Bupropion and its hydroxy metabolites as functional antagonists toward nAChR subtypes in cell lines
86Rb+ efflux assays were conducted as described under Materials and Methods and in the legend to Fig. 1. Results were fit to the logistic equation to determine molar IC50 values and Hill coefficients (values given in parentheses) presented as ± S.E.M.
| SH-SY5Y α3β4* | SH-EP1-hα4β2α4β2 | SH-EP1-hα4β4α4β4 | TE671/RD α1* | |
|---|---|---|---|---|
| μM | ||||
| Bupropion | 1.8 ± 1.1a,b (-1.24 ± 0.19) | 12 ± 1.1b (-1.24 ± 0.18) | 14 ± 1.1b (-1.19 ± 0.09) | 7.9 ± 1.1b (-1.25 ± 0.14) |
| (2S,3S) OH-bupropion | 10 ± 1.5 (-1.08 ± 0.35) | 3.3 ± 1.1a,c (-1.31 ± 0.11) | 30 ± 1.1c (-1.10 ± 0.12) | 28 ± 1.4 (-1.25 ± 0.32) |
| (2R,3R)-OH-bupropion | 6.5 ± 1.2a,b (-1.08 ± 0.18) | 31 ± 1.1 (-1.53 ± 0.27) | 41 ± 1.1c (-1.65 ± 0.19) | 7.6 ± 1.1a,b (-1.23 ± 0.13) |