Fluxametamide 是广谱杀虫剂，是 GABA-和谷氨酸门控氯离子通道拮抗剂，对M. domestica中 GABACl 和 GluCl 的IC50值分别为 1.95 和 225 ?nM。

Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- and glutamate-gated chloride channels(IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls).

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.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 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.?Overall, fluxametamide is a new type of LGCC antagonist insecticide with excellent safety for mammals at the target-site level.

928783-29-3

C20H16Cl2F3N3O3

474.26

4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3- 异恶唑基]-N-[(甲氧基氨基)亚甲基]-2-甲基苯 甲酰胺

DMSO:125 mg/mL (263.57 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years