Table 4.
Subtype selectivity of RgIA-5474.
| Subtypes of nAChR | humana IC50 [nM] (95%CI) | rata IC50 [nM] (95%CI) |
|---|---|---|
| α9α10 | 0.051 (0.027–0.095) | 0.39 (0.33–0.48) |
| α2β2 | >10,000 | >10,000 |
| α2β4 | >10,000 | >10,000 |
| α3β2 | >10,000 | >10,000 |
| α3β4 | >10,000 | >10,000 |
| α4β2 | >10,000 | >10,000 |
| α4β4 | >10,000 | >10,000 |
| α6/α3β4 | >10,000 | >10,000 |
| α6/α3β2β3 | >10,000 | >10,000 |
| α7 | 115 (102–130) | >333 |
| α1β1δε | >10,000 | NAb |
a
Data was collected in Ca 2+ containing ND-96 buffer and 100 μM ACh application. IC50 and 95% confidence intervals (CI) are expressed as the mean ± SEM from 3–5 separate oocytes;
b
peptide was not tested on this subtype. Concentration-response curves and the Hill slope values are shown in Figure S11–12 and Table S2.