IC50 values for inhibition of rat nAChRs by doubly substituted analogs of PeIA
Numbers in parentheses are 95% confidence intervals.
| α3β2 | α6/α3β2β3 | α3β4 | α6/α3β4 | Ratio of α6/α3β4 to α6/α3β2β3 | |
|---|---|---|---|---|---|
| PeIA[S9H,V10A] | 793 (675–932) pM | 506 (455–564) pM | 307 (240–394) nM | 65.1 (50.0–84.8) nM | 129 |
| PeIA[S9H,E14N] | 1.15 (1.02–1.09) nM | 753 (656–864) pM | 128 (109–151) nM | 29.5 (24.4–34.6) nM | 39 |