Functional characteristics of compounds at the α3β4 nAChR
The EC50 and nH values obtained for the compounds at the α3β4-HEK 293 cell line in the FLIPR membrane potential assay. The experiments were performed as described under Materials and Methods. Each experiment was performed in duplicate at least three times.
| Compound | EC50 (pEC50 ± S.E.M.) | nH (CI) |
|---|---|---|
| μM | ||
| ACh | 35 (4.45 ± 0.09) | 1.7 (1.4−2.0) |
| (S)-Nicotine | 8.1 (5.09 ± 0.07) | 1.8 (1.6−2.0) |
| (−)-Cytisine | 14 (4.85 ± 0.10) | 1.5 (1.3−1.7) |
| (±)-Epibatidine | 0.024 (7.62 ± 0.06) | 1.7 (1.5−1.9) |
| MCC | 44 (4.36 ± 0.09) | 1.7 (1.6−1.9) |
| 7 | 11 (4.94 ± 0.06) | 1.6 (1.4−1.8) |
| 13 | 200 (3.71 ± 0.05) | 2.1 (1.8−2.5) |
| 14 | 2.8 (5.56 ± 0.07) | 1.5 (1.3−1.8) |
| 15 | 3.0 (5.52 ± 0.04) | 2.2 (1.9−2.5) |
| 16 | N.D. | N.D. |
| 17 | 360 (3.44 ± 0.06) | 1.8 (1.6−2.1) |
| 18 | 1,400 (2.85 ± 0.15) | 0.72 (0.64−0.82) |
| 19 | 520 (3.29 ± 0.12) | 2.6 (2.2−3.1) |
| 20 | 25 (4.61 ± 0.07) | 2.1 (1.8−2.4) |
| 21 | 82 (4.09 ± 0.04) | 1.7 (1.4−2.1) |
CI, confidence interval; N.D., not determined.