Table 2.
Efficacy and Potency of TC299423 on stoichiometries of α4β2 nAChRs.
| α4β2∗ Two components |
α4β2 (α5KO) | ||
|---|---|---|---|
| High-sensitivity α4(2)β2(3) | Low-sensitivity α4(3)β2(2) | ||
| 86Rb+ efflux, Thalamus | |||
| Efficacy | 139 ± 14% | 32 ± 10% | 166 ± 32% |
| EC50 (μM) | 0.6 ± 0.1 | 10 ± 10 | 1.6 ± 0.5 |
| 86Rb+ efflux, Cortex | |||
| Efficacy | 94 ± 7% | 39 ± 4% | 169 ± 20% |
| EC50 (μM) | 2 ± 2 | 26 ± 21 | 2.4 ± 0.7 |
Efficacy values are given as a percent of the response to nicotine, 10 μM. EC50 data are expressed as mean ± SEM. See Supplementary Figure S1 for full concentration-response curves.