GABA Rdl receptors as targets for novel negative allosteric modulators with pore-blocking potential
GABA type A receptors (GABAARs) are ligand-gated pentameric ion channels found throughout vertebrate and invertebrate nervous systems. Although their structure and function are highly conserved, they can be selectively modulated. Among insect GABA receptors, the Rdl variant has received significant attention, and recent studies have shown its ability to form functional channels with LCCH3 subunits. Mutations like A302S on GABA Rdl of Drosophila confer resistance to various insecticides. Thus, the search for novel compounds able to avoid this resistance mechanism becomes urgent. Due to a lack o