γ-Lindane

γ-Lindane is an organochloro insecticide that is an antagonist of GABA_A receptors.¹ It inhibits GABA-stimulated chloride uptake by membrane vesicles isolated from rat cerebral cortex (IC₅₀ = 68 μM). It binds selectively to insect GABA_A receptors over mammalian GABA_A receptors in membrane preparations (IC₅₀s = 1, 12, 505, 833, and 150-1, 675 nM for fruit fly, house fly, human, mouse, and rat, respectively).^2,3 It binds to a human recombinant β₃ homooligomer with similar selectivity as α₁β₃γ₂-containing receptors, indicating that the binding site for γ-lindane on GABA_A receptors is located on the β₃ subunit (IC₅₀s = 0.90, 21, and 306 nM for β₃, α₁β₃γ₂, and the native receptor, respectively).⁴ γ-Lindane blocks GABA- and glutamate-induced current responses in American cockroach neurons (IC₅₀s = 1.74 and 148 nM, respectively).⁵ It is toxic to mice and adult house flies (LD₅₀s = 40 and 5.5 mg/kg, respectively) and also kills head lice in vitro and inhibits hatching.^4,6

WARNING This product is not for human or veterinary use.

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