Table 4.
Effect of α6/α3 and β4 subunit mutation on the IC50 values for inhibition of human and rat α6/α3β4 nAChRs by PeIA
Values in parentheses indicate the 95% CI of the data obtained from four oocytes per IC50 determination. Note that only the human β4L119Q mutation substantially (>3-fold) affects PeIA potency.
| nAChR | IC50 |
|---|---|
| nm | |
| Human | |
| α6/α3β4 | 9.9 (8.2–11.9)a |
| α6I177V/α3β4 | 14.6 (12.3–17.3) |
| α6/α3β4L110V | 15.7 (13.9–17.8) |
| α6/α3β4V118I | 10.6 (8.6–13.0) |
| α6/α3β4L119Q | 94.3 (87.8–101) |
| α6/α3β4L119F | 13.0 (10.7–15.7) |
| α6/α3β4V118I,L119Q | 70.7 (66.1–75.6) |
| Rat | |
| α6/α3β4 | 154 (143–166)a |
| α6V177I/α3β4 | 88.7 (76.3–103) |
| α6/α3β4V110L | 96.3 (85.9–108) |
| α6/α3β4I118V | 119 (105–134) |
| α6/α3β4Q119L | 200 (166–250) |
| α6/α3β4Q119F | 241 (212–274) |
| α6/α3β4I118V,Q119L | 116 (101–133) |
a Data from Table 1 shown for ease of comparison.