Table 1.
Drug | IC50 (μM) | |
---|---|---|
α4β2 nAChRsa | α3β4 nAChRsa | |
(+)-EDDP | 1.8 ± 0.6 | 0.9 ± 0.09 |
(-)-EDDP | 1.4 ± 0.2 | 0.7 ± 0.06 |
(+)-EMDP | 24 ± 5 | 7.4 ± 2.1 |
(-)-EMDP | 19 ± 4 | 7.0 ± 1.2 |
Mecamylamine | 1.0 ± 0.3 | 3.7 ± 1.2 |
The defined human α4β2 and α3β4 nAChRs are stably expressed in HEK cells designated YXα4β2H1 and YXα3β4H1, respectively. See Materials and Methods for details.
IC50 values were calculated from inhibition curves in which 86Rb+ efflux was stimulated by 100 μM nicotine, as described under Materials and Methods. Mecamylamine, a noncompetitive nAChR antagonist was included for comparison. Data shown are mean ± standard error of three to six independent measurements.