Table 7.
Selectivity Profile of PeIA-5667 for Human and Rat nAChRsa
|
human
|
rat
|
|||||
|---|---|---|---|---|---|---|
| nAChR | IC50 (nM) | n | IC50 ratio | IC50 (nM) | n | IC50 ratio |
| α1β1δε | >10 000 | 4 | >50 000 | ND | ||
| α2β2 | >10 000 | 4 | >50 000 | >10 000 | 4 | >20 000 |
| α2β4 | >10 000 | 4 | >50 000 | >10 000 | 4 | >20 000 |
| α3β2 | >10 000 | 4 | >50 000 | >10 000 | 5 | >20 000 |
| α3β4 | 179 (160–201) | 4 | 895 | 230 (199–265) | 4 | 489 |
| α4β2 | >10 000 | 4 | >10 000 | >10 000 | 4 | >20 000 |
| α4β4 | 4015 (3620–4453) | −4 | 20 075 | >10 000 | 5 | >20 000 |
| α6/α3β2β3 | 135 (88.2–207) | 6 | 675 | 111 (67.0–184) | 4 | 227 |
| α7 | >10 000 | 4 | >50 000 | >10 000 | 4 | >20 000 |
| α9α10 | >10 000 | 4 | >50 000 | >10 000 | 4 | >20 000 |
a
Values within parentheses indicate the 95% confidence interval; IC50 ratio calculated relative to the IC50 value for α6/α3β4; n indicates the number of oocytes tested; ND, not determined.