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.

Signaling Pathways >> Membrane Transporter/Ion Channel >> Chloride Channel

Research Areas >> Others

IC50: 1.95  nM (M. domestica GABACls), 225  nM (M. domestica GluCls)[1]

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].

Fluxametamide shows significant insecticidal activity with an LD50 (LD95) value of 12.9 ± 4.9 ng/fly (38.7 ± 6.3  ng/fly)[1].

[1]. MihoAsahi, et al. Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels. Pesticide Biochemistry and Physiology.

Shikonine | IAA-94 | Flufenamic Acid | CaCCinh-A01 | NPPB | Lubiprostone | Niflumic acid | Adjudin | Chlorotoxin TFA | Meticrane | H100 | NS1652