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. Author manuscript; available in PMC: 2008 Jan 15.
Published in final edited form as: Bioorg Med Chem. 2006 Nov 1;15(2):678–685. doi: 10.1016/j.bmc.2006.10.061

Table 1.

Radioligand binding data for MLA (1a) and the MLA analogs 1b–fa

graphic file with name nihms15552ig1.jpg

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)
a

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.