Table 1.
Agonist actions of acetylcholine and neonicotinoids on fruit fly, honeybee, and bumblebee nAChRs
Acetylcholine | Imidacloprid | Thiacloprid | Clothianidin | ||||
nAChRs | pEC50 | pEC50 | Imax | pEC50 | Imax | pEC50 | Imax |
Fruit fly (D. melanogaster) | |||||||
Dα1/Dβ1 | 5.12 ± 0.02a,* | 6.76 ± 0.23ab | 0.112 ± 0.009a | 7.64 ± 0.18ab | 0.065 ± 0.005a | 7.21 ± 0.12a | 0.296 ± 0.013a |
Dα1/Dβ1(R81T) | 5.48 ± 0.04† | 6.06 ± 0.12† | 0.032 ± 0.002† | 7.01 ± 0.09† | 0.015 ± 0.001† | 5.33 ± 0.11† | 0.326 ± 0.017 |
Dα1/Dα2/Dβ1 | 4.29 ± 0.04b | 6.39 ± 0.18a | 0.046 ± 0.004ab | 6.63 ± 0.17c | 0.020 ± 0.002bc | 5.53 ± 0.07b | 0.467 ± 0.021b |
Dα1/Dα2/Dβ1(R81T) | 4.68 ± 0.04† | 5.76 ± 0.15 | 0.023 ± 0.002 | 6.44 ± 0.18 | 0.017 ± 0.002 | ND‡ | ND |
Dα1/Dβ1/Dβ2 | 4.82 ± 0.02c | 6.97 ± 0.21ab | 0.244 ± 0.022c | 7.73 ± 0.19ab | 0.056 ± 0.005ab | 6.66 ± 0.07c | 0.411 ± 0.011bc |
Dα1/Dβ1(R81T)/Dβ2 | 5.33 ± 0.03† | 5.65 ± 0.25† | 0.025 ± 0.003† | 7.29 ± 0.09 | 0.0057 ± 0.0003† | ND | ND |
Dα1/Dα2/Dβ1/Dβ2 | 5.22 ± 0.07a | 6.92 ± 0.12ab | 0.592 ± 0.030d | 7.15 ± 0.08ac | 0.454 ± 0.019d | 6.51 ± 0.05cd | 0.821 ± 0.017d |
Dα1/Dα2/Dβ1(R81T)/Dβ2 | 4.95 ± 0.04† | 5.69 ± 0.18† | 0.081 ± 0.006† | 7.07 ± 0.12 | 0.014 ± 0.001† | 5.49 ± 0.04† | 0.951 ± 0.022† |
Honeybee (A. mellifera) | |||||||
Amα1/Amα8/Amβ1 | 5.94 ± 0.04e | 7.63 ± 0.13b | 0.075 ± 0.004a | 7.94 ± 0.19ab | 0.058 ± 0.006ab | 7.96 ± 0.07e | 0.788 ± 0.020d |
Amα1/Amα2/Amα8/Amβ1 | 5.72 ± 0.03f | 7.48 ± 0.16b | 0.070 ± 0.005a | 8.16 ± 0.13b | 0.037 ± 0.003bc | 8.09 ± 0.09e | 0.766 ± 0.024de |
Bumblebee (B. terrestris) | |||||||
Btα1/Btα8/Btβ1 | 5.80 ± 0.03ef | 7.60 ± 0.26b | 0.107 ± 0.010a | 7.29 ± 0.26abc | 0.094 ± 0.008a | 7.87 ± 0.06ef | 0.759 ± 0.018de |
Btα1/Btα2/Btα8/Btβ1 | 5.66 ± 0.03f | 7.40 ± 0.20b | 0.085 ± 0.007a | 7.14 ± 0.38ac | 0.092 ± 0.011a | 7.41 ± 0.10ag | 0.680 ± 0.029e |
Data are represented as mean ± SEM (n = 5).
Different letters (a−g) indicate that pEC50 and Imax data for each ligand differ between the wild-type nAChRs compared (one-way ANOVA, Tukey test, P < 0.05).
Indicates that data for the R81T mutant differ from that for the corresponding wild-type nAChR in D. melanogaster (two-way ANOVA, Bonferroni test, P < 0.05).
ND: could not be determined with accuracy because the concentration–response curve did not attain a maximum.