Summary of EC50, IC50, and binding affinity values (Ki) of SEN12333 at different subtypes of rat and human nAChRs and selectivity profile
Results are the means ± S.E.M. of n independent experiments. Agonist (EC50) and antagonist (IC50) activities were determined in FLIPR experiments with a double sequential addition protocol as described under Materials and Methods. Concentration ranged from 10−9 to 10−4 M.
Receptor | SEN12333 EC50 | SEN12333 IC50/Ki | n | |
|---|---|---|---|---|
| μM | ||||
| rα7 (Ki) | 0.26 ± 0.03 | 3 | ||
| rα7 (FLIPR) | 1.6 ± 0.9 | 4 | ||
| rα7 (patch clamp) | 12 | 2 | ||
| Selectivity (FLIPR) | ||||
| hα1β1δγ | Inactive | Inactive | 3 | |
| hα3β2(α5) | Inactive | 8.5 ± 3.6 | 4 | |
| hα4β2 | Inactive | 45% inhibition at 100 μM | 3 | |
| h5-HT3A | Inactive | Inactive | 4 | |
| Broad selectivity | ||||
| h histamine H3 receptor (IC50) | 0.103 | |||
| hERG | 6% inhibition at 1 μM | |||
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| 29% inhibition at 10 μM |
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