Up-regulation of α4β2 AChRs in HEK cell lines Values are presented as mean ± S.E.M. Values reported in this table reflect binding of [3H]epibatidine to fixed cells after 16 h of up-regulation. C>95 is the concentration of drug required to achieve more than 95% of maximum up-regulation.
| Up-Regulation & Line | Ligand Used to Induce Up-Regulation | ||||||
|---|---|---|---|---|---|---|---|
| Nicotine | Epibatidine | DMPP | Cytisine | MCC | DHβE | Galantamine | |
| Maximum extent (up-regulated/control) | |||||||
| WT α4β2 | 4.9 ± 0.9 | 5.4 ± 1.4 | 5.5 ± 1.1 | 5.2 ± 1.3 | 5.8 ± 1.9 | 3.3 ± 0.6 | 2.2 ± 0.2 |
| S247Fα4β2 | 2.9 ± 0.5 | 2.5 ± 0.9 | 2.5 ± 0.5 | 2.4 ± 0.7 | 1.3 ± 0.2 | 2.2 ± 0.2 | |
| Sensitivity | |||||||
| WT α4β2 | |||||||
| EC50 (nM) | 35 ± 8 | 3.6 ± 0.2 | 3800 ± 1300 | 7.5 ± 2.7 | 1500 ± 500 | 3200 ± 1600 | 3200 ± 900 |
| C>95 (nM) | 500 | 50 | 50,000 | 100 | 50,000 | 500,000 | 100,000 |
| S247Fα4β2 | |||||||
| EC50 (nM) | 27 ± 4 | 1700 ± 700 | 5.8 ± 2.1 | 7900 ± 1300 | 5700 ± 900 | 8400 ± 2900 | |
| C>95 (nM) | 500 | 20,000 | 100 | 100,000 | 200,000 | 500,000 | |