TABLE 1

Biodistribution in Nude Mouse Xenografts of Selected Peptides, 4 Hours After Intravenous Administration

%ID/g ± SD
Cell linePeptideBloodTumorKidneynRatio
AR42JH2-Met10.04 ± 0.010.87 ± 0.211.87 ± 0.60150.47
CCK-820.05 ± 0.000.49 ± 0.14*2.09 ± 0.85†40.23
H6-Met30.20 ± 0.030.59 ± 0.14*2.95 ± 0.60*80.20
MG040.06 ± 0.022.60 ± 0.65*60.45 ± 9.04*40.04
MG1150.04 ± 0.010.92 ± 0.10†3.30 ± 0.35*50.28
H2-Nle60.03 ± 0.000.73 ± 0.14†2.40 ± 2.13†20.31
H2-Met(O)70.04 ± 0.000.12 ± 0.011.21 ± 0.0310.10
CA20948H2-Met10.07 ± 0.020.59 ± 0.102.41 ± 0.9170.24
CCK-820.05 ± 0.010.46 ± 0.132.33 ± 0.6840.20
H6-Met30.21 ± 0.010.55 ± 0.143.08 ± 0.7790.18
MG1150.03 ± 0.000.75 ± 0.054.11 ± 0.3910.18
H6-Nle80.02 ± 0.000.15 ± 0.060.98 ± 0.1810.16
H2-Nle60.03 ± 0.000.53 ± 0.081.73 ± 0.3110.31
HT29-CCK2RH2-Met10.08 ± 0.010.19 ± 0.052.44 ± 0.4760.08
CCK-820.05 ± 0.000.13 ± 0.031.95 ± 0.2890.06
H6-Met30.26 ± 0.030.26 ± 0.043.47 ± 0.52130.08
MG1150.02 ± 0.000.07 ± 0.033.47 ± 0.3410.02
H6-Nle80.02 ± 0.010.05 ± 0.001.01 ± 0.0810.05

  • ↵* Statistically significant (P < 0.05) with corresponding value for H2-Met.

  • ↵† Not statistically significant (P < 0.05) with corresponding value for H2-Met.

  • ↵1 H2-Met = DOTA-HHEAYGWMDF-NH2.

  • ↵2 CCK-8 = DOTA-dYMGWMDF-NH2.

  • ↵3 H6-Met = DOTA-HHHHHH-EAYGWMDF-NH2.

  • ↵4 MG0 = DTPA-eEEEEEAYGWMDF-NH2.

  • ↵5 MG11 = DTPA-eAYGWMDF-NH2.

  • ↵6 H2-Nle = DOTA-HHEAYGWMDF-NH2.

  • ↵7 H2-Met(O) = DOTA-HHEAYGWM(sulfoxide)DF-NH2.

  • ↵8 H6-Nle = DOTA-HHHHHHEAYGWMDF-NH2.

  • SD = mean SD achieved in all studies; ratio = tumor-to-kidney ratio (column 4 mean value/column 5 mean value); CCK-8 = cholecystokinin-8; CCK2R = CCK-2 receptor.

  • Results show mean values obtained from n replicate studies in groups of 3 or 4 animals.