Binding affinity | |||||||
Code | Chemical structure | sst1 | sst2 | sst3 | sst4 | sst5 | Functional test |
SRIF-28 | 2.5 ± 0.3 | 2.6 ± 0.2 | 3.0 ± 0.5 | 2.6 ± 0.5 | 2.4 ± 0.2 | ||
HR3005 | cyclo(Arg-cyclo(Cys-Phe-D-Trp-Lys-Thr-Cys)-GABA) | 34 ± 10 | 2.4 ± 0.6 | 3.4 ± 0.8 | 68 ± 22 | 14.5 ± 4.5 | sst2: agonist; sst3: agonist |
AM8 | cyclo(Arg-cyclo(Cys-Phe-D-Trp-Lys-Thr-Cys)-DAB) | 52 ± 13 | 2.7 ± 0.1 | 3.4 ± 1.1 | 75 ± 21 | 11.7 ± 1.7 | sst2: agonist; sst3: agonist |
AM1 | DOTA-cyclo(DAB-Arg-cyclo(Cys-Phe-D-Trp-Lys-Thr-Cys)) | 124 ± 7 | 11.0 ± 1.0 | 18.0 ± 2.0 | 141 ± 25 | 35 ± 12 | sst2: agonist; sst3: agonist |
AM2 | DOTA-cyclo(DAB-Arg-cyclo(Cys-Tyr-D-Trp-Lys-Thr-Cys)) | 866 ± 120 | 21 ± 5 | 169 ± 29 | 154 ± 35 | 59 ± 8 | sst2: agonist; sst3: agonist |
AM3 | DOTA-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-D-Trp-Lys-Thr-Cys)) | 119 ± 6 | 2.3 ± 0.2 | 4.0 ± 0.03 | 97 ± 21 | 27 ± 1 | sst2: agonist; sst3: agonist |
Values are mean inhibitory concentration of 50% (IC50) ± SEM (nM; n ≥ 3).