Table 2. Amino acid sequences and blocking activities (in IC50s, nM) of α-conotoxin GIC and its analogues on expressed nAChR subtypes.
| Peptide | Sequence | Subtype | IC50 (nM) | Hill Slope | Subtype | IC50 (nM) |
|---|---|---|---|---|---|---|
| GIC | GCCSHPACAGNNQHIC* | hα3β2 | 1.13(1.10–1.16) | 0.764(0.559–0.969) | hα3β4 | 750(710–790) |
| GIC(Q13A) | GCCSHPACAGNNAHIC* | hα3β2 | 8.41(7.027–10.01) | 1.078(0.823–1.332) | hα3β4 | 660(630–690) |
| GIC(N12A) | GCCSHPACAGNAQHIC* | hα3β2 | 1980(840–4660) | 0.35(0.238–0.463) | hα3β4 | >10000 |
| GIC(N11A) | GCCSHPACAGANQHIC* | hα3β2 | 1600(545–4720) | 0.491(0.222–0.760) | hα3β4 | >10000 |
| GIC(A7L) | GCCSHPLCAGNNQHIC* | hα3β2 | >10000 | — | hα3β4 | >10000 |
| GIC(A7G) | GCCSHPGCAGNNQHIC* | hα3β2 | 4210(1566–11330) | 0.371(0.222–0.521) | hα3β4 | >10000 |
| GIC(H5A) | GCCSAPACAGNNQHIC* | hα3β2 | >10000 | — | hα3β4 | >10000 |
*C-terminal carboxamide.