Table 2. Percent Inhibition of nAChR Activity by a Single Concentration of Compounds 16 and 1a.
hα3β4 nAChR | hα4β2 nAChR | |
---|---|---|
compound | % inhibitiona,b | % inhibitiona,b |
1 | 58.2 ± 9.2 | 74.0 ± 14.2 |
2 | 82.7 ± 3.3 | 79.3 ± 6.0 |
3 | 82.8 ± 11.5 | 67.3 ± 28.0 |
4 | 53.0 ± 9.5 | 59.0 ± 7.8 |
5 | 14.0 ± 6.6 | 21.8 ± 6.2 |
6 | 19.3 ± 24.4 | 13.3 ± 24.5 |
1a | NTc | 44.1 ± 22.3 |
D-tubocurarined | 54.0 ± 23.5 | 61.0 ± 27.9 |
mecamylamined | 88.3 ± 13.3 | 91.8 ± 5.6 |
KAB-18d | NAe | 39.0 ± 11.7 |
Percent inhibition was determined at 10 μM.
Values represent means ± SM, n = 2-5.
NT = not tested.
Known nicotinic receptor antagonist.
NA = no activity at 10 μM.