Table 1. Effect of MLA Analogs 2−6 at α4β2, α3β4, and α7 nAChRs.
| α4β2 |
α3β4 |
α7 |
||||
|---|---|---|---|---|---|---|
| analog | IC50 (μM)a (95% CI)b | Imaxc | IC50 (μM)a (95% CI)b | Imaxc | IC50 (μM)a (95% CI)b | Imaxc |
| 2d | 7.15 (4.1−12.3) | 0.39 (0.24−0.54) | 16.0 (6.0−42.4) | 0.89 (0.77−1.00) | 11.2 (5.5−22.8) | 0.92 (0.34−1.5) |
| 3 | 21.1 (13.7−32.3) | 0.24 (0.24−0.27) | 7.9(5.5−11.4) | 0.80 (0.69−0.92) | 26.6 (18−37.6) | 0.58 (0.55−0.59) |
| 4 | 4.66 (2.3−9.2) | 0.52 (0.28−0.71) | 2.3 (0.9−6.2) | 0.26 (0.16−0.36) | 20.7 (7.0−61.4) | 1.06 (0.79−1.32) |
| 5e | 11.6 (5.2−25.9) | 0.58 (0.43−0.72) | 14.3 (2.5−24.8) | 0.53 (0.46−0.61) | 23.5 (12.2−45.1) | 0.53 (0.39−0.68) |
| 5f | 53.2 (18.8−150.6) | 1.06 (0.88−1.24) | ||||
| 6 | 10.9 (2.4−49.8) | 0.70 (0.58−0.82) | ||||
a
The concentration of the antagonist that inhibit 50% of ACh response (EC50; the concentration that activates 50% of maximum response) at the nAChR specified. The EC50 concentrations for ACh used were 100 (α4β2), 300, (α3β4), and 300 μM (α7).
b
95% Confidence Intervals (CI); data obtained from 3 to 12 oocytes.
c
Imax is the maximum current produced by ACh alone or ACh in the presence of antagonist (30 μM) at a specified nAChR.
d
Data taken from ref (14).
e
Data for bicyclic alcohol 5 with a 3 min preincubation.
f
Data for bicyclic alcohol 5 with no preincubation.