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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]