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Table 3 Agonistic potency toward SST2 and SST5 of all four natGa-DOTA-conjugates compared to reference somatostatin analogs

From: A new 68Ga-labeled somatostatin analog containing two iodo-amino acids for dual somatostatin receptor subtype 2 and 5 targeting

  SST2 SST5
Compounds EC50, nM
(95% CI)
EC50, nM
(95% CI)
Somatostatin-14* (1) 0.23 (0.09–0.62) 1.9 (0.77–4.5)
natGa-DOTA-ST8950 0.46 (0.23–0.92) 16 (6.7–36)
natGa-DOTA-ST8951 9.8 (3.7–26) 128 (41–512)
natGa-DOTA-TATE 0.47 (0.15–1.5) 39 (15–101)
natGa-DOTA-NOC 0.59 (0.18–1.9) 3.3 (1.3–8.5)
ST8950 (1) 0.29 (0.12–0.67) 8.5 (3.7–19)
Octreotide** (1) 0.21 (0.12–0.36) 27 (8.1–88)
Pasireotide** (1) 1.1 (0.48–2.5) 0.60 (0.21–1.7)
  1. Experiments were performed in 3 to 4 separate sessions in duplicate
  2. *Somatostatin-14 is the natural ligand and was used as control
  3. **Octreotide and pasireotide were used for comparison, additionally to natGa-DOTA-TATE and natGa-DOTA-NOC
  4. (1)From [25]