Binding Affinity (IC50 in nmol/L [mean ± SEM]) to Human GRP-R and Mouse or Rat GRP-R of Bombesin Analogs
| Peptide | Membrane-binding assay | Receptor autoradiography | ||||
|---|---|---|---|---|---|---|
| Human R (PC-3) | Rodent R (AR4-2J) | Human R (prostate cancer) | Rodent R (mouse pancreas) | |||
| [Tyr4]BB | 0.87 ± 0.32 (2) | 0.25 ± 0.18 (3) | 1.1 ± 0.0 (3) | ND | ||
| Demobesin 1 | 0.35 ± 0.33 (3) | 0.45 ± 0.18 (2) | 3.2 ± 0.7 (5) | 7.1 ± 1.1 (3) | ||
| Z-070 | 5.14 ± 3.27 (3) | 0.37 ± 0.15 (3) | 8.3 ± 1.9 (3) | 0.76 ± 0.18 3 (3) | ||
| [InIII]Z-070 | 3.87 ± 0.97 (3) | 0.17 ± 0.04 (3) | ND | ND | ||
| [YIII]Z-070 | 3.93 ± 1.23 (3) | 0.20 ± 0.00 (3) | 6.3 ± 1.3 (5) | 0.46 ± 0.03 (3) | ||
| [LuIII]Z-070 | ND | ND | 6.6 ± 2 (3) | 0.5 ± 0.1 (3) | ||
ND = not done.
Value in parentheses is number of independent studies.