Fluxametamide

Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC₅₀ of 1.95 nM and 225 nM for M. domestica GABACls and GluCls. IC50 & Target: IC50: 1.95 nM (M. domestica GABACls), 225 nM (M. domestica GluCls)^[1] In Vitro: Fluxametamide is an antagonist of GABA- and glutamate-gated chloride channels, dose-dependently inhibits currents induced by GABA and glutamate in M. domestica GABACls and GluCls, with IC₅₀ values of 1.95 (1.18-3.21) nM and 225 (137-372) nM, respectively, and displays potent antagonistic activity against T. urticae GABACls with an IC₅₀ of 0.219 (0.127-0.381) nM. Fluxametamide inhibits GABA responses in the wild-type L. striatellus GABACls with IC₅₀ values of 1.40 (0.57-3.29) nM; in the A2′N mutant GABACls, the IC₅₀ value is 3.51 (2.17-5.69) nM. Moreover, Fluxametamide scarcely inhibits GABA (EC₅₀)-induced currents in rat GABACls at 10 μM and with no inhibition on glycine (EC₅₀)-induced current in human α1 GlyCls at tested concentrations^[1]. In Vivo: Fluxametamide shows significant insecticidal activity with an LD₅₀ (LD₉₅) value of 12.9 ± 4.9 ng/fly (38.7 ± 6.3 ng/fly)^[1].