Indazapyroxamet is an orally active insect TRPV channel (Nan/Iav subunit) modulator and insecticide. Indazapyroxamet antagonizes nicotinamide-induced calcium influx, inhibits insect motor function, and impairs negative geotaxis in wild-type Drosophila melanogaster via functional TRPV channels [1].
In Vivo, Indazapyroxamet (50-400 μM; p.o.; single 3-hour feeding) induces dose-dependent impairment of negative geotaxis in wild-type Drosophila with a climbing index reduction to ~0.18 at 400 μM, and this behavioral effect requires functional TRPV channels as it is completely abolished in Nan and Iav loss-of-function mutants[1].
In Vitro, Indazapyroxamet (10 min) acts as a low-efficacy partial agonist (EC50=13.1 nM) and potent antagonist (IC50=8.1 nM) of the brown planthopper TRPV channel expressed in Drosophila S2 cells[1]. Indazapyroxamet binds to the brown planthopper TRPV channel in a pocket overlapping that of known agonists, forming a π-stacking interaction with NlIavW322 but lacking critical interactions with NlNanY178, which explains its partial agonist and antagonistic activity[1].
References:
[1]. Zhou T, et al. Functional and genetic validation for indazapyroxamet as an antagonist of insect TRPV channels[J]. Pesticide Biochemistry and Physiology, 2026: 107177.
In Vivo, Indazapyroxamet (50-400 μM; p.o.; single 3-hour feeding) induces dose-dependent impairment of negative geotaxis in wild-type Drosophila with a climbing index reduction to ~0.18 at 400 μM, and this behavioral effect requires functional TRPV channels as it is completely abolished in Nan and Iav loss-of-function mutants[1].
In Vitro, Indazapyroxamet (10 min) acts as a low-efficacy partial agonist (EC50=13.1 nM) and potent antagonist (IC50=8.1 nM) of the brown planthopper TRPV channel expressed in Drosophila S2 cells[1]. Indazapyroxamet binds to the brown planthopper TRPV channel in a pocket overlapping that of known agonists, forming a π-stacking interaction with NlIavW322 but lacking critical interactions with NlNanY178, which explains its partial agonist and antagonistic activity[1].
References:
[1]. Zhou T, et al. Functional and genetic validation for indazapyroxamet as an antagonist of insect TRPV channels[J]. Pesticide Biochemistry and Physiology, 2026: 107177.