Table 1.
Inhibition of [3H]NIC binding (probing α4β2* nAChRs) and [3H]MLA binding (probing α7* nAChRs) to rat brain membranes, nicotine-evoked [3H]DA release from superfused rat striatal slice.a
| Compounds | NIC binding (% inhibition at 100 nM) | MLA binding (% inhibition at 100 nM) | DA Release (% inhibition at 100 nM) | Compounds | NIC binding (% inhibition at 100 nM) | MLA binding (% inhibition at 100 nM) | DA Release (% inhibition at 100 nM) | ||
|---|---|---|---|---|---|---|---|---|---|
 |
 |
||||||||
| 8a |  |
11 ± 11. % | 18 ± 7.8 % | 16 ± 13 % | 11a |  |
12 ± 4.4 % | 12 ± 6.9 % | 8 ± 4 % |
| 8b |  |
24 ± 5.5 % | 3.0 ± 3.0 % | 35 ± 14 % | 11b |  |
12 ± 8.3 % | 8.0 ± 5.3 % | 46 ± 5 % |
| 8c |  |
9.8 ± 1.2 % | 0.6 ± 0.6 % | 17 ± 6 % | 11c |  |
0.5 ± 0.5 % | 18 ± 10 % | 36 ± 11 % |
| 8d |  |
0 ± 0 % | 3.9 ± 3.9 % | 12 ± 5 % | 11d |  |
3.7 ± 3.7 % | 15 ± 8.0 % | 45 ± 14 % |
| 8e |  |
38 ± 7.4 % | 15 ± 2.0 % | 31 ± 13 % | 11e |  |
7.4 ± 4.7 % | 26 ± 14 % | 43 ± 21 % |
| 8f |  |
2.9 ± 2.9 % | 53 ± 3.5 % | 17 ± 17 % | 11f |  |
13 ± 3.3 % | 16 ± 8.0% | 54 ± 10 % IC5=28 ± 11 nMb |
| 8g |  |
0 ± 0 % | 4.9 ± 3.8 % | 39 ± 17 % | 11g |  |
6.5 ± 6.5 % | 24 ± 13 % | 63 ± 12 % IC50=56 ± 45 nMb |
| 8h |  |
9.7 ± 9.7 % | 17 ± 8.9 % | 24 ± 14.3 % | 11h |  |
0.9 ± 0.9 % | 27 ± 15 % | 27 ± 2% |
| 8i |  |
0.3 ± 0.3 % | 53 ± 0.8 % | 37 ± 15 % | 11i |  |
6.6 ± 4.5 % | 33 ± 17 % | 19 ± 15 % |
| 8j |  |
0 ± 0 % | 5.7 ± 5.7 % | 41 ± 15 % | 11j |  |
9.6 ± 5.2 % | 20 ± 13 % | 64 ± 15 % IC50=3.38 ± 2.62nMb |
| 2 | bPiDDB | Ki = 48.6 µMb | Ki > 100 µMb | IC50 = 2 nMb | 3 | tPy3PIB | 10 ± 1.9 % | 0 ± 0 % | 40 ± 12 % IC50=0.2 ± 0.07 nMb |
a
Percentage of inhibition at 100 nM are presented unless otherwise specified. Each value represents data from at least three independent experiments, each performed in duplicate.
b
IC50 from full concentration response assay; data from 4–5 independent experiments, each performed in duplicate.