Effects of kdr (L1014F) and superkdr mutations on pyrethroid sensitivity of D. melanogaster Na+ channel
| Wild-Type | L1014F | M918T | T929I | M918T+L1014F | T929I+L1014F | |
|---|---|---|---|---|---|---|
| Deltamethrin | ||||||
| Kd (nma) | 4.7 ± 0.1 | 90 ± 2.1 | 995 ± 29 | 45 ± 1.1 | 479 ± 10 | 1.5 ± 1.1 mMb |
| n H | 2c | 1.8 ± 0.14 | 0.8 ± 0.1 | 0.8 ± 0.1 | 0.9 ± 0.03 | 0.3 ± 0.04 |
| Tail decay (s) - 110 mV) | τ1 = 1.9 ± 0.3d | τ1 = 1.9 ± 0.3d | 0.61 ± 0.03 | 0.96 ± 0.02 | 0.55 ± 0.01 | 1.16 ± 0.02 |
| τ2 = 215 ± 63d | τ2 = 7.4 ± 0.7e | |||||
| Permethrin | ||||||
| Kd (nMa) | 11.9 ± 0.8 | 48.3 ± 1.2 | —b | 150.4 ± 9.9 | —b | 2.3 ± 9.5 mMc |
| n H | 1.03 ± 0.07 | 0.98 ± 0.16 | 0.9 ± 0.05 | 0.29 ± 0.06 | ||
| Tail decay (ms) (−110 mV) | 746 ± 18 | 233 ± 8 | 96.8 ± 3.4 | 91.1 ± 3.2 | 86.6 ± 3 | 114.3 ± 12.7 |
↵ a Valid for all Kd values given in this table, except those in the last column (data for the T929I+L1014F mutant).
↵ b It was not possible accurately to determine Kd because of the poor solubility of the pyrethroids in aqueous solution.
↵ c Because of the damaging effects of high concentrations of deltamethrin on oocytes expressing the wild-type channel, it was not possible to obtain a plateau for the concentration-response relationship. As a result, the relationship was fitted by iteration with a fixed value for the Hill coefficient nH.
↵ d Values determined at 5 nM deltamethrin.
↵ e Values determined at 1 μM deltamethrin.