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The insect GABA-gated chloride channel is a pentameric ligand-gated ion channel (pLGIC) that mediates inhibitory neurotransmission in the insect nervous system. Its primary endogenous ligand is γ-aminobutyric acid (GABA), which, upon binding, opens the channel to allow chloride ions (Cl⁻) to flow into the neuron, resulting in hyperpolarization and reduced neuronal excitability. It is a major target for insecticides, including cyclodienes, phenylpyrazoles, and isoxazolines. Resistance to these insecticides often arises from mutations in the channel pore region. Differences between insect and mammalian GABA-gated chloride channels underpin the selective toxicity of some insecticides.
Agonist binding leading to Cl- influx and hyperpolarization (GABA). Non-competitive antagonism blocking the channel pore or stabilizing non-conducting conformations (cyclodienes, phenylpyrazoles, isoxazolines).
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