Table 2.
GABAA receptor subtype | Single-channel conductance (pS) | GABA EC50 (µM) | Hill coefficient | Characteristic time of desensitization td (s) | Characteristic time of deactivation (ms) | Activation time (ms) |
---|---|---|---|---|---|---|
α1β1γ1 | 1.2 [167] | |||||
α1β1γ2 | 30 [100] |
4.5 [167] 6 [100] |
1.2 [100] |
0.492 [100] ([GABA] = 1 mM) 0.6 [103] ([GABA] = 100 µM) |
20.5 [100] 17.4 [103] |
1.1 [100] 1 [103] (γ2S splice variant) |
α1β1γ3 | 0.6 [167] | |||||
α1β2γ1 | 0.67 [167] (human γ1, rat α1 and β2, expressed in 293 cells) | |||||
α1β2γ2 |
32 [152] 27.9 [56] (γ2S splice variant) |
5 [172] 7 [110] (γ2S splice variant) 1.71 [177] |
1.6 [110] (γ2S splice variant) 2.12 [152] |
1.4 [110] (γ2S splice variant) | 220 [110] (γ2S splice variant) | |
α1β2γ3 | 30.2 [178] | 1.3 [167] | ||||
α1β2δ | 6.71 [179] | |||||
α1β3γ1 | 2.1 [167] | |||||
α1β3γ2 |
28 [56] (γ2S splice variant) 27.5 [180] |
1.7 [167] 2.9 [151] (γ2S splice variant) 7.6 [181] (γ2L splice variant) 14 [112] (γ2L splice variant) 36.2 [158] (γ2L splice variant) 14.1 [122] (γ2L splice variant) |
1.7 [158] (γ2L splice variant) |
0.424 [111] (average of 1 and 3 mM of GABA, γ2L splice variant) 0.95 [112] (γ2L splice variant, 1 mM of GABA) |
68.6 [111] (γ2L splice variant) 143 [112] (γ2L splice variant) 82.5 [122] (γ2L splice variant) |
0.55 [101] (γ2L splice variant) 0.603 [111] (γ2L splice variant) |
α1β3δ | 27.5 [180] | 7.4 [181] |
63.4 [181] 86.8 [123] |
|||
α2β1γ2 | 30 [100] |
17 [184] 37 [100] |
1.8 [100] | 0.449 [100] ([GABA] = 1 mM) |
198.7 [100] 82 (type 1) or 51 (type 2) [103] |
0.5 [100] 0.5 [103] (γ2S splice variant) |
α2β1ε | 11.2 [185] | |||||
α2β2γ2 | 1.47 [177] | |||||
α2β3γ2 | 5.2 [151] (γ2S splice variant) | 0.391 [111] (average of 1 and 3 mM of GABA, γ2L splice variant) | 110.6 [111] (γ2L splice variant) | 0.735 [111] (γ2L splice variant) | ||
α3β1γ2 | 15.1 [167] (human α3, rat γ2 and β1, expressed in 293 cells) | |||||
α3β2γ2 |
130 [187] 15.1 [167] (human α3, rat γ2 and β2, expressed in 293 cells) 75 [110] (γ2S splice variant) 2.21 [177] |
1.5 [110] (γ2S splice variant) 1.1 [187] |
3.2 [110] (γ2S splice variant) | 680 [110] (γ2S splice variant) | ||
α3β3γ2 | 48 [151] (γ2S splice variant) | 0.701 [111] (average of 1 and 3 mM of GABA, γ2S splice variant) | 188.8 [111] (γ2L splice variant) | 1.788 [111] (γ2L splice variant) | ||
α4β1γ2 | 1.40 [177] | |||||
α4β1δ |
0.30 [188] 0.17 [177] |
1.57 [188] | 174 [177] | |||
α4β2γ2 |
3.9 [189] 1.4 [167] |
|||||
α4β2δ | 0.25 [179] | |||||
α4β3γ2 |
7.6 [151] (γ2S splice variant) 15 [112] (γ2L splice variant) |
0.408 [111] (average of 1 and 3 mM of GABA, γ2L splice variant) 0.711 [112] (γ2L splice variant, 1 mM of GABA) |
24.8 [111] (γ2L splice variant) 109 [112] (γ2L splice variant) |
0.951 [111] (γ2L splice variant) | ||
α4β3δ | 0.35 [188] | 1.8 [188] | ||||
α5β1γ2 | 5.6 [167] | |||||
α5β2γ2 |
5.8 [187] 4.2 [167] 0.47 [177] |
1.5 [187] | ||||
α5β2γ3 | 4.9 [190] | 1.9 [190] | ||||
α5β3γ2 | 24.9 [180] | 11.6 [151] (γ2S splice variant) | 1.315 [111] (average of 1 and 3 mM of GABA, γ2L splice variant) | 41.5 [111] (γ2L splice variant) | 1.247 [111] (γ2L splice variant) | |
α6β1γ2 | 0.5 [167] | |||||
α6β2γ1 | 0.4 [167] | |||||
α6β2γ2 |
5.2 [156] (γ2S splice variant) 1.4 [189] 0.34 [172] 0.50 [179] (γ2S splice variant) |
|||||
α6β2δ |
0.52 [156] (γ2S splice variant) 1.2 [167] 0.21 [179] |
|||||
α6β3γ2 | 1 [151] (γ2S splice variant) | 0.596 [111] (average of 1 and 3 mM of GABA, γ2L splice variant) | 163.8 [111] (γ2L splice variant) | 1.052 [111] (γ2L splice variant) | ||
α6β3δ | 340.4 [123] | |||||
ρ1 | 1.7 [116] | 3.5 [116] | 14.5 [116] (30 µM of GABA) | 154 [116] | ||
ρ2 | 2.6 [116] | 3.3 [116] | 8.2 [116] (30 µM of GABA) | 180 [116] |
Roman: rat subunits; bold: human subunits; bold italics: mouse subunits. The Hill coefficient, GABA EC50, main conductance state and characteristic times of activation, deactivation and desensitization of the most abundant subtypes in vivo, i.e. ternary subtypes and ρ homopentamers, are presented. Information on other subtypes can be found in [13, 103, 112, 114, 116, 123, 125, 130, 146, 152–157, 176, 180, 182, 191, 192]