Leptophos oxon

Leptophos oxon, a metabolite of leptophos, is a GABA_A receptor chloride channel inhibitor with an IC₅₀ values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABA_A receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease^[2]. In Vitro:Leptophos oxon (15 min pre-incubation) inhibits GABAa receptor-mediated ³⁶Cl^- influx in rat brain membrane microsacs with an IC₅₀ of 89.6 ± 30.4 μM^[2].
Leptophos oxon (90 min) inhibits [³⁵S]TBPS binding to rat brain GABAₐ receptors with an IC₅₀ of 13.4 ± 0.1 μM^[2].
Leptophos oxon (60 min) inhibits [³⁵S]TBPS binding to voltage-dependent Cl^- channels in Torpedo californica electric organ membranes with an IC₅₀ of 2.4 ± 0.1 μM, with maximum inhibition reaching 70-80% of control^[2]. In Vivo:Leptophos oxon (25 mg/kg of leptophos; p.o.) is a minor metabolite of leptophos in female Swiss mice, representing less than 1% of total recovered radioactivity and excreted exclusively in feces^[1].