Table 1.
Biodistribution of 111In-DOTA-Nle-CycMSHhex in B16/F1 melanoma-bearing C57 mice. The data were presented as percent injected dose/gram or as percent injected dose (Mean±SD, n=5)
Tissues | 0.5 h | 2 h | 4 h | 24 h | 2 h NDP blockade | 2 h L-lysine co-injection |
---|---|---|---|---|---|---|
Percent injected dose/gram (%ID/g) | ||||||
Tumor | 24.94±4.58 | 19.39±1.65 | 17.01±2.54 | 10.53±1.11 | 0.81±0.03* | 14.48±3.25 |
Brain | 0.21±0.07 | 0.02±0.01 | 0.06±0.03 | 0.03±0.01 | 0.01±0.01 | 0.04±0.01 |
Blood | 3.33±0.35 | 0.11±0.07 | 0.05±0.02 | 0.02±0.01 | 0.07±0.05 | 0.92±0.48 |
Heart | 1.24±0.15 | 0.16±0.10 | 0.12±0.03 | 0.07±0.05 | 0.06±0.02 | 0.37±0.02 |
Lung | 2.45±0.83 | 0.32±0.10 | 0.10±0.05 | 0.10±0.03 | 0.30±0.06 | 0.75±0.21 |
Liver | 2.75±0.26 | 1.46±0.20 | 1.72±0.07 | 1.89±0.14 | 1.46±0.08 | 1.42±0.30 |
Spleen | 1.09±0.33 | 0.41±0.13 | 0.47±0.13 | 0.32±0.08 | 0.44±0.02 | 0.43±0.07 |
Stomach | 3.20±0.98 | 1.25±0.24 | 1.49±0.12 | 1.34±0.42 | 0.36±0.14 | 1.64±0.78 |
Kidneys | 16.20±4.32 | 9.52±0.44 | 9.99±1.39 | 9.31±0.91 | 11.56±0.56 | 6.66±0.62* |
Muscle | 0.60±0.22 | 0.15±0.08 | 0.10±0.08 | 0.03±0.01 | 0.02±0.01 | 0.10±0.08 |
Pancreas | 1.18±0.38 | 0.14±0.02 | 0.16±0.02 | 0.23±0.08 | 0.12±0.02 | 0.21±0.05 |
Bone | 1.34±0.40 | 0.18±0.10 | 0.22±0.15 | 0.16±0.03 | 0.05±0.04 | 0.55±0.14 |
Skin | 4.11±0.72 | 0.66±0.23 | 0.53±0.05 | 0.64±0.16 | 0.29±0.02 | 1.02±0.09 |
Percent injected dose (%ID) | ||||||
Intestines | 2.16±0.28 | 1.40±0.56 | 3.03±1.06 | 1.41±0.86 | 1.14±0.47 | 1.85±0.73 |
Urine | 57.00±3.91 | 82.23±5.83 | 84.61±5.21 | 87.29±3.60 | 92.25±1.56 | 76.79±5.35 |
Tumor to normal tissue uptake ratio | ||||||
Tumor/Blood | 7.49 | 176.27 | 340.20 | 526.50 | 11.57 | 15.74 |
Tumor/Kidneys | 1.54 | 2.04 | 1.70 | 1.13 | 0.07 | 2.17 |
Tumor/Lung | 10.18 | 60.59 | 170.10 | 105.30 | 2.70 | 19.31 |
Tumor/Liver | 9.07 | 13.28 | 9.89 | 5.57 | 0.55 | 10.20 |
Tumor/Muscle | 41.57 | 129.27 | 170.10 | 351.00 | 40.50 | 144.80 |
Tumor/Skin | 6.07 | 29.38 | 32.09 | 16.45 | 2.79 | 14.20 |
P <0.05, significance comparison between the tumor uptakes of 111In-DOTA-Nle-CycMSHhex with or without NDP-MSH blockade, and between the kidney uptakes of 111In-DOTA-Nle-CycMSHhex with or without L-lysine co-injection.