Compound | Concentration | Up-regulation (EC50) | Binding affinity1-a |
---|---|---|---|
μm | Ki nm | ||
Activator | |||
A-85380 | 0.0001–10 | 0.008 ± 0.001 | 0.05 |
ABT-418 | 0.001–100 | 10.47 ± 4.50 | 7.89 |
(−)-Cytisine | 0.001–10 | 4.00 ± 1.94 | 0.44 |
DMPP | 0.001–100 | 12.47 ± 2.40 | 10.71 |
(±)-Epibatidine | 0.0001–10 | 0.010 ± 0.002 | 0.07 |
(+)-Nicotine | 0.01–100 | 4.61 ± 1.10 | 26.25 |
(−)-Nicotine | 0.001–100 | 0.49 ± 0.18 | 1.05 |
Antagonist | |||
d-Tubocurarine | 0.001–300 | >300 | 3481 |
DHβE | 1–1000 | 107.0 ± 38.51 | 60.13 |
Mecamylamine | 0.01–100 | N.E.1-b | >10,000 |
Values are mean ± standard error from three to five separate determinations, each performed in duplicate. Cells were grown in six-well multiwell plates and treated with varying concentrations of the compounds for 168 hr. Binding assays were performed with [3H]cytisine, (6 nm) using membranes prepared from the samples as described in Materials and Methods.