Nicotine analog binding to mammalian α7 nAChRs as measured by displacement of [125I]α-BTX–specific binding
Mean Ki estimates ± one sample S.D. are given
| Compound | Rat Brain Receptor | Human Receptor (SH-EP1 Cell) | ||||
|---|---|---|---|---|---|---|
| Ki (nM) | −Hill Slope | n | Ki (nM) | −Hill Slope | n | |
| Nic (N) | 808 ± 85 | 3.0 | 6 | 551 ± 140 | 1.1 | 5 |
| 1′-MeN | 817 ± 74 | 2.5 | 3 | 917 ± 200*** | 1.5 | 4 |
| 1′-EtNorN | 2620 ± 340*** | 2.3 | 4 | 2370 ± 32*** | 1.2 | 4 |
| 2′-MeN | 181 ± 34*** | 2.9 | 7 | 144 ± 24*** | 1.2 | 4 |
| 3′-Trans-MeN | 752 ± 120 | 2.4 | 4 | 756 ± 54* | 1.2 | 4 |
| 3′-Cis-MeN | 3120 ± 500***,ŧŧŧ | 3.1 | 4 | 4780 ± 12***,ŧŧŧ | 1.0 | 3 |
| 4′-Trans-MeN | 3910 ± 30*** | 2.4 | 4 | 6850 ± 630*** | 1.5 | 5 |
| 4′-Cis-MeN | 2930 ± 58***,ŧŧŧ | 2.4 | 4 | 3300 ± 16***,ŧŧŧ | 1.3 | 2 |
| 5′-Trans-MeN | 2130 ± 76*** | 1.5 | 3 | 1970 ± 420*** | 1.1 | 4 |
| 5′-Cis-MeN | 34,800 ± 2600***,ŧŧŧ | 2.0 | 4 | 22,500 ± 2600***,ŧŧŧ | 1.1 | 4 |
n = the number of experiments.
↵* P < 0.05, **P < 0.01, ***P < 0.001, comparison with nicotine. (These P values were obtained from one-way ANOVA of log-transformed data with Dunnett’s multiple comparison post-test.)
ŧP < 0.05, ŧŧP < 0.01, ŧŧŧP < 0.001, comparison of cis- and trans-enantiomers; these P values were obtained from a two-tailed t test and, thus, are not corrected for multiple comparisons. Et, ethyl; Me, methyl; N, nicotine; NorN, nornicotine.