Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
Broflanilide is an insecticide and metabolized to desmethyl-broflanilide, which is a potent and selective antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM. Desmethyl-broflanilide shows weak activity against human GABAA α1β2γ2 receptor, the mammalian GABAA α1β3γ2 receptor and human glycine receptor (GlyR) α1β with IC50s of >3 μM, and less potently inhibits GlyR α1-A288Gβ and GlyR α1-A288G (IC50s, 0.706, 0.149 μM)[1].
[1]. Nakao T, et al. Broflanilide: A meta-diamide insecticide with a novel mode of action. Bioorg Med Chem. 2016 Feb 1;24(3):372-7.