Activities and binding affinities of α-conotoxin variants at nAChRs (human α7 and α3β4 subtypes) and mollusc AChBPs (Ac-AChBP and Ls-AChBP)a.
| Peptide name | pIC50 | pKi | ||
|---|---|---|---|---|
| α7 nAChR | α3β4 nAChR | Ac-AChBP | Ls-AChBP | |
| EpI[Y(SO3)15Y]-OH | NAb | 5.87 (6.05–5.67) | 6.00 (6.29–5.77) | <4.00 |
| EpI-OH | NA | 6.30 (6.47–6.13) | 6.50 (6.77–6.24) | <4.00 |
| EpI[Y(SO3)15Y]-NH2 | NA | 6.46 (6.57–6.36) | 7.57 (7.70–7.44) | <4.00 |
| EpI-NH2 (native) | NA | 7.19 (7.24–7.14) | 8.38 (8.51–8.23) | <4.00 |
| AnIB[Y(SO3)16Y]-OH | NA | NA | 8.00 (8.19–7.79) | <4.00 |
| AnIB-OH | NA | NA | 8.66 (8.85–8.44) | <4.00 |
| AnIB[Y(SO3)16Y]-NH2 | NA | NA | 8.96 (9.10–8.82) | 4.61 (4.99–4.15) |
| AnIB-NH2 (native) | NA | NA | 9.40 (9.52–9.30) | 5.27 (5.51–5.03) |
| PnIA[Y(SO3)15Y]-OH | NA | NA | 7.51 (7.60–7.42) | <4.00 |
| PnIA-OH | NA | NA | 8.33 (8.43–8.23) | <4.00 |
| PnIA[Y(SO3)15Y]-NH2 | NA | NA | 8.85 (8.96–8.77) | 5.04 (5.49–4.57) |
| PnIA-NH2 (native) | NA | NA | 8.92 (9.05–8.80) | 5.42 (6.21–4.68) |
a
Data represent mean with 95% confidence interval.
b
NA = not active: no inhibition of calcium influx was observed at the highest concentration tested (10 μM).