Table 2. Binding affinity of selected compounds at the human α3β4α5 nAChR using [125I]AT-1012 and [3H]epibatidine as radioligands.
Binding was conducted as described in Materials and Methods. Data show average ± SD from at least 2 experiments conducted in triplicate for [3H]epibatidine binding and quadruplicate for [125I]AT-1012 binding. In each cell, the upper line is the Ki and the lower line, in parentheses, is the Hill coefficient. [125I]AT-1012 does not have specific binding to α4β2 nAChR.
| Binding affinity (Ki nM) at human α3β4α5 nAChR | ||
|---|---|---|
| Compound | [125I]AT-1012 | [3H] epibatidine |
| Epibatidine | 1.10±0.04 (0.88±0.02) |
0.58±0.02 (0.98±0.02) |
| Nicotine | 1305±219 (0.75±0.05) |
1573±35 (0.91±0.04) |
| AT-1001 | 1.75±0.14 (0.95±0.05) |
3.34±0.03 (0.82±0.04) |
| AT-1012 | 0.68±0.06 (0.96±0.09) |
1.08±0.05 (0.81 ±0.0 3) |