Binding characteristics of compounds to native mAChRs
The [3H]NMS competition binding assay to rat brain membranes were performed as described under Materials and Methods. The ratios between the binding affinities from the [3H]NMS assay (KimAChR) and the Ki values from [3H]Epibatidine binding to α4β2 and α3β4 nAChRs are also given.
| Compound | Ki (pKi ± S.E.M) | nH(CI) | KimAChR/Kiα4β2 | KimAChR/Kiα3β4 |
|---|---|---|---|---|
| μM | ||||
| 7 | 51 (4.29 ± 0.08) | 0.85 (0.81−0.89) | 230 | 140 |
| 13 | 74 (4.13 ± 0.02) | 0.96 (0.73−1.3) | 5700 | 7.1 |
| 14 | 9.7 (5.01 ± 0.05) | 0.81 (0.75−0.89) | 1700 | 160 |
| 15 | 6.6 (5.18 ± 0.01) | 0.88 (0.81−0.95) | 550 | 47 |
| 17 | 2.9 (5.53 ± 0.05) | 0.88 (0.84−0.92) | 1.9 | 0.034 |
| 18 | 0.55 (6.26 ± 0.05) | 0.96 (0.78−1.2) | 0.011 | 0.0068 |
| 19 | 4.2 (5.38 ± 0.02) | 0.97 (0.84−1.1) | 33 | 0.21 |
| 20 | 4.1 (5.38 ± 0.09) | 0.82 (0.72−0.92) | 33 | 2.7 |
| 21 | 48 (4.32 ± 0.03) | 0.98 (0.85−1.1) | 340 | 25 |
CI, confidence interval.