TABLE 2.
IC50 values for PeIA and analogs with single substitutions on α3β4 nAChRs expressed in X. laevis oocytes.
| Peptide | IC50 value (μM) | Log change in IC50 relative to PeIA |
|---|---|---|
| PeIA | 1.57 (1.28–1.92) | - |
| [S9A]PeIA | 3.79 (3.01–4.78) | 0.4 |
| [S9R]PeIA | 18.7 (5.09–68.9) | 1.1 |
| [S9D]PeIA | > 10 | > 0.8 |
| [S9Y]PeIA | 0.22 (0.20–0.27) | −0.9 |
| [V10I]PeIA | 3.47 (2.30–5.24) | 0.3 |
| [V10L]PeIA | 0.87 (0.71–1.05) | −0.3 |
| [V10Nle]PeIA | 1.18 (1.08–1.29) | −0.1 |
| [N11A]PeIA | 0.30 (0.23–0.41) | −0.7 |
| [N11Adi]PeIA | 3.60 (2.91–4.46) | 0.4 |
| [N11Api]PeIA | 0.90 (0.78–1.04) | −0.2 |
| [N11Asu]PeIA | 0.16 (0.13–0.20) | −1.0 |
| [L15A]PeIA | 0.78 (0.68–0.91) | −0.3 |
| [L15V]PeIA | 0.24 (0.21–0.26) | −0.8 |
| [L15I]PeIA | 0.27 (0.24–0.30) | −0.8 |
| [L15Nle]PeIA | 1.49 (1.34–1.65) | −0.1 |
Values in parentheses indicate the 95% CI; negative log values indicate increased potency and positive values indicate decreased potency relative to native PeIA.