Fluxametamide is a new type of LGCC (ligand-gated chloride channel) antagonist insecticide with excellent safety for mammals at the target-site level. Fluxametamide potently inhibited the specific binding of [3H]EBOB to housefly-head membranes, suggesting that fluxametamide affects insect γ-aminobutyric acid (GABA)-gated chloride channels (GABACls). Next, the antagonism of housefly GABACls and glutamate-gated chloride channels (GluCls) was examined using the two-electrode voltage clamp (TEVC) method. Fluxametamide inhibited agonist responses in both ion channels expressed in Xenopus oocytes in the nanomolar range, indicating that this insecticide is a ligand-gated chloride channel (LGCC) antagonist. Fluxametamide exerts distinctive antagonism of arthropod GABACls by binding to a site different from those for existing antagonists. In contrast to its profound actions on the arthropod LGCCs, the antagonistic activity of fluxametamide against rat GABACls and human glycine-gated chloride channels was nearly insignificant, suggesting that fluxametamide has high target-site selectivity for arthropods over mammals[1].
Fluxametamide/氟甲酰胺 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Drosophila melanogaster
Rdl point mutants
Oral (via sucrose solution)
5.6 mg/L
Single exposure for 48 hours
Assessed susceptibility of Rdl mutants to fluxametamide, revealing significant resistance in I276C (RR=12.6) and moderate resistance in I276F+G279S double mutant (RR=4.5).
Insects. 2024 May 6;15(5):334
Fall armyworm (Spodoptera frugiperda)
Laboratory-selected resistant strain
Diet incorporation assay
0.024–0.063 mg/L
Continuous selection for 10 generations
To assess the resistance risk and fitness costs of fluxametamide in FAW. Results showed that after 10 generations of selection, the resistance factor was only 2.63-fold, and the realized heritability was low (h2=0.084). Additionally, the resistant strain showed no significant cross-resistance to other insecticides except emamectin benzoate.
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