Table 1.
compd | RTI-7527- | R1 | R2 | R3 | α7 nAChR [125I]iodo-MLA Ki, nM (-nH) | α, β nAChR [3H]epibatidine Ki, nM (-nH) |
---|---|---|---|---|---|---|
1a | MLA | CH3 | H | H | 0.87 ± 0.13 (1.09 ± 0.15) | 739 ± 43 (0.68 ± 0.02) |
1b | 58 | H | CH3 | H | 2.12 ± 0.47 (1.2 ± 0.34) | 352 ± 47 (0.89 ± 0.08) |
1c | 60 | CH3 | CH3 | H | 1.78 ± 0.15 (0.92 ± 0.05) | 602 ± 127 (0.93 ± 0.09) |
1d | 62 | CH3 | H | CH3 | 2.46 ± 0.87 (0.98 ± 0.18) | 321 ± 33 (0.88 ± 0.08) |
1e | 59 | C6H5 | H | H | 1.67 ± 0.75 (1.44 ± 0.42) | 219 ± 23 (0.75 ± 0.04) |
1f | 61 | C6H11 | H | H | 26.8 ± 3.62 (0.88 ± 0.21) | 1103 ± 400 (1.21 ± 0.02) |
Data represent the mean ± SE from at least three independent experiments. -nH is the Hill coefficient determined from a four-parameter logistic fit to the data.