Table 1.
Receptor | SS14 |
Octreotide |
Lanreotide |
Pasireotide |
CRN02481 |
|||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Human |
Mouse |
Human |
Mouse |
Human |
Mouse |
Human |
Mouse |
Human |
Mouse |
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pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | pEC50 ± SEM | EC50 (nM) | |
SST1 | 9.0 ± 0.1 | 1.0 | ND | ND | <5.0 | >10,000 | ND | ND | <5.0 | >10,000 | ND | ND | 6.7 ± 0.2 | 180 | ND | ND | <6.0 | >1000 | ND | ND |
SST2 | 9.9 ± 0.1 | 0.13 | 10 ± 0.5 | 0.03 | 10 ± 0.1 | 0.06 | 11 ± 0.0 | 0.02 | 10 ± 0.0 | 0.1 | 10.6 | 0.03 | 9.2 ± 0.1 | 0.59 | 9.1 ± 0.1 | 0.88 | 6.4 ± 0.0 | 440 | 6.5 ± 0.1 | 320 |
SST3 | 9.8 ± 0.0 | 0.16 | 9.8 ± 0.1 | 0.15 | 8.3 ± 0.1 | 5.2 | ND | ND | 6.7 ± 0.1 | 200 | ND | ND | 9.1 ± 0.1 | 0.78 | ND | ND | 7.4 ± 0.1 | 39 | 8.0 ± 0.1 | 10 |
SST4 | 9.7 ± 0.0 | 0.20 | ND | ND | 6.4 ± 0.1 | 450 | ND | ND | 6.1 ± 0.1 | 820 | ND | ND | <5.1 | >8100 | ND | ND | 8.2 ± 0.1 | 5.7 | ND | ND |
SST5 | 10 ± 0.1 | 0.06 | 10 ± 0.1 | 0.07 | 8.6 ± 0.1 | 2.7 | 12 ± 0.1 | 0.002 | 7.8 ± 0.1 | 16 | ND | ND | 10.1 ± 0.1 | 0.081 | 10.5 | 0.032 | 9.4 ± 0.1 | 0.37 | 10 ± 0.1 | 0.04 |
ND: Not determined. pEC50 and SEM given with two significant figures.