Table 1.
Potencies of RgIA and its mutants on rat and human α9α10 nAChR subtypes expressed in Xenopus laevis oocytes.
| Compound | α9α10 (Rat) | α9α10 (Human) | ||
|---|---|---|---|---|
| IC50 * (nM) | Hillslope | IC50 (nM) | Hillslope | |
| RgIA | 2.60 (2.10–3.22) | 0.80 (0.68–0.92) | 1400 (1000–1960) | 0.51 (0.42–0.60) |
| 1 | 41.07 (31.67–53.27) | 0.78 (0.65–0.92) | >10000 | - |
| 2 | 705.4 (478.8–1039) | 0.56 (0.42–0.70) | >10000 | - |
| 3 | 31.77 (26.66–37.87) | 0.84 (0.71–0.97) | 6440 (2790–1490) | 0.51 (0.24–0.77) |
| 4 | >10000 | - | >10000 | - |
| 5 | >10000 | - | >10000 | - |
| 6 | >10000 | - | >10000 | - |
| 7 | >10000 | - | >10000 | - |
| 8 | 2129(1697–2671) | 0.93(0.76–1.11) | 6950 (4500–10700) | 1.32 (0.51–2.13) |
| 9 | 1752 (1351–2272) | 1.02 (0.77–1.26) | >10000 | - |
| 10 | 6012 (4747–7614) | 0.88 (0.69–1.08) | >10000 | - |
| 11 | >10000 | - | >10000 | - |
| 12 | 533.4 (389.9–729.6) | 0.71 (0.56–0.85) | >10000 | - |
| 13 | 1.33 (1.086–1.638) | 0.99 (0.80–1.17) | 1050 (700–1590) | 0.46 (0.37–0.54) |
| 14 | 215.7 (170–273.8) | 0.85 (0.68–1.02) | 2170 (1800–2580) | 1.09 (0.92–1.27) |
| 15 | 288.5 (224.9–398.9) | 0.72 (0.59–0.86) | 680 (650–720) | 1.47 (1.32–1.62) |
* Numbers in parentheses are 95% confidence intervals, and all data calculated by GraphPad Prism from the values of 3−11 oocytes (n = 3–11).