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. 2017 Oct 16;92(2):833–844. doi: 10.1007/s00204-017-2089-4

Table 1.

Pharmacological signature of expressed GABAA receptor isoforms

GABAA isoform Sensitivity to positive allosteric modulators Sensitivity to inhibitors
α1β12γL Diazepam+, Propofol+, Allopregnanolone+ SAS+, Bicuculline+, Fipronil+
α1β2γ2L Diazepam+, Propofol+, Allopregnanolone+ Fipronil+
α1β3γ2L Diazepam+, Propofol+, Allopregnanolone+ Fipronil+
α2β2γ2L Diazepam+, Propofol+ Fipronil+
α2β3γ2L Diazepam+, Propofol+, Allopregnanolone+ SASneg, Bicuculline+, Fipronil+, Zn2+neg
α2β3 Diazepamneg, Propofol+, Fipronil+
α4β3γ2L Diazepamneg, Propofol+, Fipronil+
α4β3δ Diazepamneg, Allopregnanolone+, DS2+ Fipronil+
α6β1γ2L Diazepamneg SAS+, Bicuculline+, Fipronil+
α6β2γ2L Diazepamneg, Propofol+ Fipronil+
α6β3γ2L Diazepamneg, Propofol+, Allopregnanolone+ SASneg, Bicuculline+, Fipronil+, Zn2+neg
α6β3 ND Zn2+ positive
α6β3γ1 Diazepamneg, Propofol+ Fipronil+
α6β3δ Diazepamneg, DS2+ Fipronil+

Sensitivity to 10 μM diazepam, 250 nM Allopregnanolone, 100 μM Propofol, 50 μM DS2 (4-chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide), 10 μM Fipronil, 100 μM Bicuculline, 10 μM SAS (salicylidene salicylhydrazide) and 10 μM ZnCl2 was tested on 3–10 cells per subunit combination

ND Not determined