TABLE 5.
EC50 and Rmax values for compound-evoked 3H-dopamine release from rat striatum. Rat striatal synaptosomes were exposed to the nAChR compounds to evoke 3H-dopamine release. Release is expressed as the % release relative to that occurring with 10 μM nicotine. For the EC50 values, the numbers in parentheses represent the 95% confidence intervals (CI). Rmax values are expressed as mean ± SEM of 3 to 4 assays, with 2 rats per assay.
| Compound | EC50 (CI) μM | Rmax % of 10 μM nicotine |
|---|---|---|
| TC-2696 | 6.3 (1.2 – 31) | 204 ± 43 |
| TI-10165 | 0.81 (0.14 – 4.0) | 78 ± 9.1 |
| TC-8831 | 0.14 (0.10 – 0.26) | 91 ± 3.8 |
| TC-10600 | 1.49 (0.65 – 3.39) | 72 ± 5.7 |
| Sazetidinea | 0.001 | 96 ± 6 |
| Nicotine | 3.0 (1.3 – 7.3) | 100 ± 8.9 |
| Varenicline | 0.05 (0.01 – 0.20) | 41 ± 5.0 |
a
Taken from (Zwart et al., 2008)