Table 1 Affinity profiles (IC50 values) for human sst1–sst5 receptors of a series of common somatostatin analogues (Reubi et al. 2000), having been determined by receptor autoradiography on sectioned cell pellets, and SiTATE, having been determined by competitive displacement assays on cell membranes
From: Favorable SSTR subtype selectivity of SiTATE: new momentum for clinical [18F]SiTATE PET
Peptides | hsst1 | hsst2 | hsst3 | hsst4 | hsst5 |
|---|---|---|---|---|---|
SST-28 | 5.2 ± 0.3 | 2.7 ± 0.3 | 7.7 ± 0.9 | 5.6 ± 0.4 | 4.0 ± 0.3 |
Octreotide | > 10.000 | 2.0 ± 0.7 | 187 ± 55 | > 1.000 | 22 ± 6 |
DOTA-TOC | > 10.000 | 14 ± 2.6 | 880 ± 324 | > 1.000 | 393 ± 84 |
Ga-DOTA-TOC | > 10.000 | 2.5 ± 0.5 | 613 ± 140 | > 1.000 | 73 ± 21 |
DOTA-[Tyr3]-octreotate | > 10.000 | 1.5 ± 0.4 | > 1.000 | 453 ± 176 | 547 ± 160 |
Ga-DOTA-[Tyr3]-octreotate | > 10.000 | 0.2 ± 0.04 | > 1.000 | 300 ± 140 | 377 ± 18 |
SiTATE | > 10.000 | 1.0 ± 0.2 | 712 ± 507 | 364 ± 291 | > 1.000 |