metalloenzymes ·
.
peptidomimetics · radiopharmaceuticals · tumor targeting
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