HN
N
NH
N
R
R
R
R
R =
OCH 2 COOH
OCH 2 COOH
26
HN
N
NH
N
R
R
R
R
R =
SO 3 Na
27
HN
N
NH
N
OCH 2 COOH
HOOCH 2 CO
OCH 2 COOH
O
HOOCH 2 CO
OCH 2 COOH
HOOCH 2 CO
O
O
O
O
O
O
328
Re
3.4 Phthalocyanine Radiolabeling
3.4.1 Copper-64
64 Cu labeled phthalocyanines (Pcs) have been employed for PET imaging agents.
64 Cu labeled sulfonated metallophthalocyanines (PcS),
64 CuPcS 29, was employed
for biodistribution studies in tumor-bearing rats using PET imaging [17].
Biodistribution results showed that tumor uptake was low (0.2%ID/g) and most
64 Cu was taken up by the kidneys and liver (20 and 12%ID/g, respectively). Guérin
et al. reported various modified
64 Cu labeled sulfonated metallophthalocyanines
(
64 CuPcS n ) 30a-d and their biodistribution studies [80]. The amphiphilic derivatives
64 CuPcS 2 and
64 CuPcS 3 C 6 (1–1.5% injected dose per gram, respectively)
exhibited the highest tumor-to-background ratios.
64 Cu-labeled frozen micellar naphthalocyanines (nanonaps) were used for
whole-body PET imaging of the gastrointestinal tract [81]. Labeling was achieved
in just 30 min with over 65% radiolabeling when nanonaps were incubated with
64 Cu in aqueous solution (Fig. 3.8a). The movement of the nanonaps through the
GI tract was monitored by using PET imaging (Fig. 3.8b). Serial whole-body
consecutive coronal images of the mouse are shown in Fig. 3.8c.
70
V. Rajendiran et al.