Table 1.
Spadin analogs and their ability to inhibit TREK-1 channel activity and reduce immobility times in FST.
| Figure 2 code | Peptide names | Modifications | % of TREK-1 inhibition | n | P | FST immobility times (s) | p |
|---|---|---|---|---|---|---|---|
| a | PE 12-28 (Spadin) | Not modified | 44.37 ± 8.817 | 7 | 0.0024 | 88.3 ± 7.0 | 0.0001 |
| b | PE 12-27 | Not modified | 28.39 ± 9.916 | 22 | 0.0093 | 100.2 ± 5.0 | 0.0001 |
| c | PE 14-25 | Not modified | −14.73 ± 10.6 | 8 | 0.2074 | 112.2 ± 7.1 | 0.0080 |
| d | PE 22-27 | Not modified | 25.7 ± 20.01 | 10 | 0.2311 | 168.2 ± 4.2 | ns |
| e | PE 22-25 | Not modified | 36.02 ± 17.47 | 14 | 0.0599 | 100.2 ± 5.0 | 0.0001 |
| f | PE 22-28 | Not modified | 55.46 ± 4.555 | 13 | 0.0001 | 91.8 ± 6.1 | 0.0001 |
| g | Biotinylated-PE 22-28 | Addition N-terminus | 53.03 ± 6.416 | 12 | 0.0001 | 112.1 ± 4.3 | 0.0001 |
| h | DansyI-PE 22-28 | Addition N-terminus | 48.78 ± 14.52 | 10 | 0.0084 | 104.6 ± 11.8 | 0.0010 |
| i | PE 22-28-O-Methyl | Addition C-terminus | 42.98 ± 13.47 | 12 | 0.0086 | 137.1 ± 8.1 | 0.0200 |
| j | PE 22-28-O-Ethyl | Addition C-terminus | 41.39 ± 11.52 | 10 | 0.0058 | 113.2 ± 8.5 | 0.0001 |
| k | Formyl-PE 22-28 | Addition N-terminus | 32.45 ± 12.22 | 10 | 0.0262 | ND | |
| l | G/A-PE 22-28 | Substitution-N- terminus | 50.61 ± 7.935 | 10 | 0.0001 | 110.2 ± 3.6 | 0.0001 |
| m | Biotinylated G/A-PE 22-28 | Addition + substitution N-terminus | 46.11 ± 7.743 | 11 | 0.0001 | 140.7 ± 7.1 | 0.0200 |
| n | PI-PE 22-28 | Addition N-terminus | 46.19 ± 7.565 | 7 | 0.0009 | 119.7 ± 11.8 | 0.0070 |
| o | Biotinylated-PI-PE 22-28 | Addition N-terminus | 49.11 ± 7.454 | 10 | 0.0001 | 124.1 ± 11.7 | 0.0080 |
| Palmitoyl-PE 22-28 | Addition N-terminus | 26.69 ± 16.45 | 12 | 0.133 | ND | ||
| FITC-PE 22-28 | Addition N-terminus | 22.1 ± 12.63 | 9 | 0.1183 | ND | ||
| Acetyl-PE 22-28 | Addition N-terminus | 20.49 ± 8.777 | 15 | 0.035 | ND | ||
| Myristoyl-PE 22-28 | Addition N-terminus | 18.04 ± 17.77 | 13 | 0.3302 | ND | ||
| Long Chain biotinylated- PE 22-28 | Addition N-terminus | 15.86 ± 11.21 | 12 | 0.1847 | ND | ||
| 5'FAM-PE 22-28 | Addition N-terminus | 6.633 ± 7.065 | 11 | 0.3699 | ND | ||
| F-Moc-PE 22-28 | Addition N-terminus | 5.826 ± 10.91 | 11 | 0.6051 | ND | ||
| Stearic acid-PE 22-28 | Addition N-terminus | 5.412 ± 5.496 | 32 | 0.3399 | ND |
n, numbers of cells. In FST experiments, n, 10 mice for each peptide.
ns, not significant, ND, Not determined, p-values are from Student's t-test.
Bolded values correspond to the spadin-analogs retained for further studies.