Induction of Ds by 5-min incubations
Data obtained from X. laevis oocytes. All evoked responses are net charge values, normalized to the average net charge in two initial 60 μM ACh applications. “Ds Induction” refers to rank order for the relative effectiveness of each drug for stabilizing receptors in the Ds, state as measured by the ability of PNU-120596 application to stimulate currents of the predesensitized receptors.
| Compound | Evoked Response | ACh Residual | PAM-Evoked | Ds Induction |
|---|---|---|---|---|
| ACh, 1 mM | 1.12 ± 0.08 | 0.01 ± 0.01 | 32.1 ± 2.3 | 1 |
| diOHBA, 100 μM | 0.78 ± 0.06 | 0.01 ± 0.01 | 13.3 ± 1.56 | 3 |
| 4OH2MeOBA, 100 μM | 0.61 ± 0.03 | 0.02 ± 0.01 | 0.95 ± 0.15 | 5 |
| Tropisetron, 10 μM | 0.61 ± 0.03 | 0.01 ± 0.01 | 25.6 ± 2.2 | 2 |
| diMeOBA, 100 μM | 0.52 ± 0.17 | 0.03 ± 0.03 | 2.97 ± 0.38 | 4 |
| Lobeline, 100 μM | 0.07 ± 0.02 | 0.21 ± 0.06 | 0.13 ± 0.02 | 6 |
diOHBA, 3-(2,4-dihydroxybenzylidene)anabaseine; 4OH2MeOBA, 3-(4-hydroxy, 2-methoxybenzylidene)anabaseine; tropisetron, (1R,5S)-8-methyl-8-azabicyclo[3.20.1]octan-3-yl-1-methyl-indole-3-carboxylate; diOHBA, 3-(2,4-dihydroxybenzylidene)anabaseine; diMeOBA, 3-(2,4-dimethoxybenzylidene)anabaseine; lobeline, 2-[6-(2-hydroxy-2-phenyl-ethyl)-1-methyl-2-piperidyl]-1-phenyl-ethanone.