Gamma-aminobutyric acid-gated chloride channel (RDL) (RDL)

The cockroach GABA-gated chloride channel is a pentameric transmembrane protein belonging to the Cys-loop ligand-gated ion channel (LGIC) superfamily (UniProt: P22523). It is primarily encoded by the RDL (Resistance to dieldrin) gene and serves as the principal mediator of fast inhibitory neurotransmission in the insect central nervous system (PubMed: 17069845). Upon binding of the neurotransmitter gamma-aminobutyric acid (GABA), the channel undergoes a conformational change that allows the selective passage of chloride ions into the neuron, resulting in hyperpolarization and inhibition of action potentials (PubMed: 25530077). This receptor is a major molecular target for various insecticide classes, including cyclodienes (e.g., dieldrin), fiproles (e.g., fipronil), and isoxazolines (e.g., fluralaner), which act as non-competitive antagonists by binding within the ion pore and preventing chloride conductance (PubChem: CID 3352). The resulting over-excitation of the nervous system leads to paralysis and death in cockroaches and other pests. Because of its distinct pharmacological profile compared to mammalian GABA receptors, it serves as a key site for developing selective pest control agents (PubMed: 10936505). However, widespread use of these chemicals has led to the emergence of resistance, often linked to specific point mutations within the channel's pore-lining region (PubMed: 11158375).

Other names

RDL receptorResistance to dieldrin proteinIonotropic GABA receptorGABA receptor subunit RDLGABA-gated chloride channel

Non-competitive antagonism of the chloride channel pore