Figure 1.
Inhibition of GABAA current by fipronil and its derivatives. A) Whole-cell patch-clamp recordings showing the inhibition of GABA-induced Cl− currents by fipronil (top), fipronil desulfinyl imidate (middle) and hydroxy-fipronil (bottom) at concentrations of 100 nM and 1000 nM. Scale bars indicate 1 nA and 5 s, respectively. B) Concentration-response curves showing the percentage of α1β3γ2L GABAA currents blocked by increasing concentrations of fipronil, fipronil desulfinyl imidate and or hydroxy-fipronil. The inhibitory EC50 values are 1.2 ± 0.2 nM (n = 6) for fipronil, 2.8 ± 1.4 nM (n = 23) for fipronil desulfinyl imidate, and 1000 ± 341 nM (n = 7) for hydroxy-fipronil.