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Table 2 Affinity profiles of the nat Ga, nat Lu, and nat Y complexes of DOTATATE and HA-DOTATATE for hsst 1 -hsst 5 receptors

From: Twins in spirit - episode I: comparative preclinical evaluation of [68Ga]DOTATATE and [68Ga]HA-DOTATATE

Peptide

hsst 1

hsst 2

hsst 3

hsst 4

hsst 5

natGa-DOTATATE

>1,000 (2)

1.2 ± 0.6 (5)

>1,000 (2)

>1,000 (3)

>1,000 (3)

natLu-DOTATATE

>1,000 (2)

2.0 ± 0.8 (5)

162 ± 16 (2)

>1,000 (3)

>1,000 (3)

natGa-HA-DOTATATE

>1,000 (2)

1.4 ± 0.8 (5)

>1,000 (2)

>1,000 (3)

102 ± 65 (4)

natLu-HA-DOTATATE

>1,000 (2)

2.0 ± 1.6 (5)

93 ± 1 (2)

>1,000 (3)

222 ± 148 (4)

natY-HA-DOTATATE

n.d.

2.4 ± 0.3 (2)

n.d.

n.d.

680 (1)

  1. Affinity profiles were determined using membrane preparations of CHO cells stably transfected with the respective sst subtype (supplier: Millipore) and [Leu8,D-Trp22,[125I]Tyr25]-somatostatin 28 as the radioligand. Values represent IC50 ± SD [nM]; the number of independent experiments is shown in parentheses. n.d., not determined.